Nature Reviews Materials2021ReviewDrug Delivery
Mandana T. Manzari, Yosi Shamay, Hiroto Kiguchi, Neal Rosen, Maurizio Scaltriti, And Daniel A. Heller
Precision medicine has transformed cancer therapy by enabling molecular profiling and optimised drug design, but clinical translation of many precision therapeutics is hindered by pharmacological limitations, including toxicities and drug resistance. Drug delivery materials can modulate a drug’s pharmacokinetics…
Read the article →Nature Communications2021ReviewNon-viral Gene Delivery
Han X, Zhang H, Butowska K, Swingle Kl, Alameh M-G, Weissman D, Mitchell Mj
RNA therapeutics—ASOs, siRNAs, miRNAs, mRNAs, and CRISPR-Cas9 sgRNAs—are limited by nuclease degradation, large size, and negative charge. Ionisable lipids are the key LNP component that condenses RNA, enables endosomal escape, and reduces toxicity. Since 2008, many ionisable lipids have been created, but the field…
Read the article →Bioengineering & Translational Medicine2021ReviewNon-viral Gene Delivery
Schlich M, Palomba R, Costabile G, Mizrahy S, Pannuzzo M, Peer D, Decuzzi P
Endosomal escape remains the major intracellular barrier for RNA therapeutics. Only a small fraction of RNA delivered by ionisable lipid nanoparticles (LNPs) reaches the cytosol, where siRNA, miRNA, mRNA, and CRISPR components must act. A deeper mechanistic understanding is needed to design next-generation LNPs with…
Read the article →ACS Nano.2021ReviewNon-viral Gene Delivery
Rumiana Tenchov, Robert E. Bird, Allison E. Curtze, Qiongqiong Angela Zhou
Lipid nanoparticles (LNPs) have become key delivery vehicles across pharmaceuticals, with renewed prominence as the delivery platform for COVID-19 mRNA vaccines. The field lacks a broad, quantitative landscape of LNP research across liposomes, solid lipid nanoparticles, nanostructured lipid carriers, cationic…
Read the article →APL Bioengineering2021ReviewNon-viral Gene Delivery
Matthew R. Aronson, Scott H. Medina, Michael J. Mitchell
Most clinically approved cancer therapies are potent and toxic small molecules limited by severe off-target toxicities and poor tumour-specific localisation. Liposomal encapsulation reduces toxicity, but reliance on passive targeting via the enhanced permeability and retention (EPR) effect leaves unresolved issues…
Read the article →Molecules2021ReviewNon-viral Gene Delivery
Wan, Z.; Zheng, R.; Moharil, P.; Liu, Y.; Chen, J.; Sun, R.; Song, X.; Ao, Q
Cancer immunotherapy can produce durable clinical responses, but systemic delivery of immunostimulatory agents is limited by short half-lives, off-target toxicities (e.g., cytokine release syndrome), low response rates (10–30%), and poor efficacy in solid tumours. Polymeric micelles offer a biocompatible, modifiable…
Read the article →Frontiers in Bioengineering and Biotechnology2021ReviewNon-viral Gene Delivery
Chang D, Ma Y, Xu X, Xie J, Ju S
Polymeric nanoparticles are widely used for cancer theranostics because of their biocompatibility, biodegradability, and structural versatility, but conventional delivery still faces poor target specificity, uncontrolled release, and systemic toxicity. Stimuli-responsive polymeric nanoplatforms are proposed to…
Read the article →2020ResearchNon-viral Gene Delivery
Vitor Francisco, Catarina Rebelo, Artur Filipe Rodrigues, Josephine Blersch, Hugo Fernandes, Lino Ferreira
Non-viral vectors such as nanoparticles (NPs) show promise for RNA-based therapies, but suffer from limited cell targeting, poor cellular internalisation, and inadequate endolysosomal escape capacity. The field lacks a systematic, high-throughput approach to identify effective polymeric nanocarriers that can deliver…
Read the article →Biomaterials Science (accepted manuscript; manuscript ID BM-ART-09-2020ResearchNon-viral Gene Delivery
Rui Zhang, Rakan El-Mayta, Timothy Murdoch, Claude Warzecha, Margaret Billingsley, Sarah Shepherd, Ningqiang Gong, Lili Wang, James Wilson, Daeyeon Lee, Michael J. Mitchell
LNP delivery to liver versus spleen is difficult to predict from formulation parameters, and the role of helper phospholipids in biodistribution and protein adsorption is incompletely understood. This study probed how helper lipid identity (DOPE vs DSPC) affects LNP accumulation in liver/spleen and interactions with…
Read the article →Acta Biomaterialia2020ResearchNon-viral Gene Delivery
Yusuke Sato, Nana Okabe, Yusuke Note, Kazuki Hashiba, Masatoshi Maeki, Manabu Tokeshi, Hideyoshi Harashima
Small-sized lipid nanoparticles (LNPs) are attractive for tissue penetration but often lose potency because lipid components diffuse out and serum proteins adsorb onto poorly packed surfaces. The study asked how the hydrophobic scaffold structure of pH-sensitive cationic lipids affects small-LNP stability, lipid…
Read the article →Journal of Controlled Release2020ResearchNon-viral Gene Delivery
Nour Shobaki, Yusuke Sato, Yuichi Suzuki, Nana Okabe, Hideyoshi Harashima
Tumour-associated macrophages (TAMs) are largely M2-like and promote tumour growth, angiogenesis, metastasis, and immune suppression. There is a need for systemic delivery systems that can target TAMs and manipulate their pro-tumour functions with siRNA for cancer immunotherapy. Optimised CL4H6-LNPs had 90% siRNA…
Read the article →Nature Communications2020ResearchNon-viral Gene Delivery
Siddharth Patel, N. Ashwanikumar, Ema Robinson, Yan Xia, Cosmin Mihai, Joseph P. Griffith Iii, Shangguo Hou, Adam A. Esposito, Tatiana Ketova, Kevin Welsher, John L. Joyal, Örn Almarsson, Gaurav Sahay
Endosomal sequestration of lipid-based nanoparticles (LNPs) remains a formidable barrier to delivery, with only <2% of LNPs reaching the cytosol. The role of cholesterol structure in LNP-mediated mRNA delivery and endosomal escape was poorly understood. There is a need to decode the structural characteristics of…
Read the article →International Immunopharmacology2020ReviewNon-viral Gene Delivery
Hashemi V, Farhadi S, Ghasemi Chaleshtari M, Et Al.
Dendritic cell (DC)-based cancer immunotherapy has shown impressive outcomes, including the first FDA-approved anti-cancer vaccine, but clinical application faces challenges such as limited durable responses, antigen selection issues, and immunosuppressive tumour microenvironments. Nanoparticles (NPs) are promising…
Read the article →Frontiers in Molecular Biosciences2020ReviewDrug Delivery
Yao Y, Zhou Y, Liu L, Xu Y, Chen Q, Wang Y, Wu S, Deng Y, Zhang J, Shao A.
Conventional chemotherapy and targeted therapy are limited by systemic toxicity, poor tumour targeting, and multidrug resistance (MDR). Nanoparticle-based drug delivery offers improved pharmacokinetics, biocompatibility, enhanced permeability and retention (EPR), precise targeting, and potential to overcome…
Read the article →2020ReviewNon-viral Gene Delivery
Zeb A, Rana I, Choi H-I, Et Al.
Biopharmaceuticals have become clinically and commercially important due to their specificity, potency, targeting ability, and reduced side effects, but their macromolecular structure and intrinsic instability make formulation and administration challenging; parenteral delivery remains the only viable option in most…
Read the article →Nature Communications2020ReviewNon-viral Gene Delivery
Karen Bulaklak And Charles A. Gersbach
Gene therapy is at an inflection point: recent approvals and clinical successes have validated the field, but broader application is still limited by immune responses to vectors, inefficient delivery outside the retina and liver, and regulatory frameworks that are poorly suited to personalised, potentially curative…
Read the article →Bioconjugate Chemistry2020ReviewNon-viral Gene Delivery
Francia V, Schiffelers Rm, Cullis Pr, Witzigmann D
LNPs are clinically advanced vectors for siRNA, mRNA, and DNA delivery, but their in vivo behaviour is strongly influenced by the biological environment. Upon administration, biomolecules adsorb to the LNP surface and form a “biomolecular corona,” which defines the particle’s biological identity, affects stability…
Read the article →2020ReviewNon-viral Gene Delivery
Liu C, Zhang L, Dong N, Zhang W, Chen X, Gao R, Sun H.
Cationic liposomes (CLs) are promising non-viral gene-delivery vectors, but their clinical use in cancer gene therapy is limited by extracellular barriers (opsonisation, RES clearance, poor tumour penetration) and intracellular barriers (endosomal/lysosomal entrapment, restricted cytoplasmic/nuclear transport). The…
Read the article →Advanced Drug Delivery Reviews2020ReviewDrug Delivery
Nina Filipczak, Jiayi Pan, Satya Siva Kishan Yalamarty, Vladimir P. Torchilin
Liposomes remain an important nano-sized drug delivery system because of their biomimetic bilayer, ease of preparation, and biocompatibility, but clinical translation is still limited by reproducibility, scale-up, stability, and payload-specific barriers. The review updates recent advances in liposome preparation…
Read the article →International Journal of Nanomedicine2020ReviewNon-viral Gene Delivery
Chen, C.-K.; Huang, P.-K.; Law, W.-C.; Chu, C.-H.; Chen, N.-T.; Lo, L.-W
Gene therapy is limited by the fragile nature of therapeutic DNA/RNA and by safety concerns with viral vectors. Non-viral polymeric vectors are attractive, but conventional cationic polymers such as PEI, PDMAEMA, and PLL are often non-degradable, causing accumulation, cytotoxicity, and poor gene unpacking. This…
Read the article →Pharmaceutics2020ReviewNon-viral Gene Delivery
Wahane A, Waghmode A, Kapphahn A, Dhur K, Gupta A, Bahal R
Nucleic acid analogs and genome-editing proteins have broad therapeutic potential, but clinical translation is limited by poor cell- and organ-specific delivery, endosomal entrapment, enzymatic degradation, and short bioavailability. The review examines lipid- and polymer-based non-viral vectors as strategies to…
Read the article →Molecular Therapy2019ReviewNon-viral Gene Delivery
Piotr S. Kowalski, Arnab Rudra, Lei Miao, Daniel G. Anderson
mRNA has broad therapeutic potential for vaccination, protein replacement, and gene editing, but its clinical translation is limited by the need for improved intracellular delivery systems. mRNA is much larger than siRNA or ASOs (~300–5,000 kDa, ~1–15 kb vs ~14 kDa and 4–10 kDa, respectively), making delivery more…
Read the article →Nanoscale2019ResearchNon-viral Gene Delivery
Dongyu Chen, Shanthi Ganesh, Weimin Wang, Mansoor Amiji
Protein corona formation in biological fluids can alter nanoparticle cellular uptake, transfection, and gene silencing, but the relationship between LNP surface chemistry and corona-mediated delivery is incompletely understood. This study examined how PEG lipid chain length and PEG molar ratio affect protein corona…
Read the article →Journal of Controlled Release2019ResearchNon-viral Gene Delivery
Yusuke Sato, Kazuki Hashiba, Kosuke Sasaki, Masatoshi Maeki, Manabu Tokeshi, Hideyoshi Harashima
Endosomal escape remains a major rate-limiting step for siRNA delivery. The structure–activity relationships (SAR) of pH-sensitive cationic lipids were incompletely understood, limiting rational design of lipid nanoparticles (LNPs) for efficient in vivo siRNA delivery to hepatocytes. Hydrophilic head group structure…
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