pH-Sensitive liposomes-principle and application in cancer therapy

Karanth, Hamsaraj; Murthy, R. S. R.

doi:10.1211/jpp.59.4.0001

Cited by 257 publications

(162 citation statements)

References 140 publications

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“…The mobility ability of laboratory-bred Daphnia after 24 and 48 h of exposure to the surfactants was used to determine the IC 50 value, the concentration estimated to immobilize 50% of the Daphnia. The pH of the test medium was 8.0, with total hardness of 250 mg/L (expressed as CaCO 3 ) and a Ca/Mg ratio of 4:1 [38]. A geometric series of 10 concentration values was tested for each amphiphile.…”

Section: Acute Toxicity Testsmentioning

confidence: 99%

“…Micelles and vesicles are colloidal aggregates of great biomedical relevance, in particular in connection with drug delivery [1][2][3], gene delivery [4,5] and drug antimicrobial activity [6,7]. In the case of vesicles, they have been classically prepared from polar lipids or their mixtures (liposomes) [1] or from mimicking non-natural double-tailed surfactants, such as dialkyldimethylammonium halides [1,8,9].…”

Section: Introductionmentioning

confidence: 99%

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Physicochemical and toxicological properties of novel amino acid-based amphiphiles and their spontaneously formed catanionic vesicles

Brito

Marques

Silva

et al. 2009

Colloids and Surfaces B: Biointerfaces

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a b s t r a c tThe design of efficient liposomal systems for drug delivery is of considerable biomedical interest. In this context, vesicles prepared from cationic/anionic surfactants may offer several advantages, mainly due to their spontaneity in formation and long-term stability. There is also an impending need to produce less toxic, more biocompatible amphiphiles, while maintaining the desirable aggregation properties. In this work, we present data for acute toxicity to Daphnia magna (IC 50 ), and potential ocular irritation (HC 50 ) for some newly prepared ionic surfactants with dodecyl chains, derived from the amino acids tyrosine (Tyr), serine (Ser), hydroxyproline (Hyp) and lysine (Lys). The micellization behavior of the compounds, evaluated from surface tension measurements, is presented and compared to more conventional ionic amphiphiles. Two types of spontaneouly formed catanionic vesicles, composed either by a dodecyltrimethylammonium bromide (DTAB)/Lys-derivative and or Ser-/Lys-derivative mixture, have also been tested for their ecotoxicity and hemolytic potential. All the micelle-forming surfactants as well as the vesicle-containing mixtures are found to have lower ecotoxicity than the reference surfactant DTAB. Moreover, the results from hemolysis and hemoglobin denaturation tests show that the Tyr-and Lys-derivatives are moderately irritant, whereas the Hyp-and Ser-ones are just slightly irritant. Even more significantly, the vesicle-containing mixtures exhibit lower hemolytic activity than the neat surfactants, a positive result for their potential use in liposomal formulations.

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Section: Acute Toxicity Testsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Physicochemical and toxicological properties of novel amino acid-based amphiphiles and their spontaneously formed catanionic vesicles

Brito

Marques

Silva

et al. 2009

Colloids and Surfaces B: Biointerfaces

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“…Although PEGylation increases the longevity of the liposomes in the circulation, in some cases it does not guarantee the escape of liposomes from endosomes, allowing the degradation of their contents prior to achieving their target. With the purpose of overcoming this problem, pH-labile linkers have been introduced between the hydrophilic PEG and the hydrophobic moiety, linkers that are cleaved upon exposure to the relatively low-endosomal pH or the acidotic tumor mass [57].…”

Section: Internal Stimulimentioning

confidence: 99%

Liposomal Nanoformulations as Current Tumor-Targeting Approach to Cancer Therapy

Porfire¹,

Achim²,

Tefas³

et al. 2017

Liposomes

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The liposomes present great potential for applications in targeted delivery of chemotherapeutics in the treatment of cancer. The use of liposomal drug carriers as vehicles for targeting of chemotherapeutic agents to tumor tissues is based on their advantages over other dosage forms, represented by their low systemic toxicity, their bioavailability, and their possibility to enhance the solubility of different chemotherapeutic agents, due to the ability to encapsulate both hydrophilic and lipophilic drugs. They enhance the therapeutic index of anticancer drugs by increasing the drug concentration in tumor cells through tumor targeting. The available approaches used for tumor targeting using liposomes are passive targeting, active targeting, and triggered drug release. The most advanced targeting strategies proposed for cancer treatment are the development of multifunctional liposomes, having combined targeting mechanism. In this chapter, the tumor-targeting mechanisms are described in detail as well as the possibilities to design the targeted liposomal nanocarrier in order to reach the desired target in the body and minimizing the off-target effects. Moreover, the current status of preclinical and clinical evaluation is highlighted.

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“…The pH-sensitive liposomes have been prepared for numerous applications in drug delivery including chemotherapy (Karanth & Murthy, 2007). In a study, engineered drug carriers capable of spontaneous accumulation in tumor areas via the enhanced permeability and retention (EPR) effect have been reported.…”

Section: Uptake and Intracellular Delivery Of Bioactive By Ph-sensitimentioning

confidence: 99%

A review of mechanistic insight and application of pH-sensitive liposomes in drug delivery

2014

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The pH-sensitive liposomes have been extensively used as an alternative to conventional liposomes in effective intracellular delivery of therapeutics/antigen/DNA/diagnostics to various compartments of the target cell. Such liposomes are destabilized under acidic conditions of the endocytotic pathway as they usually contain pH-sensitive lipid components. Therefore, the encapsulated content is delivered into the intracellular bio-environment through destabilization or its fusion with the endosomal membrane. The therapeutic efficacy of pHsensitive liposomes enables them as biomaterial with commercial utility especially in cancer treatment. In addition, targeting ligands including antibodies can be anchored on the surface of pH-sensitive liposomes to target specific cell surface receptors/antigen present on tumor cells. These vesicles have also been widely explored for antigen delivery and serve as immunological adjuvant to enhance the immune response to antigens. The present review deals with recent research updates on application of pH-sensitive liposomes in chemotherapy/ diagnostics/antigen/gene delivery etc.

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pH-Sensitive liposomes-principle and application in cancer therapy

Cited by 257 publications

References 140 publications

Physicochemical and toxicological properties of novel amino acid-based amphiphiles and their spontaneously formed catanionic vesicles

Physicochemical and toxicological properties of novel amino acid-based amphiphiles and their spontaneously formed catanionic vesicles

Liposomal Nanoformulations as Current Tumor-Targeting Approach to Cancer Therapy

A review of mechanistic insight and application of pH-sensitive liposomes in drug delivery

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