载多烯紫杉醇Solutol HS15/Pluronic F127混合胶束及叶酸接枝的Solutol HS15/Pluronic F127载药混合胶束的制备、优化及对比表征

doi:10.5246/jcps.2015.02.011

中国药学(英文版) ›› 2015, Vol. 24 ›› Issue (2): 95-103.DOI: 10.5246/jcps.2015.02.011

载多烯紫杉醇Solutol HS15/Pluronic F127混合胶束及叶酸接枝的Solutol HS15/Pluronic F127载药混合胶束的制备、优化及对比表征

吴文婷, 关志宇^*

江西中医药大学药学院药剂学系, 江西南昌 330004

收稿日期:2014-09-28 修回日期:2014-11-14 出版日期:2015-02-01 发布日期:2014-12-01
通讯作者: Tel.: 13479148809
基金资助:
The Key Disciplines Research Funds for the Young Teachers (Grant No. 2013jzzdxk038).

Docetaxel-loaded mixed micelles composed of Solutol HS15 and Pluronic F127 or folate-conjugated F127: preparation, optimization and in vitro comparative characterization

Wenting Wu, Zhiyu Guan^*

Department of Pharmaceutics, College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China

Received:2014-09-28 Revised:2014-11-14 Online:2015-02-01 Published:2014-12-01
Contact: Tel.: 13479148809
Supported by:
The Key Disciplines Research Funds for the Young Teachers (Grant No. 2013jzzdxk038).

摘要/Abstract

摘要：

采用薄膜水化法制备了载多烯紫杉醇Solutol HS15/Pluronic F127混合胶束(SF-DTX)及叶酸接枝的Solutol HS15/Pluronic F127载药混合胶束(FSF-DTX)。体外表征实验表明, 两种载药混合胶束体系均呈球型, 粒径分别为(22.2±0.43) nm, (24.3±0.26) nm; 均具备较高包封率, SF-DTX为99.05%, FSF-DTX为90.28%, 且均有缓释特性。同时, 细胞摄取及细胞毒性实验结果表明两种混合胶束体系均在一定程度上可以逆转肿瘤多药耐药性(MDR), 且FSF较之于SF胶束体系能更明显增强耐药人口腔上皮细胞癌细胞(KBv)对DTX的摄取, 是一种潜在的肿瘤靶向性载药体系。

关键词: Solutol HS 15, Pluronic F127, 混合胶束, 叶酸接枝, 肿瘤多药耐药

Abstract:

In this study, two kinds of docetaxel (DTX)-loaded mixed micelles, composed of Solutol HS15 (HS15)/Pluronic F127 (F127) or folate-conjugated F127, (SF-DTX and FSF-DTX), were prepared by the thin-film hydration method and evaluated in vitro. Both SF-DTX and FSF-DTX were spherical with diameter close to 23 nm. They had high encapsulating efficiency (99.05% and 90.28% for SF-DTX and FSF-DTX, respectively) and sustained-release property. SF and FSF were able to enhance the cellular accumulation of DTX in KBv cells and reduce ATP content in A-549 cells. They also were able to reverse multidrug resistance (MDR). In vitro cytotoxicity and cellular accumulation of DTX suggested an active targeting of FSF-DTX. It could be concluded from the results that the novel F127/HS15 system could serve as a potential nanocarrier with the ability of overcoming MDR, and folate-conjugated F127/HS15 might achieve active targeting at the same time.

Key words: Solutol HS 15, Pluronic F127, Mixed micelle, Folate-conjugation, Multidrug resistance

中图分类号:

R943

Supporting:

吴文婷, 关志宇. 载多烯紫杉醇Solutol HS15/Pluronic F127混合胶束及叶酸接枝的Solutol HS15/Pluronic F127载药混合胶束的制备、优化及对比表征[J]. 中国药学(英文版), 2015, 24(2): 95-103.

Wenting Wu, Zhiyu Guan. Docetaxel-loaded mixed micelles composed of Solutol HS15 and Pluronic F127 or folate-conjugated F127: preparation, optimization and in vitro comparative characterization[J]. Journal of Chinese Pharmaceutical Sciences, 2015, 24(2): 95-103.

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载多烯紫杉醇Solutol HS15/Pluronic F127混合胶束及叶酸接枝的Solutol HS15/Pluronic F127载药混合胶束的制备、优化及对比表征

Docetaxel-loaded mixed micelles composed of Solutol HS15 and Pluronic F127 or folate-conjugated F127: preparation, optimization and in vitro comparative characterization

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