Issue 4, 2016

Reverse micelles-in-microspheres with sustained release of water-soluble combretastatin A4 phosphate for S180 tumor treatment

Abstract

Combretastatin A4 phosphate (CA4P), the water-soluble phosphate pro-drug of combretastatin A4 (CA4), acts as a novel vascular disrupting agent (VDA). It strongly inhibits tubulin polymerization and selectively exerts action against tumor blood vessels. However, its quite short half-life (∼30 min) results in a short action time and consequently limits its application. Therefore, it is beneficial to develop a sustained-release preparation of CA4P for relatively long action duration. On the other hand, conventional PLGA microspheres display poor encapsulation capability for water-soluble small molecules due to rapid diffusion outside. Hence, we developed CA4P-loaded microspheres (CA4P-MS) composed of methoxy poly(ethylene glycol)-b-polylactide (PELA) reverse micelles and PLGA with a nano-in-micro sea-island structure. The CA4P encapsulation efficiency of CA4P-MS reached 92.88%. More interestingly, sustained drug release was achieved, which contributed to the prolonged inhibition effect on S180 tumor during a 30-day period with one-time subcutaneous administration. In conclusion, our study established a biodegradable polymer based platform to construct microspheres for water-soluble small molecular compounds with sustained release and a long-lasting action.

Graphical abstract: Reverse micelles-in-microspheres with sustained release of water-soluble combretastatin A4 phosphate for S180 tumor treatment

Article information

Article type
Paper
Submitted
24 nóv. 2015
Accepted
17 des. 2015
First published
18 des. 2015

J. Mater. Chem. B, 2016,4, 760-767

Author version available

Reverse micelles-in-microspheres with sustained release of water-soluble combretastatin A4 phosphate for S180 tumor treatment

L. wu and L. Qiu, J. Mater. Chem. B, 2016, 4, 760 DOI: 10.1039/C5TB02468D

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