本文主要研究内容
作者（2019）在《Gambogic acid-encapsulated polymeric micelles improved therapeutic effects on pancreatic cancer》一文中研究指出：Gambogic acid(GA) is a natural product with potent anticancer activity in vitro. However, poor water solubility and systematic toxicity limit the further clinical application of GA. Micellization of hydrophobic molecule could effectively ameliorate aqueous dispersity of GA and induce better blood retention and tumor accumulation, hence lead to improved stability and therapeutic effect of GA. In this study, monomethyl poly(ethylene glycol)-poly(ε-caprolactone)-poly(trimethylene carbonate)(MPEG-P(CL-ran-TMC)) was used to encapsulate GA by a single-step solid dispersion method to form a GA encapsulated MPEG-P(CLran-TMC) micelles(GA micelles). GA micelles were characterized with a small particle size(44 ±1 nm),high drug loading content(26.28% ± 0.12%) and high-efficiency encapsulation(87.59% ± 0.41 %). Compared with free GA, GA micelles showed better dispersion in water, prolonged release behavior in vitro, and enhanced tumor cellular uptake. GA micelles could also effectively induce apoptosis in AsPC-1 cells.Compared with free GA, GA micelles exhibited superior antitumor efficacy and better apoptosis induced effect in a subcutaneous xenograft mouse model of AsPC-1 cells. In conclusion, GA micelles which showed high-efficiency anti-tumor effect in vitro and in vivo may serve as a candidate for pancreatic cancer therapy.
Abstract
Gambogic acid(GA) is a natural product with potent anticancer activity in vitro. However, poor water solubility and systematic toxicity limit the further clinical application of GA. Micellization of hydrophobic molecule could effectively ameliorate aqueous dispersity of GA and induce better blood retention and tumor accumulation, hence lead to improved stability and therapeutic effect of GA. In this study, monomethyl poly(ethylene glycol)-poly(ε-caprolactone)-poly(trimethylene carbonate)(MPEG-P(CL-ran-TMC)) was used to encapsulate GA by a single-step solid dispersion method to form a GA encapsulated MPEG-P(CLran-TMC) micelles(GA micelles). GA micelles were characterized with a small particle size(44 ±1 nm),high drug loading content(26.28% ± 0.12%) and high-efficiency encapsulation(87.59% ± 0.41 %). Compared with free GA, GA micelles showed better dispersion in water, prolonged release behavior in vitro, and enhanced tumor cellular uptake. GA micelles could also effectively induce apoptosis in AsPC-1 cells.Compared with free GA, GA micelles exhibited superior antitumor efficacy and better apoptosis induced effect in a subcutaneous xenograft mouse model of AsPC-1 cells. In conclusion, GA micelles which showed high-efficiency anti-tumor effect in vitro and in vivo may serve as a candidate for pancreatic cancer therapy.
论文参考文献
论文详细介绍
论文作者分别是来自Chinese Chemical Letters的，发表于刊物Chinese Chemical Letters2019年04期论文，是一篇关于,Chinese Chemical Letters2019年04期论文的文章。本文可供学术参考使用，各位学者可以免费参考阅读下载，文章观点不代表本站观点，资料来自Chinese Chemical Letters2019年04期论文网站，若本站收录的文献无意侵犯了您的著作版权，请联系我们删除。