Solubility enhancement of paclitaxel using a linear-dendritic block copolymer

被引：42
作者：
Zhou, Zhengyuan [1 ]
D'Emanuele, Antony [1 ]
Attwood, David [2 ]
机构：
[1] Univ Cent Lancashire, Sch Pharm & Biomed Sci, Preston PR1 2HE, Lancs, England
[2] Univ Manchester, Sch Pharm & Pharmaceut Sci, Manchester M13 9PL, Lancs, England
来源：
INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2013年 / 452卷 / 1-2期
关键词：
Paclitaxel; Dendrimer; Micellisation; Drug solubilisation; Block copolymer; Worm-like micelles; TARGETED DRUG-DELIVERY; IN-VIVO EVALUATION; AQUEOUS-SOLUTION; ETHYLENE-OXIDE; ASSOCIATION PROPERTIES; 1,2-BUTYLENE OXIDE; POLYMERIC MICELLES; DIBLOCK COPOLYMERS; TRIBLOCK COPOLYMER; NANOPARTICLES;
D O I：
10.1016/j.ijpharm.2013.04.075
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The solubilising capacities of micelles of a linear-dendritic copolymer (BE-PAMAM), formed by conjugating the poly(butylene oxide) (B)-poly(ethylene oxide) (E) block copolymer B16E42(BE) with a G2 PAMAM dendrimer, have been compared with those of the diblock copolymer B16E42 for the anti-cancer drug paclitaxel. The BE-PAMAM copolymer showed a greater solubility enhancement than BE under equivalent conditions. Drug-loading efficiency was improved using a solvent-loading method compared with the conventional solution-loading method. The solubility of paclitaxel was increased 3700-fold by micellar encapsulation in a 2% (w/v) BE-PAMAM copolymer solution at 37 degrees C using this solubilisation technique. Dynamic light scattering and transmission electron microscopy studies indicated a transition of spherical to worm-like micelles of the BE copolymer induced by the encapsulation of drug molecules. A sustained release of encapsulated drug was observed, with approximately 80% and 60% paclitaxel being released from 2% (w/v) solutions of BE and BE-PAMAM respectively after 24 h of dialysis at 37 degrees C. (C) 2013 Elsevier B.V. All rights reserved.
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收藏
页码：173 / 179
页数：7
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