Studies on Drug Release Characteristics and Anti-angiogenic Activity of V inblastine Sulfate Thermosensitive Hydrogels

F U Xu-dong;HU Jing - hong;LU You-xing;ZHNG Meng-you

Chinese Pharmaceutical Journal ›› 2009, Vol. 44 ›› Issue (22) : 1723-1726.

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PDF(2993 KB)
Chinese Pharmaceutical Journal ›› 2009, Vol. 44 ›› Issue (22) : 1723-1726.
Article

Studies on Drug Release Characteristics and Anti-angiogenic Activity of V inblastine Sulfate Thermosensitive Hydrogels

  • F U Xu-dong ， HU Jiang - hong ， LU You-xiang ， ZHANG Meng-you
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Abstract

OBJECTIVE To examine drug release profile of vinblastine sulfate (VBL) thermosensitive hydrogels and evaluate its anti-angiogenic activity. METHODS Vinblastine sulfate hydrogels were prepared with MPEG-PLGA. HPLC was used to determine drug content and in vitro release rate. The anti-angiogenic effect in vivo was evaluated with chicken chorioallantoic membrane (CAM) neovascularisation model. RESULTS Gelation temperature was decreased with the increased MPEG-PLGA concentration. 20% MPEG-PLGA solution became a gel state at physiological temperature (37 ℃).VBL hydrogels emerged 10%~30% burst release at 2 h, initial burst release was decreased with the increased MPEG-PLGA concentration. Drug release rate became slower during 2~3 d and became faster after 3 d. About 80% of VBL was released at day 10 from hydrogels at 10% and 20% MPEG-PLGA concentration. VBL hydrogels significantly inhibited small vessels forming at the dose of 2.8×10-3pg·egg-1 and 5.6×10-3pg·egg-1, markedly inhibited the big vessels angiogenesis at the dose of 5.6×10-3pg·egg-1. Anti-angiogenic effect on small vessels of VBL hydrogels at the dose of 2.8×10-3pg·egg-1 was greater than VBL solution at the same dose. VBL hydrogels and solution at the dose of 5.6×10-3pg·egg-1 had similar anti-angiogenic effects on small and big vessels. CONCLUSION VBL hydrogels exerted a remarkable controlled release characteristic and could significantly reduce CAM neovascularisation by continue action at lower dose.

Key words

vinblastine sulfate / MPEG-PLGA / thermosensitive hydrogels / chick chorioallantoic membrane / angiogenic Inhibitor

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F U Xu-dong;HU Jing - hong;LU You-xing;ZHNG Meng-you . Studies on Drug Release Characteristics and Anti-angiogenic Activity of V inblastine Sulfate Thermosensitive Hydrogels[J]. Chinese Pharmaceutical Journal, 2009, 44(22): 1723-1726

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（ 收稿日期 ： 2008-11-20 ）

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