pH-Sensitive Liposomes

Chu, Chun-Jung; Szoka, Francis C.

doi:10.3109/08982109409037050

Cited by 79 publications

(61 citation statements)

References 57 publications

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“…Inclusion of Chol in DOPE/OA liposome formulations resulted in a significant increase in plasma stability, without decreasing their pH-sensitivity [5]. The use of other amphiphilic stabilizers that were shown to be resistant to the extraction by albumin (such as Chol derivatives-CHEMS, or lipids with double acyl chains-DPSG) resulted in the formation of liposomes exhibiting higher stability in biological fluids, while maintaining their pH-sensitivity [25,46]. In addition to the limitations related to stability and changes in pH-sensitivity, the in vivo efficacy of pHsensitive liposomes depends strongly on the interactions with serum components (opsonins) that influence their pharmacokinetics and biodistribution.…”

Section: Long-circulating Dope-containing Ph-sensitive Liposomesmentioning

confidence: 99%

“…Such properties determine the liposome efficacy to mediate cytoplasmic delivery of the encapsulated molecules [1,2,25].…”

Section: Biophysical Properties Underlying the Phsensitivity Of Liposmentioning

confidence: 99%

“…This has been attributed to the tendency of PE-containing liposomes to form aggregates, due to the poor hydration of its headgroup, which can explain their high affinity to adhere to cell membranes [25,28].…”

Section: Binding and Cell Internalizationmentioning

confidence: 99%

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On the formulation of pH-sensitive liposomes with long circulation times

Simões

Moreira

Fonseca

et al. 2004

Advanced Drug Delivery Reviews

447

244

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Strategies used to enhance liposome-mediated drug delivery in vivo include the enhancement of stability and circulation time in the bloodstream, targeting to specific tissues or cells, and facilitation of intracytoplasmic delivery. pH-sensitive liposomes have been developed to mediate the introduction of highly hydrophilic molecules or macromolecules into the cytoplasm. These liposomes destabilize under acidic conditions found in the endocytotic pathway, and usually contain phosphatidylethanolamine (PE) and titratable stabilizing amphiphiles. Formulations without PE have also been developed. Encapsulated compounds are thought to be transported into the cytoplasm through destabilization of or fusion with the endosome membrane. Incorporation of a low mole percentage of poly(ethylene glycol) (PEG)-conjugated lipids into pHsensitive liposomes confers prolonged circulation times to these liposomes, which are otherwise cleared rapidly. While the incorporation of PEG -lipids reduces the pH-dependent release of encapsulated fluorescent markers in vitro, it does not hinder the cytoplasmic delivery of the markers per cell-associated liposome. This suggests that intracellular delivery is not dictated simply by the destabilization of the liposomes. Antibodies or ligands to cell surface receptors can be coupled to pH-sensitive or sterically stabilized pH-sensitive liposomes for targeting. pH-sensitive liposomes have been used to deliver anticancer drugs, antibiotics, antisense oligonucleotides, ribozymes, plasmids, proteins and peptides to cells in culture or in vivo. D

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Section: Long-circulating Dope-containing Ph-sensitive Liposomesmentioning

confidence: 99%

“…Such properties determine the liposome efficacy to mediate cytoplasmic delivery of the encapsulated molecules [1,2,25].…”

Section: Biophysical Properties Underlying the Phsensitivity Of Liposmentioning

confidence: 99%

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On the formulation of pH-sensitive liposomes with long circulation times

Simões

Moreira

Fonseca

et al. 2004

Advanced Drug Delivery Reviews

447

244

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“…This internalization has been attributed to the tendency of PE-containing liposomes to form aggregates, owing to the poor hydration of its head group, which can explain their high affinity to adhere to cell membranes (Chu & Szoka 1994;Collins 1995).…”

Section: Binding and Cell Internalizationmentioning

confidence: 99%

“…The selection of the amphiphilic stabilizers, as well as its molar percentage with respect to the PE content, is enforced by the desired properties of the liposomes, together with the extent of cellular internalization, the fusogenic ability, pH sensitivity and stability in biological fluids. The aforementioned properties determine the liposome efficacy to mediate cytoplasmic delivery of the encapsulated molecules (Torchilin et al 1993;Chu & Szoka 1994;Drummond et al 2000).…”

Section: Biophysical Properties Underlying the Ph Sensitivity Of Lipomentioning

confidence: 99%

pH-Sensitive liposomes-principle and application in cancer therapy

Karanth

Murthy

2007

Journal of Pharmacy and Pharmacology

256

156

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The purpose of this review is to provide an insight into the different aspects of pH-sensitive liposomes. The review consists of 6 parts: the first introduces different types of medications made in liposomal drug delivery to overcome several drawbacks; the second elaborates the development of pH-sensitive liposomes; the third explains diverse mechanisms associated with the endocytosis and the cytosolic delivery of the drugs through pH-sensitive liposomes; the fourth describes the role and importance of pHsensitive lipid dioleoylphosphatidylethanolamine (DOPE) and research carried on it; the fifth explains successful strategies used so far using the mechanism of pH sensitivity for fusogenic activity; the final part is a compilation of research that has played a significant role in emphasizing the success of pH-sensitive liposomes as an efficient drug delivery system in the treatment of malignant tumours. pH-Sensitive liposomes have been extensively studied in recent years as an amicable alternative to conventional liposomes in effectively targeting and accumulating anti-cancer drugs in tumours. This research suggests that pH-sensitive liposomes are more efficient in delivering anti-cancer drugs than conventional and long-circulating liposomes due to their fusogenic property. Research focused on the clinical and therapeutic side of pH-sensitive liposomes would enable their commercial utility in cancer treatment.

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Lipidic and Polymeric Nanomedicines in Clinical Applications

2024

Nanotechnology in Therapeutics

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pH-Sensitive Liposomes

Cited by 79 publications

References 57 publications

On the formulation of pH-sensitive liposomes with long circulation times

On the formulation of pH-sensitive liposomes with long circulation times

pH-Sensitive liposomes-principle and application in cancer therapy

Lipidic and Polymeric Nanomedicines in Clinical Applications

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