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A Facile and Efficient Approach for the Production of Reversible Disulfide Cross-linked Micelles
Published on: December 23, 2016
Cholic acid-based novel micellar nanoplatform for delivering FDA-approved taxanes
Gaurav Bharadwaj1, Viet Nhan1,2, ShanChao Yang1
1Department of Biochemistry & Molecular Medicine, UC Davis Cancer Center, University of California Davis, Sacramento, CA 95817, USA.
Aim:
To structurally modify our existing cholic acid (CA)-based telodendrimer (TD; PEG5K-CA8) 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 PEG5K-CA8, 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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