ArticleThe AAPS journal2011
Relationships between liposome properties, cell membrane binding, intracellular processing, and intracellular bioavailability.
Article in The AAPS journal, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
29 citing papers in PubMed, 73 citations in OpenAlex.
- Novel Gold-Functionalization of Liposomes and Its Impact on Cellular Uptake and Trafficking.Molecular pharmaceutics · 2026Article
- Insights into Liposomal and Gel-Based Formulations for Dermatological Treatments.Gels (Basel, Switzerland) · 2025Review
- Maleimide conjugated PEGylated liposomal antibiotic to combat multi-drug resistant Escherichia coli and Klebsiella pneumoniae with enhanced wound healing potential.Scientific reports · 2024Article
- Cornea-SELEX for aptamers targeting the surface of eyes and liposomal drug delivery.Exploration (Beijing, China) · 2024Article
- Comparative Studies of the Uptake and Internalization Pathways of Different Lipid Nano-Systems Intended for Brain Delivery.Pharmaceutics · 2023Article
- Induced Vascular Normalization-Can One Force Tumors to Surrender to a Better Microenvironment?Pharmaceutics · 2023Review
- pH-Responsive Lipid Nanoparticles Achieve Efficient mRNA Transfection in Brain Capillary Endothelial Cells.Pharmaceutics · 2022Article
- Liposome Formulation and In Vitro Testing in Non-Physiological Conditions Addressed to Ex Vivo Kidney Perfusion.International journal of molecular sciences · 2022Article
- Influence of Liposomes' and Lipoplexes' Physicochemical Characteristics on Their Uptake Rate and Mechanisms by the Placenta.International journal of molecular sciences · 2022Article
- Octreotide-Targeted Lcn2 siRNA PEGylated Liposomes as a Treatment for Metastatic Breast Cancer.Bioengineering (Basel, Switzerland) · 2021Article
- The liposomal delivery of hydrophobic oxidovanadium complexes imparts highly effective cytotoxicity and differentiating capacity in neuroblastoma tumour cells.Scientific reports · 2020Article
- Liposomal delivery of hydrophobic RAMBAs provides good bioavailability and significant enhancement of retinoic acid signalling in neuroblastoma tumour cells.Journal of drug targeting · 2020Article
- TargetAntiAngio: A Sequence-Based Tool for the Prediction and Analysis of Anti-Angiogenic Peptides.International journal of molecular sciences · 2019Article
- Article
- Liposomal formulations of carboplatin injected by convection-enhanced delivery increases the median survival time of F98 glioma bearing rats.Journal of nanobiotechnology · 2018Article
- Strategies for the enhanced intracellular delivery of nanomaterials.Drug discovery today · 2018Review
- Quantitative contributions of processes by which polyanion drugs reduce intracellular bioavailability and transfection efficiency of cationic siRNA lipoplex.Journal of controlled release : official journal of the Controlled Release Society · 2018Article
- AlPcSInternational journal of nanomedicine · 2018Article
- Luminescent CdSe@ZnS nanocrystals embedded in liposomes: a cytotoxicity study in HeLa cells.Toxicology research · 2017Article
- Liposomal Delivery Enhances Immune Activation by STING Agonists for Cancer Immunotherapy.Advanced biosystems · 2017Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
Abstract
Positive surface charge enhances liposome uptake into cells. Pegylation, used to confer stealth properties to enable in vivo applications of cationic liposomes, compromises internalization. The goal of this study was to determine the quantitative relationships between these two liposome properties (separately and jointly), liposomes binding to cell membrane, and the subsequent internalization and residence in intracellular space (referred to as intracellular bioavailability). The results, obtained in pancreatic Hs-766T cancer cells, revealed nonlinear and inter-dependent relationships, as well as substantial qualitative and quantitative differences. The proportionality constant K of intracellular and membrane-bound liposomes at equilibrium (i.e., I(eq) and B(eq)) showed a positive triphasic relationship with surface charge and a negative biphasic relationship with pegylation. Near-neutral liposomes showed little internalization of the membrane-bound moiety, increasing to a constant K value for medium charge liposomes (+15 to +35 mV zeta potential), followed by a further increase for highly charged liposomes (greater than or equal to +46 mV). The decline of pegylation with K value showed a breakpoint at 2%. The negative consequences of pegylation (%PEG) were partially offset by increasing charge (ZP). The best-fitting regression equations are: B(eq) = -1.36 × %PEG + 0.33 × ZP; I(eq) = -1.52 × %PEG + 0.34 × ZP. It suggested that 1% pegylation increase can be offset with 4 mV ZP. The differences are such that it may be possible to balance these parameters to simultaneously maximize the stealth property and intracellular bioavailability of cationic liposomes.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.