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Journal ArticleDOI

Polysorbate Surfactants as Drug Carriers: Tween 20-Amphotericin B Conjugates as Anti-Fungal and Anti-Leishmanial Agents

TL;DR: Synthesis of drug conjugates with surfactants such as Tween-20 could open up new opportunities to improve the solubility of many drugs, reduce their toxicity and could possibly target the brain as polysorbates known to facilitate nanoparticulate systems to cross the blood-brain barrier.
Abstract: Background Amphotericin B (AmB), a polyene antibiotic used for the treatment of fungal and leishmanial infections is virtually insoluble in water and exhibits severe toxicity. AmB has been conjugated to various soluble polymers for improving its solubility and reducing its toxicity. Conjugating AmB to a polysorbate surfactant such as polyoxyethylene sorbitan monolaurate (Tween 20), was examined to improve its solubility and reduce its toxicity. Methods AmB was coupled to Tween 20 via carbamate linkage at 15 and 30 wt% concentrations in high yield by activating the hydroxyl groups of the surfactant using p- nitrophenyl chloroformate. The conjugates were characterized by using 1H NMR, IR, UV and HPLC analysis and were examined for their toxicity, and anti-fungal and anti-leishmanial activities in vitro. Results Tween-AmB conjugates were soluble to the extent of 10 mg/mL in water, showed improved critical micelle concentration in comparison with AmB, exhibited negligible hemolytic potential even at a concentration of 1000 µM and were not toxic against human embryonic kidney cell line (HEK293T) at similar concentrations. The conjugates showed potent anti-fungal activity against Candida albicans, Candida parapsilosis and Cryptococcus neoformans and anti-leishmanial activity against intramacrophage amastigotes of Leishmania donovani. Conclusions Tween 20 is a surfactant approved by the US FDA as an additive in food and pharmaceutical preparations. Synthesis of drug conjugates with surfactants such as Tween-20 could open up new opportunities to improve the solubility of many drugs, reduce their toxicity and could possibly target the brain as polysorbates known to facilitate nanoparticulate systems to cross the blood-brain barrier.
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Journal ArticleDOI
TL;DR: An overview of nano-emulsions for drug delivery can be found in this article, where the authors introduce nano-sized emulsions with sizes ranging from tens to hundreds of nanometers, and have great potential applications in pharmaceutics, foods and cosmetics due to their attractive properties.

55 citations

Journal ArticleDOI
TL;DR: An overview of nano-emulsions for drug delivery can be found in this article , where the authors introduce nano-sized emulsions with sizes ranging from tens to hundreds of nanometers, and have great potential applications in pharmaceutics, foods and cosmetics due to their attractive properties.

49 citations

Journal ArticleDOI
TL;DR: Insight is provided into the novel drug delivery strategies that were investigated for AmB over the last 5 years and a final critical selection of emerging concepts and most promising approaches are selected, based on the significance of preclinical antileishmanial and toxicity data.
Abstract: Introduction: Among the drugs in clinical use for the treatment of leishmaniases, amphotericin B (AmB) is the most effective and has been the most extensively studied for the development of drug delivery strategies. Liposomal amphotericin B (AmBisome®) still represents the best therapeutic option for leishmaniases, however, its clinical efficacy depends on the patient immunological status and the endemic region. Moreover, the need for parenteral administration, its side effects and high cost significantly limit its use in developing countries. Areas covered: This article provides insight into the novel drug delivery strategies that were investigated for AmB over the last 5 years and a final critical selection of emerging concepts and most promising approaches, based on the significance of preclinical antileishmanial and toxicity data. Expert opinion: The feasibility of oral and topical delivery of AmB has been established in experimental models of leishmaniases. Highly effective AmB nanocarriers containing active targeting ligand and/or immunomodulatory component have also emerged. Translating these advances to the clinic still relies on the full demonstration of safety and efficacy in humans and on the viability and cost-effectiveness of large-scale industrial production.

35 citations

Journal ArticleDOI
TL;DR: In this article, a review of toxicity aspects of nanoparticular-based drug delivery systems is presented, which would be beneficial for future researchers to develop nanoparticulate delivery vehicles for the improvement of delivery approaches in a safer way.

35 citations

Journal ArticleDOI
TL;DR: Polysorbates (PSs) are synthetic nonionic surfactants consisting of polyethoxy sorbitan fatty acid esters as discussed by the authors, which have been widely employed as emulsifiers and stabilizers in various drug formulations and food additives.
Abstract: Polysorbates (PSs) are synthetic nonionic surfactants consisting of polyethoxy sorbitan fatty acid esters. PSs have been widely employed as emulsifiers and stabilizers in various drug formulations and food additives. Recently, various PS-based formulations have been developed for safe and efficient drug delivery. This review introduces the general features of PSs and PS-based drug carriers, summarizes recent progress in the development of PS-based drug formulations, and discusses the physicochemical properties, biological safety, P-glycoprotein inhibitory properties, and therapeutic applications of PS-based drug formulations. Additionally, recent advances in brain-targeted drug delivery using PS-based drug formulations have been highlighted. This review will help researchers understand the potential of PSs as effective drug formulation agents.

12 citations