4.4 Article

Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

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AAPS PHARMSCITECH
卷 17, 期 2, 页码 436-445

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SPRINGER
DOI: 10.1208/s12249-015-0369-y

关键词

controlled release; cubosomes; docetaxel; gelation; thermoresponsive gel

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The aim of the present study was to develop and evaluate a thermoresponsive depot system comprising of docetaxel-loaded cubosomes. The cubosomes were dispersed within a thermoreversible gelling system for controlled drug delivery. The cubosome dispersion was prepared by dilution method, followed by homogenization using glyceryl monooleate, ethanol and Pluronic(A (R)) F127 in distilled water. The cubosome dispersion was then incorporated into a gelling system prepared with Pluronic(A (R)) F127 and Pluronic(A (R)) F68 in various ratios to formulate a thermoresponsive depot system. The thermoresponsive depot formulations undergo a thermoreversible gelation process i.e., they exists as free flowing liquids at room temperature, and transforms into gels at higher temperatures e.g., body temperature, to form a stable depot in aqueous environment. The mean particle size of the cubosomes in the dispersion prepared with Pluronic(A (R)) F127, with and without the drug was found to be 170 and 280 nm, respectively. The prepared thermoresponsive depot system was evaluated by assessing various parameters like time for gelation, injectability, gel erosion, and in-vitro drug release. The drug-release studies of the cubosome dispersion before incorporation into the gelling system revealed that a majority (similar to 97%) of the drug was released within 12 h. This formulation also showed a short lag time (similar to 3 min). However, when incorporated into a thermoresponsive depot system, the formulation exhibited an initial burst release of similar to 21%, and released only similar to 39% drug over a period of 12 h, thus indicating its potential as a controlled drug delivery system.

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