Cholic acid-based novel micellar nanoplatform for delivering FDA-approved taxanes

基于胆酸的新型胶束纳米平台用于递送FDA批准的紫杉烷类药物

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Abstract

AIM: To structurally modify our existing cholic acid (CA)-based telodendrimer (TD; PEG(5K)-CA(8)) for effective micellar nanoencapsulation and delivery of the US FDA-approved members of taxane family. MATERIALS & METHODS: Generation of hybrid TDs was achieved by replacing four of the eight CAs with biocompatible organic moieties using solution-phase peptide synthesis. Drug loading was done using the standard evaporation method. RESULTS: Hybrid TDs can generate micelles with narrow size distributions, low critical micelle concentration values (1-6 μM), better hematocompatibility and lack of in vitro cytotoxicity. CONCLUSION: Along with PEG(5K)-CA(8), CA-based hybrid nanoplatform is the first of its kind that can stably encapsulate all three FDA-approved taxanes with nearly 100% efficiency up to 20% (w/w) loading.

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