4.7 Article

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

Journal

NANOMEDICINE
Volume 12, Issue 10, Pages 1153-1164

Publisher

FUTURE MEDICINE LTD
DOI: 10.2217/nnm-2017-0361

Keywords

cabazitaxel; cholic acid; docetaxel; drug delivery; micelle; nanoparticle; paclitaxel; taxane; telodendrimer

Funding

  1. NIH [3R01CA115483, 1U01CA198880-01, 5R01CA199668]

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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 mu M), better hematocompatibility and lack of in vitro cytotoxicity. Conclusion: Along with PEG(5K)-CA(8), CA-based hybridnanoplatform 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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