Structural evolution of ionizable lipids for nucleic acid delivery

Wait 5 sec.

Opalinska, J. B. & Gewirtz, A. M. Nucleic-acid therapeutics: basic principles and recent applications. Nat. Rev. Drug. Discov. 1, 503–514 (2002).Article  PubMed  Google Scholar Kulkarni, J. A. et al. The current landscape of nucleic acid therapeutics. Nat. Nanotechnol. 16, 630–643 (2021).Article  PubMed  Google Scholar Junt, T. & Barchet, W. Translating nucleic acid-sensing pathways into therapies. Nat. Rev. Immunol. 15, 529–544 (2015).Article  PubMed  Google Scholar Mendes, B. B. et al. Nanodelivery of nucleic acids. Nat. Rev. Methods Primer 2, 24 (2022).Article  Google Scholar Sridharan, K. & Gogtay, N. J. Therapeutic nucleic acids: current clinical status. Br. J. Clin. Pharmacol. 82, 659–672 (2016).Article  PubMed  PubMed Central  Google Scholar Li, M. et al. Nucleic acid tests for clinical translation. Chem. Rev. 121, 10469–10558 (2021).Article  PubMed  Google Scholar Corey, D. R., Damha, M. J. & Manoharan, M. Challenges and opportunities for nucleic acid therapeutics. Nucleic Acid. Ther. 32, 8–13 (2022).Article  PubMed  Google Scholar Gewirtz, A. M., Sokol, D. L. & Ratajczak, M. Z. Nucleic acid therapeutics: state of the art and future prospects. Blood 92, 712–736 (1998).Article  PubMed  Google Scholar Lu, M., Xing, H., Zheng, A., Huang, Y. & Liang, X.-J. Overcoming pharmaceutical bottlenecks for nucleic acid drug development. Acc. Chem. Res. 56, 224–236 (2023).Article  PubMed  Google Scholar Mollé, L. M., Smyth, C. H., Yuen, D. & Johnston, A. P. R. Nanoparticles for vaccine and gene therapy: overcoming the barriers to nucleic acid delivery. WIREs Nanomed. Nanobiotechnol. 14, e1809 (2022).Article  Google Scholar Zhang, H., Vandesompele, J., Braeckmans, K., De Smedt, S. C. & Remaut, K. Nucleic acid degradation as barrier to gene delivery: a guide to understand and overcome nuclease activity. Chem. Soc. Rev. 53, 317–360 (2024).Article  PubMed  Google Scholar Weng, Y. et al. Improved nucleic acid therapy with advanced nanoscale biotechnology. Mol. Ther. Nucleic Acids 19, 581–601 (2020).Article  PubMed  Google Scholar Schlich, M. et al. Cytosolic delivery of nucleic acids: the case of ionizable lipid nanoparticles. Bioeng. Transl. Med. 6, e10213 (2021).Article  PubMed  PubMed Central  Google Scholar Kumar, R. et al. Polymeric delivery of therapeutic nucleic acids. Chem. Rev. 121, 11527–11652 (2021).Article  PubMed  Google Scholar Cullis, P. R. & Felgner, P. L. The 60-year evolution of lipid nanoparticles for nucleic acid delivery. Nat. Rev. Drug. Discov. 23, 709–722 (2024).Article  PubMed  Google Scholar Nguyen, J. & Szoka, F. C. Nucleic acid delivery: the missing pieces of the puzzle? Acc. Chem. Res. 45, 1153–1162 (2012).Article  PubMed  PubMed Central  Google Scholar Felnerova, D., Viret, J.-F., Glück, R. & Moser, C. Liposomes and virosomes as delivery systems for antigens, nucleic acids and drugs. Curr. Opin. Biotechnol. 15, 518–529 (2004).Article  PubMed  Google Scholar Sun, D. & Lu, Z.-R. Structure and function of cationic and ionizable lipids for nucleic acid delivery. Pharm. Res. 40, 27–46 (2023).Article  PubMed  PubMed Central  Google Scholar Woodle, M. C. & Scaria, P. Cationic liposomes and nucleic acids. Curr. Opin. Colloid Interface Sci. 6, 78–84 (2001).Article  Google Scholar Rao, N. M. Cationic lipid-mediated nucleic acid delivery: beyond being cationic. Chem. Phys. Lipids 163, 245–252 (2010).Article  PubMed  Google Scholar Bailey, A. L. & Cullis, P. R. Modulation of membrane fusion by asymmetric transbilayer distributions of amino lipids. Biochemistry 33, 12573–12580 (1994).Article  PubMed  Google Scholar Cullis, P. R. & Hope, M. J. Lipid nanoparticle systems for enabling gene therapies. Mol. Ther. 25, 1467–1475 (2017).Article  PubMed  PubMed Central  Google Scholar Wang, C., Zhang, Y. & Dong, Y. Lipid nanoparticle–mRNA formulations for therapeutic applications. Acc. Chem. Res. 54, 4283–4293 (2021).Article  PubMed  PubMed Central  Google Scholar Hou, X., Zaks, T., Langer, R. & Dong, Y. Lipid nanoparticles for mRNA delivery. Nat. Rev. Mater. 6, 1078–1094 (2021).Article  PubMed  PubMed Central  Google Scholar Wan, C., Allen, T. M. & Cullis, P. R. Lipid nanoparticle delivery systems for siRNA-based therapeutics. Drug. Deliv. Transl. Res. 4, 74–83 (2014).Article  PubMed  Google Scholar Anfaal, Z., Khan, Z. A. & Aslam, M. A. FDA approves mRESVIA: embracing the new era of RSV prevention with advanced mRNA technology. Ann. Pharmacother. 59, 676–677 (2025).Article  PubMed  Google Scholar Akinc, A. et al. The Onpattro story and the clinical translation of nanomedicines containing nucleic acid-based drugs. Nat. Nanotechnol. 14, 1084–1087 (2019).Article  PubMed  Google Scholar Tenchov, R., Bird, R., Curtze, A. E. & Zhou, Q. Lipid nanoparticles — from liposomes to mRNA vaccine delivery, a landscape of research diversity and advancement. ACS Nano 15, 16982–17015 (2021).Article  PubMed  Google Scholar Verma, M. et al. The landscape for lipid-nanoparticle-based genomic medicines. Nat. Rev. Drug. Discov. 22, 349–350 (2023).Article  PubMed  Google Scholar Schoenmaker, L. et al. mRNA-lipid nanoparticle COVID-19 vaccines: structure and stability. Int. J. Pharm. 601, 120586 (2021).Article  PubMed  PubMed Central  Google Scholar Kulkarni, J. A., Witzigmann, D., Chen, S., Cullis, P. R. & Van Der Meel, R. Lipid nanoparticle technology for clinical translation of siRNA therapeutics. Acc. Chem. Res. 52, 2435–2444 (2019).Article  PubMed  Google Scholar Eygeris, Y., Gupta, M., Kim, J. & Sahay, G. Chemistry of lipid nanoparticles for RNA delivery. Acc. Chem. Res. 55, 2–12 (2022).Article  PubMed  Google Scholar Witzigmann, D. et al. Lipid nanoparticle technology for therapeutic gene regulation in the liver. Adv. Drug. Deliv. Rev. 159, 344–363 (2020).Article  PubMed  PubMed Central  Google Scholar Hanafy, B. I. et al. Advancing cellular-specific delivery: machine learning insights into lipid nanoparticles design and cellular tropism. Adv. Healthc. Mater. 14, 2500383 (2025).Article  Google Scholar Zong, Y., Lin, Y., Wei, T. & Cheng, Q. Lipid nanoparticle (LNP) enables mRNA delivery for cancer therapy. Adv. Mater. 35, 2303261 (2023).Article  Google Scholar Kon, E., Ad-El, N., Hazan-Halevy, I., Stotsky-Oterin, L. & Peer, D. Targeting cancer with mRNA–lipid nanoparticles: key considerations and future prospects. Nat. Rev. Clin. Oncol. 20, 739–754 (2023).Article  PubMed  Google Scholar Eygeris, Y., Patel, S., Jozic, A. & Sahay, G. Deconvoluting lipid nanoparticle structure for messenger RNA delivery. Nano Lett. 20, 4543–4549 (2020).Article  PubMed  Google Scholar Xu, L. et al. Lipid nanoparticles for drug delivery. Adv. NanoBiomed Res. 2, 2100109 (2022).Article  Google Scholar Maharjan, R., Kim, K. H., Lee, K., Han, H.-K. & Jeong, S. H. Machine learning-driven optimization of mRNA-lipid nanoparticle vaccine quality with XGBoost/Bayesian method and ensemble model approaches. J. Pharm. Anal. 14, 100996 (2024).Article  PubMed  PubMed Central  Google Scholar Żak, M. M. & Zangi, L. Lipid nanoparticles for organ-specific mRNA therapeutic delivery. Pharmaceutics 13, 1675 (2021).Article  PubMed  PubMed Central  Google Scholar Kim, C., Lee, Y., Lee, H. & Kim, B. Advances in mRNA-lipid nanoparticle engineering for immune cell targeting and immune modulation. Small Methods 9, e01401 (2025).Article  PubMed  Google Scholar Lindsay, K. E. et al. Visualization of early events in mRNA vaccine delivery in non-human primates via PET–CT and near-infrared imaging. Nat. Biomed. Eng. 3, 371–380 (2019).Article  PubMed  Google Scholar Xiao, X. et al. Impact of stimuli-responsiveness on the mRNA delivery efficiency of low-generation dendrimer nanogels. Biomacromolecules 26, 5c01272 (2025).Article  Google Scholar Han, X. et al. An ionizable lipid toolbox for RNA delivery. Nat. Commun. 12, 7233 (2021).Article  PubMed  PubMed Central  Google Scholar Xu, Y., Golubovic, A., Xu, S., Pan, A. & Li, B. Rational design and combinatorial chemistry of ionizable lipids for RNA delivery. J. Mater. Chem. B 11, 6527–6539 (2023).Article  PubMed  Google Scholar Qiu, M., Li, Y., Bloomer, H. & Xu, Q. Developing biodegradable lipid nanoparticles for intracellular mRNA delivery and genome editing. Acc. Chem. Res. 54, 4001–4011 (2021).Article  PubMed  Google Scholar Rietwyk, S. & Peer, D. Next-generation lipids in RNA interference therapeutics. ACS Nano 11, 7572–7586 (2017).Article  PubMed  Google Scholar Zou, Y. et al. Structure–activity relationships of pH-responsive and ionizable lipids for gene delivery. Int. J. Pharm. 617, 121596 (2022).Article  PubMed  Google Scholar Lee, S. M. et al. Structure–activity relationship of ionizable lipids for siRNA and mRNA lipid nanoparticle design. ACS Biomater. Sci. Eng. 11, 4844–4852 (2025).Article  PubMed  PubMed Central  Google Scholar Zhang, Y., Sun, C., Wang, C., Jankovic, K. E. & Dong, Y. Lipids and lipid derivatives for RNA delivery. Chem. Rev. 121, 12181–12277 (2021).Article  PubMed  PubMed Central  Google Scholar Tardi, P., Boman, N. & Cullis, P. Liposomal doxorubicin. J. Drug. Target. 4, 129–140 (1996).Article  PubMed  Google Scholar Smith, J. G., Walzem, R. L. & Bruce German, J. Liposomes as agents of DNA transfer. Biochim. Biophys. Acta Rev. Biomembr. 1154, 327–340 (1993).Article  Google Scholar Malone, R. W., Felgner, P. L. & Verma, I. M. Cationic liposome-mediated RNA transfection. Proc. Natl Acad. Sci. USA 86, 6077–6081 (1989).Article  PubMed  PubMed Central  Google Scholar Zhang, S. et al. Cationic compounds used in lipoplexes and polyplexes for gene delivery. J. Controlled Rel. 100, 165–180 (2004).Article  Google Scholar Balazs, D. A. & Godbey, W. Liposomes for use in gene delivery. J. Drug. Deliv. 2011, 1–12 (2011).Article  Google Scholar Lächelt, U. & Wagner, E. Nucleic acid therapeutics using polyplexes: a journey of 50 years (and beyond). Chem. Rev. 115, 11043–11078 (2015).Article  PubMed  Google Scholar Matsumoto, M. et al. Hybrid vector including polyethylenimine and cationic lipid, DOTMA, for gene delivery. Int. J. Pharm. 363, 58–65 (2008).Article  PubMed  Google Scholar Zou, Y. et al. pH-sensitive, tail-modified, ester-linked ionizable cationic lipids for gene delivery. Biomater. Adv. 139, 212984 (2022).Article  PubMed  Google Scholar Settanni, G., Brill, W., Haas, H. & Schmid, F. pH-dependent behavior of ionizable cationic lipids in mRNA-carrying lipoplexes investigated by molecular dynamics simulations. Macromol. Rapid Commun. 43, 2100683 (2022).Article  Google Scholar Philipp, J. et al. pH-dependent structural transitions in cationic ionizable lipid mesophases are critical for lipid nanoparticle function. Proc. Natl Acad. Sci. USA 120, e2310491120 (2023).Article  PubMed  PubMed Central  Google Scholar Kim, Y. et al. Physiological barriers to nucleic acid therapeutics and engineering strategies for lipid nanoparticle design, optimization, and clinical translation. Pharmaceutics 17, 1309 (2025).Article  PubMed  PubMed Central  Google Scholar Pei, D. Endosomal escape of lipid nanoparticles: a perspective on the literature data. ACS Nano 19, 40293–40303 (2025).Article  PubMed  PubMed Central  Google Scholar Gilleron, J. et al. Image-based analysis of lipid nanoparticle-mediated siRNA delivery, intracellular trafficking and endosomal escape. Nat. Biotechnol. 31, 638–646 (2013).Article  PubMed  Google Scholar Wittrup, A. et al. Visualizing lipid-formulated siRNA release from endosomes and target gene knockdown. Nat. Biotechnol. 33, 870–876 (2015).Article  PubMed  PubMed Central  Google Scholar Johansson, J. M. et al. Cellular and biophysical barriers to lipid nanoparticle mediated delivery of RNA to the cytosol. Nat. Commun. 16, 5354 (2025).Article  PubMed  PubMed Central  Google Scholar He, Z., Liu, Z. & Chen, Y. Chemical design strategy of ionizable lipids for in vivo mRNA delivery. ChemMedChem 19, e202400199 (2024).Article  PubMed  Google Scholar Cheng, X. & Lee, R. J. The role of helper lipids in lipid nanoparticles (LNPs) designed for oligonucleotide delivery. Adv. Drug. Deliv. Rev. 99, 129–137 (2016).Article  PubMed  Google Scholar Tang, X., Zhang, Y. & Han, X. Ionizable lipid nanoparticles for mRNA delivery. Adv. NanoBiomed Res. 3, 2300006 (2023).Article  Google Scholar Mrksich, K., Padilla, M. S. & Mitchell, M. J. Breaking the final barrier: evolution of cationic and ionizable lipid structure in lipid nanoparticles to escape the endosome. Adv. Drug. Deliv. Rev. 214, 115446 (2024).Article  PubMed  PubMed Central  Google Scholar Suzuki, Y. & Ishihara, H. Structure, activity and uptake mechanism of siRNA-lipid nanoparticles with an asymmetric ionizable lipid. Int. J. Pharm. 510, 350–358 (2016).Article  PubMed  Google Scholar Kulkarni, J. A. et al. On the formation and morphology of lipid nanoparticles containing ionizable cationic lipids and siRNA. ACS Nano 12, 4787–4795 (2018).Article  PubMed  Google Scholar Shin, J. E. et al. Transition temperature-guided design of lipid nanoparticles for effective mRNA delivery. ACS Appl. Mater. Interfaces 17, 28012–28024 (2025).Article  PubMed  PubMed Central  Google Scholar Lewis, M. M. et al. Optimization of ionizable lipids for aerosolizable mRNA lipid nanoparticles. Bioeng. Transl. Med. 8, e10580 (2023).Article  PubMed  PubMed Central  Google Scholar Lam, K. et al. Unsaturated, trialkyl ionizable lipids are versatile lipid-nanoparticle components for therapeutic and vaccine applications. Adv. Mater. 35, 2209624 (2023).Article  Google Scholar Akinc, A. et al. A combinatorial library of lipid-like materials for delivery of RNAi therapeutics. Nat. Biotechnol. 26, 561–569 (2008).Article  PubMed  PubMed Central  Google Scholar Semple, S. C. et al. Rational design of cationic lipids for siRNA delivery. Nat. Biotechnol. 28, 172–176 (2010).Article  PubMed  Google Scholar Love, K. T. et al. Lipid-like materials for low-dose, in vivo gene silencing. Proc. Natl Acad. Sci. USA 107, 1864–1869 (2010).Article  PubMed  PubMed Central  Google Scholar He, Z., Le, Z., Liu, Z. & Chen, Y. Multicomponent reaction-based combinatorial chemistry for accelerating the discovery of therapeutic protein and nucleic acid delivery materials. NPG Asia Mater. 17, 14 (2025).Article  Google Scholar Miao, L. et al. Delivery of mRNA vaccines with heterocyclic lipids increases anti-tumor efficacy by STING-mediated immune cell activation. Nat. Biotechnol. 37, 1174–1185 (2019).Article  PubMed  Google Scholar He, Z. et al. A multidimensional approach to modulating ionizable lipids for high-performing and organ-selective mRNA delivery. Angew. Chem. Int. Ed. 135, e202310401 (2023).Article  Google Scholar Vlasova, K. Y. et al. Synthesis of ionizable lipopolymers using split-Ugi reaction for pulmonary delivery of various size RNAs and gene editing. Nat. Commun. 16, 4021 (2025).Article  PubMed  PubMed Central  Google Scholar Xu, Y. et al. Rational design and modular synthesis of biodegradable ionizable lipids via the Passerini reaction for mRNA delivery. Proc. Natl Acad. Sci. USA 122, e2409572122 (2025).Article  PubMed  PubMed Central  Google Scholar Gong, N. et al. Mannich reaction-based combinatorial libraries identify antioxidant ionizable lipids for mRNA delivery with reduced immunogenicity. Nat. Biomed. Eng. 9, 2181–2195 (2025).Article  PubMed  Google Scholar Han, X. et al. Fast and facile synthesis of amidine-incorporated degradable lipids for versatile mRNA delivery in vivo. Nat. Chem. 16, 1687–1697 (2024).Article  PubMed  PubMed Central  Google Scholar Han, X. et al. Optimization of the activity and biodegradability of ionizable lipids for mRNA delivery via directed chemical evolution. Nat. Biomed. Eng. 8, 1412–1424 (2024).Article  PubMed  Google Scholar Dong, Y. et al. Lipopeptide nanoparticles for potent and selective siRNA delivery in rodents and nonhuman primates. Proc. Natl Acad. Sci. USA 111, 3955–3960 (2014).Article  PubMed  PubMed Central  Google Scholar Miyasaki, K. et al. Formulation methods for peptide-modified lipid nanoparticles. J. Controlled Rel. 385, 114030 (2025).Article  Google Scholar Qin, J. et al. RGD peptide-based lipids for targeted mRNA delivery and gene editing applications. RSC Adv. 12, 25397–25404 (2022).Article  PubMed  PubMed Central  Google Scholar Lin, Y. et al. Tissue-specific mRNA delivery and prime editing with peptide–ionizable lipid nanoparticles. Nat. Mater. 25, 133–145 (2025).Article  PubMed  Google Scholar Xu, S. et al. Tumor-tailored ionizable lipid nanoparticles facilitate IL-12 circular RNA delivery for enhanced lung cancer immunotherapy. Adv. Mater. 36, 2400307 (2024).Article  Google Scholar Hashiba, K. et al. Branching ionizable lipids can enhance the stability, fusogenicity, and functional delivery of mRNA. Small Sci. 3, 2200071 (2023).Article  PubMed  Google Scholar Wu, S. et al. Isosteric 3D bicyclo[1.1.1]pentane (BCP) core-based lipids for mRNA delivery and CRISPR/Cas gene editing. J. Am. Chem. Soc. 146, 34733–34742 (2024).Article  PubMed  PubMed Central  Google Scholar Cheng, M. H. Y. et al. Induction of bleb structures in lipid nanoparticle formulations of mRNA leads to improved transfection potency. Adv. Mater. 35, 2303370 (2023).Article  Google Scholar Udepurkar, A. et al. Structure and morphology of lipid nanoparticles for nucleic acid drug delivery: a review. ACS Nano 19, 21206–21242 (2025).Article  PubMed  Google Scholar Wang, M. et al. Enhanced intracellular siRNA delivery using bioreducible lipid-like nanoparticles. Adv. Healthc. Mater. 3, 1398–1403 (2014).Article  PubMed  Google Scholar Liu, S. et al. Membrane-destabilizing ionizable phospholipids for organ-selective mRNA delivery and CRISPR–Cas gene editing. Nat. Mater. 20, 701–710 (2021).Article  PubMed  PubMed Central  Google Scholar Xue, L. et al. Combinatorial design of siloxane-incorporated lipid nanoparticles augments intracellular processing for tissue-specific mRNA therapeutic delivery. Nat. Nanotechnol. 20, 132–143 (2025).Article  PubMed  Google Scholar Chen, Z. et al. Modular design of biodegradable ionizable lipids for improved mRNA delivery and precise cancer metastasis delineation in vivo. J. Am. Chem. Soc. 145, 24302–24314 (2023).Article  PubMed  Google Scholar Chaudhary, N. et al. Amine headgroups in ionizable lipids drive immune responses to lipid nanoparticles by binding to the receptors TLR4 and CD1d. Nat. Biomed. Eng. 8, 1483–1498 (2024).Article  PubMed  PubMed Central  Google Scholar Kim, M. et al. Engineered ionizable lipid nanoparticles for targeted delivery of RNA therapeutics into different types of cells in the liver. Sci. Adv. 7, eabf4398 (2021).Article  PubMed  PubMed Central  Google Scholar Song, D., Zhao, Y., Wang, Z. & Xu, Q. Tuning lipid nanoparticles for RNA delivery to extrahepatic organs. Adv. Mater. 36, 2401445 (2024).Article  Google Scholar Fu, L. et al. ‘Passive’ nanoparticles for organ-selective systemic delivery: design, mechanism and perspective. Chem. Soc. Rev. 52, 7579–7601 (2023).Article  PubMed  PubMed Central  Google Scholar Padilla, M. S. et al. Branched endosomal disruptor (BEND) lipids mediate delivery of mRNA and CRISPR–Cas9 ribonucleoprotein complex for hepatic gene editing and T cell engineering. Nat. Commun. 16, 996 (2025).Article  PubMed  PubMed Central  Google Scholar Samaridou, E., Simon, J., Beck-Broichsitter, M., Davidson, G. & Levkin, P. A. Rational design of unsaturated, thioether ionizable lipids for enhanced in vivo mRNA delivery. Adv. Healthc. Mater. 14, 2501037 (2025).Article  PubMed  PubMed Central  Google Scholar Eygeris, Y. et al. Thiophene-based lipids for mRNA delivery to pulmonary and retinal tissues. Proc. Natl Acad. Sci. USA 121, e2307813120 (2024).Article  PubMed  PubMed Central  Google Scholar Shuvaev, V. V. et al. Systemic delivery of biotherapeutic RNA to the myocardium transiently modulates cardiac contractility in vivo. Proc. Natl Acad. Sci. USA 122, e2409266122 (2025).Article  PubMed  PubMed Central  Google Scholar Somu Naidu, G. et al. Ionizable lipids with optimized linkers enable lung-specific, lipid nanoparticle-mediated mRNA delivery for treatment of metastatic lung tumors. ACS Nano 19, 6571–6587 (2025).Article  PubMed  PubMed Central  Google Scholar Qiu, M. et al. Lung-selective mRNA delivery of synthetic lipid nanoparticles for the treatment of pulmonary lymphangioleiomyomatosis. Proc. Natl Acad. Sci. USA 119, e2116271119 (2022).Article  PubMed  PubMed Central  Google Scholar Dong, W. et al. Multicomponent synthesis of imidazole-based ionizable lipids for highly efficient and spleen-selective messenger RNA delivery. J. Am. Chem. Soc. 146, 15085–15095 (2024).Article  PubMed  Google Scholar Wu, S. et al. Carbonate-bearing ionizable lipids for mRNA delivery to splenic NK cells. J. Am. Chem. Soc. 147, 28665–28673 (2025).Article  PubMed  Google Scholar Xue, L. et al. Multiarm-assisted design of dendron-like degradable ionizable lipids facilitates systemic mRNA delivery to the spleen. J. Am. Chem. Soc. 147, 1542–1552 (2025).Article  PubMed  PubMed Central  Google Scholar Liu, S. et al. Zwitterionic phospholipidation of cationic polymers facilitates systemic mRNA delivery to spleen and lymph nodes. J. Am. Chem. Soc. 143, 21321–21330 (2021).Article  PubMed  PubMed Central  Google Scholar Huo, H. et al. A fluorinated ionizable lipid improves the mRNA delivery efficiency of lipid nanoparticles. J. Mater. Chem. B 11, 4171–4180 (2023).Article  PubMed  Google Scholar Cheng, Q. et al. Selective organ targeting (SORT) nanoparticles for tissue-specific mRNA delivery and CRISPR–Cas gene editing. Nat. Nanotechnol. 15, 313–320 (2020).Article  PubMed  PubMed Central  Google Scholar Dilliard, S. A., Cheng, Q. & Siegwart, D. J. On the mechanism of tissue-specific mRNA delivery by selective organ targeting nanoparticles. Proc. Natl Acad. Sci. USA 118, e2109256118 (2021).Article  PubMed  PubMed Central  Google Scholar Carrasco, M. J. et al. Ionization and structural properties of mRNA lipid nanoparticles influence expression in intramuscular and intravascular administration. Commun. Biol. 4, 956 (2021).Article  PubMed  PubMed Central  Google Scholar Simonsen, J. B. & Larsson, P. A perspective on the apparent pKa of ionizable lipids in mRNA–LNPs. J. Controlled Rel. 384, 113879 (2025).Article  Google Scholar Tilstra, G. et al. Iterative design of ionizable lipids for intramuscular mRNA delivery. J. Am. Chem. Soc. 145, 2294–2304 (2023).Article  PubMed  Google Scholar Swingle, K. L. et al. Placenta-tropic VEGF mRNA lipid nanoparticles ameliorate murine pre-eclampsia. Nature 637, 412–421 (2025).Article  PubMed  Google Scholar Rhym, L. H., Manan, R. S., Koller, A., Stephanie, G. & Anderson, D. G. Peptide-encoding mRNA barcodes for the high-throughput in vivo screening of libraries of lipid nanoparticles for mRNA delivery. Nat. Biomed. Eng. 7, 901–910 (2023).Article  PubMed  Google Scholar Alzahrani, R. F. et al. Folate- and chitosan-functionalized lipid nanoparticles for co-delivery of pioglitazone and simvastatin to enhance hepatic cancer therapy: effects on IL-1β, IL-6, BCL2/BAX gene expression, and GPX4, COX-2, and MMP-9 activities. Mol. Biol. Rep. 52, 926 (2025).Article  PubMed  Google Scholar Xue, L. et al. Rational design of bisphosphonate lipid-like materials for mRNA delivery to the bone microenvironment. J. Am. Chem. Soc. 144, 9926–9937 (2022).Article  PubMed  Google Scholar Yoon, I. et al. Piperazine-derived bisphosphonate-based ionizable lipid nanoparticles enhance mRNA delivery to the bone microenvironment. Angew. Chem. Int. Ed. 64, e202415389 (2025).Article  Google Scholar Ma, F. et al. Neurotransmitter-derived lipidoids (NT-lipidoids) for enhanced brain delivery through intravenous injection. Sci. Adv. 6, eabb4429 (2020).Article  PubMed  PubMed Central  Google Scholar Wang, C. et al. Intravenous administration of blood–brain barrier-crossing conjugates facilitate biomacromolecule transport into central nervous system. Nat. Biotechnol. 43, 1783–1789 (2025).Article  PubMed  Google Scholar Liu, Z. et al. Furan-derived lipid nanoparticles for transporting mRNA to the central nervous system. J. Am. Chem. Soc. 147, 16007–16017 (2025).Article  PubMed  Google Scholar Xue, Y. et al. Lipid nanoparticles enhance mRNA delivery to the central nervous system upon intrathecal injection. Adv. Mater. 37, 2417097 (2025).Article  Google Scholar Wang, C. et al. Blood–brain-barrier-crossing lipid nanoparticles for mRNA delivery to the central nervous system. Nat. Mater. 24, 1653–1663 (2025).Article  PubMed  PubMed Central  Google Scholar Cao, D. et al. Lipid nanoparticles for mRNA delivery in brain via systemic administration. Sci. Adv. 11, eadw0730 (2025).Article  PubMed  PubMed Central  Google Scholar Geisler, H. C. et al. EGFR-targeted ionizable lipid nanoparticles enhance in vivo mRNA delivery to the placenta. J. Controlled Rel. 371, 455–469 (2024).Article  Google Scholar Parhiz, H. et al. PECAM-1 directed re-targeting of exogenous mRNA providing two orders of magnitude enhancement of vascular delivery and expression in lungs independent of apolipoprotein E-mediated uptake. J. Controlled Rel. 291, 106–115 (2018).Article  Google Scholar Kheirolomoom, A. et al. In situ T-cell transfection by anti-CD3-conjugated lipid nanoparticles leads to T-cell activation, migration, and phenotypic shift. Biomaterials 281, 121339 (2022).Article  PubMed  Google Scholar Tombácz, I. et al. Highly efficient CD4+ T cell targeting and genetic recombination using engineered CD4+ cell-homing mRNA–LNPs. Mol. Ther. 29, 3293–3304 (2021).Article  PubMed  PubMed Central  Google Scholar Rurik, J. G. et al. CAR T cells produced in vivo to treat cardiac injury. Science 375, 91–96 (2022).Article  PubMed  PubMed Central  Google Scholar Zeng, J. et al. Rapid receptor internalization potentiates CD7-targeted lipid nanoparticles for efficient mRNA delivery to T cells and in vivo CAR T-cell engineering. J. Controlled Rel. 396, 115043 (2026).Article  Google Scholar Hunter, T. L. et al. In vivo CAR T cell generation to treat cancer and autoimmune disease. Science 388, 1311–1317 (2025).Article  PubMed  Google Scholar Veiga, N. et al. Cell specific delivery of modified mRNA expressing therapeutic proteins to leukocytes. Nat. Commun. 9, 4493 (2018).Article  PubMed  PubMed Central  Google Scholar Liu, W., Zhang, M., Lv, H. & Yang, C. Formulation-driven optimization of PEG-lipid content in lipid nanoparticles for enhanced mRNA delivery in vitro and in vivo. Pharmaceutics 17, 950 (2025).Article  PubMed  PubMed Central  Google Scholar Hashiba, K. et al. Impact of lipid tail length on the organ selectivity of mRNA-lipid nanoparticles. Nano Lett. 24, 12758 (2024).PubMed  PubMed Central  Google Scholar Su, K. et al. Reformulating lipid nanoparticles for organ-targeted mRNA accumulation and translation. Nat. Commun. 15, 5659 (2024).Article  PubMed  PubMed Central  Google Scholar Zhao, Y. et al. Replacing cholesterol and PEGylated lipids with zwitterionic ionizable lipids in LNPs for spleen-specific mRNA translation. Sci. Adv. 11, eady6460 (2025).Article  PubMed  PubMed Central  Google Scholar Strelkova Petersen, D. M., Chaudhary, N., Arral, M. L., Weiss, R. M. & Whitehead, K. A. The mixing method used to formulate lipid nanoparticles affects mRNA delivery efficacy and organ tropism. Eur. J. Pharm. Biopharm. 192, 126–135 (2023).Article  PubMed  PubMed Central  Google Scholar Liu, K. et al. Multiomics analysis of naturally efficacious lipid nanoparticle coronas reveals high-density lipoprotein is necessary for their function. Nat. Commun. 14, 4007 (2023).Article  PubMed  PubMed Central  Google Scholar Hatit, M. Z. C. et al. Species-dependent in vivo mRNA delivery and cellular responses to nanoparticles. Nat. Nanotechnol. 17, 310–318 (2022).Article  PubMed  PubMed Central  Google Scholar Khalil, I. A., Younis, M. A., Kimura, S. & Harashima, H. Lipid nanoparticles for cell-specific in vivo targeted delivery of nucleic acids. Biol. Pharm. Bull. 43, 584–595 (2020).Article  PubMed  Google Scholar Lee, J. et al. Chirality-controlled lipid nanoparticles for mRNA delivery. ACS Appl. Mater. Interfaces 17, 18150–18159 (2025).Article  PubMed  Google Scholar Hatit, M. Z. C. et al. Nanoparticle stereochemistry-dependent endocytic processing improves in vivo mRNA delivery. Nat. Chem. 15, 508–515 (2023).Article  PubMed  PubMed Central  Google Scholar De, C. K. et al. The overlooked stereoisomers of the ionizable lipid ALC315. J. Am. Chem. Soc. 147, 28595–28600 (2025).Article  PubMed  PubMed Central  Google Scholar Zhang, Z. et al. Cardiolipin-mimic lipid nanoparticles without antibody modification delivered senolytic in vivo CAR-T therapy for inflamm-aging. Cell Rep. Med. 6, 102209 (2025).Article  PubMed  PubMed Central  Google Scholar Ni, H. et al. Piperazine-derived lipid nanoparticles deliver mRNA to immune cells in vivo. Nat. Commun. 13, 4766 (2022).Article  PubMed  PubMed Central  Google Scholar Wang, S. et al. Accelerating diabetic wound healing by ROS-scavenging lipid nanoparticle–mRNA formulation. Proc. Natl Acad. Sci. USA 121, e2322935121 (2024).Article  PubMed  PubMed Central  Google Scholar Cai, W., Luo, T., Chen, X., Mao, L. & Wang, M. A combinatorial library of biodegradable lipid nanoparticles preferentially deliver mRNA into tumor cells to block mutant RAS signaling. Adv. Funct. Mater. 32, 2204947 (2022).Article  Google Scholar Holland, R. et al. Silicon ether ionizable lipids enable potent mRNA lipid nanoparticles with rapid tissue clearance. ACS Nano 18, 10374–10387 (2024).Article  PubMed  PubMed Central  Google Scholar Li, Y. et al. Incorporation of disulfide bonds into ionizable lipids enables efficient splenic mRNA delivery and potent immunotherapy in mice. Chem. Eng. J. 516, 164285 (2025).Article  Google Scholar Zhao, S. et al. Acid-degradable lipid nanoparticles enhance the delivery of mRNA. Nat. Nanotechnol. 19, 1702–1711 (2024).Article  PubMed  PubMed Central  Google Scholar Li, Y. et al. Combinatorial library of cyclic benzylidene acetal-containing pH-responsive lipidoid nanoparticles for intracellular mRNA delivery. Bioconjug. Chem. 31, 1835–1843 (2020).Article  PubMed  PubMed Central  Google Scholar Lv, K. et al. Discovery of ketal-ester ionizable lipid nanoparticle with reduced hepatotoxicity, enhanced spleen tropism for mRNA vaccine delivery. Adv. Sci. 11, 2404684 (2024).Article  Google Scholar Whitehead, K. A. et al. Degradable lipid nanoparticles with predictable in vivo siRNA delivery activity. Nat. Commun. 5, 4277 (2014).Article  PubMed  PubMed Central  Google Scholar Patel, P. et al. Development of amino acid-modified biodegradable lipid nanoparticles for siRNA delivery. Acta Biomater. 154, 374–384 (2022).Article  PubMed  PubMed Central  Google Scholar Maier, M. A. et al. Biodegradable lipids enabling rapidly eliminated lipid nanoparticles for systemic delivery of RNAi therapeutics. Mol. Ther. 21, 1570–1578 (2013).Article  PubMed  PubMed Central  Google Scholar Movahedi, F., Hu, R. G., Becker, D. L. & Xu, C. Stimuli-responsive liposomes for the delivery of nucleic acid therapeutics. Nanomed. Nanotechnol. Biol. Med. 11, 1575–1584 (2015).Article  Google Scholar Golba, B. et al. Visible light conjugation with triazolinediones as a route to degradable poly(ethylene glycol)–lipids for mRNA lipid nanoparticle formulation. Angew. Chem. Int. Ed. 135, e202301102 (2023).Article  Google Scholar Mo, Y. et al. Light-activated siRNA endosomal release (LASER) by porphyrin lipid nanoparticles. ACS Nano 17, 4688–4703 (2023).Article  PubMed  Google Scholar Zhao, Y. et al. Nanomechanical action opens endo-lysosomal compartments. Nat. Commun. 14, 6645 (2023).Article  PubMed  PubMed Central  Google Scholar Chen, F. et al. Ultrasound-activatable lipid nanoplatform for region-confined innate immune stimulation and mRNA vaccination therapy of cancer. J. Am. Chem. Soc. 147, 42221–42236 (2025).PubMed  Google Scholar Zhang, H. et al. Delivery of mRNA vaccine with a lipid-like material potentiates antitumor efficacy through Toll-like receptor 4 signaling. Proc. Natl Acad. Sci. USA 118, e2005191118 (2021).Article  PubMed  PubMed Central  Google Scholar Ripoll, M. et al. An imidazole modified lipid confers enhanced mRNA–LNP stability and strong immunization properties in mice and non-human primates. Biomaterials 286, 121570 (2022).Article  PubMed  PubMed Central  Google Scholar Han, X. et al. Adjuvant lipidoid-substituted lipid nanoparticles augment the immunogenicity of SARS-CoV-2 mRNA vaccines. Nat. Nanotechnol. 18, 1105–1114 (2023).Article  PubMed  Google Scholar Li, B. et al. Enhancing the immunogenicity of lipid-nanoparticle mRNA vaccines by adjuvanting the ionizable lipid and the mRNA. Nat. Biomed. Eng. 9, 167–184 (2023).Article  PubMed  Google Scholar Moku, G., Vangala, S., Gulla, S. K. & Yakati, V. In vivo targeting of DNA vaccines to dendritic cells via the mannose receptor induces long-lasting immunity against melanoma. ChemBioChem 22, 523–531 (2021).Article  PubMed  Google Scholar Das, R. et al. Hybrid LNP prime dendritic cells for nucleotide delivery. Adv. Sci. 10, 2303576 (2023).Article  Google Scholar Lou, G. et al. Delivery of self-amplifying mRNA vaccines by cationic lipid nanoparticles: the impact of cationic lipid selection. J. Controlled Rel. 325, 370–379 (2020).Article  Google Scholar Xu, X. et al. Use of a liver-targeting immune-tolerogenic mRNA lipid nanoparticle platform to treat peanut-induced anaphylaxis by single- and multiple-epitope nucleotide sequence delivery. ACS Nano 17, 4942–4957 (2023).Article  PubMed  PubMed Central  Google Scholar Ju, Y. et al. Anti-PEG antibodies boosted in humans by SARS-CoV-2 lipid nanoparticle mRNA vaccine. ACS Nano 16, 11769–11780 (2022).Article  PubMed  Google Scholar Luozhong, S. et al. Poly(carboxybetaine) lipids enhance mRNA therapeutics efficacy and reduce their immunogenicity. Nat. Mater. 24, 1852–1861 (2025).Article  PubMed  PubMed Central  Google Scholar Xiao, Y. et al. High-density brush-shaped polymer lipids reduce anti-PEG antibody binding for repeated administration of mRNA therapeutics. Nat. Mater. 24, 1840–1851 (2025).Article  PubMed  PubMed Central  Google Scholar Li, Z. et al. Charge-altering releasable transporters enhance mRNA delivery in vitro and exhibit in vivo tropism. Nat. Commun. 14, 6983 (2023).Article  PubMed  PubMed Central  Google Scholar McKinlay, C. J. et al. Charge-altering releasable transporters (CARTs) for the delivery and release of mRNA in living animals. Proc. Natl Acad. Sci. USA 114, E448–E456 (2017).Article  PubMed  PubMed Central  Google Scholar Haabeth, O. A. W. et al. mRNA vaccination with charge-altering releasable transporters elicits human T cell responses and cures established tumors in mice. Proc. Natl Acad. Sci. USA 115, E9153–E9161 (2018).Article  PubMed  PubMed Central  Google Scholar Yang, K. et al. Biodegradable lipid-modified poly(guanidine thioctic acid)s: a fortifier of lipid nanoparticles to promote the efficacy and safety of mRNA cancer vaccines. J. Am. Chem. Soc. 146, 11679–11693 (2024).Article  PubMed  Google Scholar Deyhimfar, R. et al. The clinical impact of mRNA therapeutics in the treatment of cancers, infections, genetic disorders, and autoimmune diseases. Heliyon 10, e26971 (2024).Article  PubMed  PubMed Central  Google Scholar Singh, D. Advances in lipid nanoparticle delivery systems for targeted cytokine immunotherapy in autoimmune disorders. Cytokine 198, 157098 (2026).Article  PubMed  Google Scholar De Picciotto, S. et al. Selective activation and expansion of regulatory T cells using lipid encapsulated mRNA encoding a long-acting IL-2 mutein. Nat. Commun. 13, 3866 (2022).Article  PubMed  PubMed Central  Google Scholar Schulze-Tanzil, G. et al. Interleukin-10 and articular cartilage: experimental therapeutical approaches in cartilage disorders. Curr. Gene Ther. 9, 306–315 (2009).Article  PubMed  Google Scholar Raphael, I., Joern, R. R. & Forsthuber, T. G. Memory CD4+ T cells in immunity and autoimmune diseases. Cells 9, 531 (2020).Article  PubMed  PubMed Central  Google Scholar Koide, H. et al. Engineering of lipid nanoparticles by the multifunctionalization of the surface with amino acid derivatives for the neutralization of a target toxic peptide. Adv. Funct. Mater. 31, 2005641 (2021).Article  Google Scholar Chen, Z. et al. Crown-like biodegradable lipids enable lung-selective mRNA delivery and dual-modal tumor imaging in vivo. J. Am. Chem. Soc. 146, 34209–34220 (2024).Article  PubMed  Google Scholar Dahlman, J. E. et al. Barcoded nanoparticles for high throughput in vivo discovery of targeted therapeutics. Proc. Natl Acad. Sci. USA 114, 2060–2065 (2017).Article  PubMed  PubMed Central  Google Scholar Hamilton, A. G. et al. High-throughput in vivo screening identifies differential influences on mRNA lipid nanoparticle immune cell delivery by administration route. ACS Nano 18, 16151–16165 (2024).Article  PubMed  Google Scholar Xue, L. et al. High-throughput barcoding of nanoparticles identifies cationic, degradable lipid-like materials for mRNA delivery to the lungs in female preclinical models. Nat. Commun. 15, 1884 (2024).Article  PubMed  PubMed Central  Google Scholar Dobrowolski, C. et al. Nanoparticle single-cell multiomic readouts reveal that cell heterogeneity influences lipid nanoparticle-mediated messenger RNA delivery. Nat. Nanotechnol. 17, 871–879 (2022).Article  PubMed  PubMed Central  Google Scholar Hanna, A. R., Issadore, D. A. & Mitchell, M. J. High-throughput platforms for machine learning-guided lipid nanoparticle design. Nat. Rev. Mater. 11, 50–64 (2025).Article  Google Scholar Li, B. et al. Accelerating ionizable lipid discovery for mRNA delivery using machine learning and combinatorial chemistry. Nat. Mater. 23, 1002–1008 (2024).Article  PubMed  Google Scholar Chan, A. et al. Designing lipid nanoparticles using a transformer-based neural network. Nat. Nanotechnol. 20, 1491–1501 (2025).Article  PubMed  PubMed Central  Google Scholar Witten, J. et al. Artificial intelligence-guided design of lipid nanoparticles for pulmonary gene therapy. Nat. Biotechnol. 43, 1790–1799 (2025).Article  PubMed  Google Scholar Xu, Y. et al. AGILE platform: a deep learning powered approach to accelerate LNP development for mRNA delivery. Nat. Commun. 15, 6305 (2024).Article  PubMed  PubMed Central  Google Scholar Wang, W. et al. Artificial intelligence-driven rational design of ionizable lipids for mRNA delivery. Nat. Commun. 15, 10804 (2024).Article  PubMed  PubMed Central  Google Scholar Kumar, G. & Ardekani, A. M. Machine-learning framework to predict the performance of lipid nanoparticles for nucleic acid delivery. ACS Appl. Bio Mater. 8, 3717–3727 (2025).Article  PubMed  Google Scholar Harrison, P. J. et al. Deep-learning dodels for lipid nanoparticle-based drug delivery. Nanomed 16, 1097–1110 (2021).Article  Google Scholar Wang, W. et al. Prediction of lipid nanoparticles for mRNA vaccines by the machine learning algorithm. Acta Pharm. Sin. B 12, 2950–2962 (2022).Article  PubMed  Google Scholar Wu, K. et al. TransMA: an explainable multi-modal deep learning model for predicting properties of ionizable lipid nanoparticles in mRNA delivery. Brief. Bioinform. 26, bbaf307 (2025).Article  PubMed  PubMed Central  Google Scholar Moayedpour, S. et al. Representations of lipid nanoparticles using large language models for transfection efficiency prediction. Bioinformatics 40, btae342 (2024).Article  PubMed  PubMed Central  Google Scholar Cui, K. et al. Iterative screening of vitamin E-based functional lipid nanoparticles for mRNA delivery. ACS Nano 19, 20672–20692 (2025).Article  PubMed  Google Scholar Shepherd, S. J. et al. Scalable mRNA and siRNA lipid nanoparticle production using a parallelized microfluidic device. Nano Lett. 21, 5671–5680 (2021).Article  PubMed  PubMed Central  Google Scholar Huang, X., Ma, Y., Ma, G. & Xia, Y. Unlocking the therapeutic applicability of LNP–mRNA: chemistry, formulation, and clinical strategies. Research 7, 0370 (2024).Article  PubMed  PubMed Central  Google Scholar McKay, P. F. et al. Self-amplifying RNA SARS-CoV-2 lipid nanoparticle vaccine candidate induces high neutralizing antibody titers in mice. Nat. Commun. 11, 3523 (2020).Article  PubMed  PubMed Central  Google Scholar Swingle, K. L. et al. Circular RNA lipid nanoparticle vaccine against SARS-CoV-2. Proc. Natl Acad. Sci. USA 122, e2505718122 (2025).Article  PubMed  PubMed Central  Google Scholar Dilliard, S. A. & Siegwart, D. J. Passive, active and endogenous organ-targeted lipid and polymer nanoparticles for delivery of genetic drugs. Nat. Rev. Mater. 8, 282–300 (2023).Article  PubMed  PubMed Central  Google Scholar Kim, Y. et al. Mannose-conjugated cholesterol containing lipid nanoparticles for active targeted mRNA delivery to liver sinusoidal endothelial and kupffer cells. Bioconjug. Chem. 36, 2181–2196 (2025).Article  PubMed  PubMed Central  Google Scholar Johnson, L. T. et al. Lipid nanoparticle (LNP) chemistry can endow unique in vivo RNA delivery fates within the liver that alter therapeutic outcomes in a cancer model. Mol. Pharm. 19, 3973–3986 (2022).Article  PubMed  PubMed Central  Google Scholar Álvarez-Benedicto, E. et al. Spleen SORT LNP generated in situ CAR T cells extend survival in a mouse model of lymphoreplete B cell lymphoma. Angew. Chem. Int. Ed. 62, e202310395 (2023).Article  Google Scholar Kranz, L. M. et al. Systemic RNA delivery to dendritic cells exploits antiviral defence for cancer immunotherapy. Nature 534, 396–401 (2016).Article  PubMed  Google Scholar Vaidya, A. et al. Endogenous targeting of lipid nanoparticles to kidney tumors. ACS Nano 19, 30860–30871 (2025).Article  PubMed  PubMed Central  Google Scholar Lokugamage, M. P., Sago, C. D., Gan, Z., Krupczak, B. R. & Dahlman, J. E. Constrained nanoparticles deliver siRNA and sgRNA to T cells in vivo without targeting ligands. Adv. Mater. 31, 1902251 (2019).Article  Google Scholar Chen, M. Z. et al. A versatile antibody capture system drives specific in vivo delivery of mRNA-loaded lipid nanoparticles. Nat. Nanotechnol. 20, 1273–1284 (2025).Article  PubMed  PubMed Central  Google Scholar Bangham, A. D. & Horne, R. W. Negative staining of phospholipids and their structural modification by surface-active agents as observed in the electron microscope. J. Mol. Biol. 8, 660–IN10 (1964).Article  PubMed  Google Scholar Uemura, K., Nicolotti, R. A., Six, H. R. & Kinsky, S. C. Antibody formation in response to liposomal model membranes sensitized with N-substituted phosphatidylethanolamine derivatives. Biochemistry 13, 1572–1578 (1974).Article  PubMed  Google Scholar Cullis, P. R. & De Kruijff, B. Lipid polymorphism and the functional roles of lipids in biological membranes. Biochim. Biophys. Acta BBA 559, 399–420 (1979).Article  PubMed  Google Scholar Kielian, M. C., Keränen, S., Kääriäinen, L. & Helenius, A. Membrane fusion mutants of Semliki Forest virus. J. Cell Biol. 98, 139–145 (1984).Article  PubMed  PubMed Central  Google Scholar Felgner, P. L. et al. Lipofection: a highly efficient, lipid-mediated DNA-transfection procedure. Proc. Natl Acad. Sci. USA 84, 7413–7417 (1987).Article  PubMed  PubMed Central  Google Scholar Jayaraman, M. et al. Maximizing the potency of siRNA lipid nanoparticles for hepatic gene silencing in vivo. Angew. Chem. Int. Ed. 51, 8529–8533 (2012).Article  Google Scholar Dahlman, J. E. et al. In vivo endothelial siRNA delivery using polymeric nanoparticles with low molecular weight. Nat. Nanotechnol. 9, 648–655 (2014).Article  PubMed  PubMed Central  Google Scholar Fenton, O. S. et al. Bioinspired alkenyl amino alcohol ionizable lipid materials for highly potent in vivo mRNA delivery. Adv. Mater. 28, 2939–2943 (2016).Article  PubMed  PubMed Central  Google Scholar Zhang, L. et al. Effect of mRNA–LNP components of two globally-marketed COVID-19 vaccines on efficacy and stability. npj Vaccines 8, 156 (2023).Article  PubMed  PubMed Central  Google Scholar Jacob, F. & Monod, J. Genetic regulatory mechanisms in the synthesis of proteins. J. Mol. Biol. 3, 318–356 (1961).Article  PubMed  Google Scholar Lockard, R. E. & Lingrel, J. B. The synthesis of mouse hemoglobin chains in a rabbit reticulocyte cell-free system programmed with mouse reticulocyte 9S RNA. Biochem. Biophys. Res. Commun. 37, 204–212 (1969).Article  PubMed  Google Scholar Nicolau, C., Le Pape, A., Soriano, P., Fargette, F. & Juhel, M. F. In vivo expression of rat insulin after intravenous administration of the liposome-entrapped gene for rat insulin I. Proc. Natl Acad. Sci. USA 80, 1068–1072 (1983).Article  PubMed  PubMed Central  Google Scholar Wolff, J. A. et al. Direct gene transfer into mouse muscle in vivo. Science 247, 1465–1468 (1990).Article  PubMed  Google Scholar Jirikowski, G. F., Sanna, P. P., Maciejewski-Lenoir, D. & Bloom, F. E. Reversal of diabetes insipidus in brattleboro rats: intrahypothalamic injection of vasopressin mRNA. Science 255, 996–998 (1992).Article  PubMed  Google Scholar Martinon, F. et al. Induction of virus-specific cytotoxic T lymphocytes in vivo by liposome-entrapped mRNA. Eur. J. Immunol. 23, 1719–1722 (1993).Article  PubMed  Google Scholar Barenholz, Y. Doxil — the first FDA-approved nano-drug: lessons learned. J. Controlled Rel. 160, 117–134 (2012).Article  Google Scholar Boczkowski, D., Nair, S. K., Snyder, D. & Gilboa, E. Dendritic cells pulsed with RNA are potent antigen-presenting cells in vitro and in vivo. J. Exp. Med. 184, 465–472 (1996).Article  PubMed  PubMed Central  Google Scholar Meidenbauer, N., Andreesen, R. & Mackensen, A. Dendritic cells for specific cancer immunotherapy. Biol. Chem. 382, 507–520 (2001).Article  PubMed  Google Scholar Karikó, K., Buckstein, M., Ni, H. & Weissman, D. Suppression of RNA recognition by toll-like receptors: the impact of nucleoside modification and the evolutionary origin of RNA. Immunity 23, 165–175 (2005).Article  PubMed  Google Scholar Zimmermann, T. S. et al. RNAi-mediated gene silencing in non-human primates. Nature 441, 111–114 (2006).Article  PubMed  Google Scholar Geall, A. J. et al. Nonviral delivery of self-amplifying RNA vaccines. Proc. Natl Acad. Sci. USA 109, 14604–14609 (2012).Article  PubMed  PubMed Central  Google Scholar Ibragimova, A. A. et al. mRNA-based personalized cancer vaccines: opportunities, challenges and outcomes. Acta Naturae 17, 17–37 (2025).Article  PubMed  PubMed Central  Google Scholar Chakraborty, C., Bhattacharya, M., Das, A., Agoramoorthy, G. & Lee, S.-S. CRISPR–Cas9-mediated therapeutics: current clinical trials and therapy approval landscape to treat human diseases. Mol. Ther. Nucleic Acids 37, 102859 (2026).Article  PubMed  PubMed Central  Google Scholar Raigani, M., Eftekhari, Z., Adeli, A. & Kazemi-Lomedasht, F. Advancing gene editing therapeutics: clinical trials and innovative delivery systems across diverse diseases. Mol. Ther. Nucleic Acids 36, 102666 (2025).Article  PubMed  PubMed Central  Google Scholar Wang, H. et al. One-step generation of mice carrying mutations in multiple genes by CRISPR/Cas-mediated genome engineering. Cell 153, 910–918 (2013).Article  PubMed  PubMed Central  Google Scholar