School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
Int J Pharm. 2013 Aug 16;452(1-2):173-9. doi: 10.1016/j.ijpharm.2013.04.075. Epub 2013 May 4.
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°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 24h of dialysis at 37°C.
由聚（氧化丁烯）（B）-聚（氧化乙烯）（E）嵌段共聚物 B16E42（BE）与 G2 PAMAM 树枝状大分子偶联形成的线性树枝状共聚物（BE-PAMAM）胶束的增溶能力已被用于比较与抗癌药物紫杉醇。在同等条件下，BE-PAMAM 共聚物比 BE 具有更大的增溶能力。与传统的溶液加载方法相比，使用溶剂加载方法可以提高药物载药效率。使用这种增溶技术，在 37°C 下，将紫杉醇包封在 2%（w/v）的 BE-PAMAM 共聚物溶液中，其溶解度增加了 3700 倍。动态光散射和透射电子显微镜研究表明，药物分子的包封诱导了 BE 共聚物从球形到蠕虫状胶束的转变。观察到包封药物的持续释放，在 37°C 下透析 24 小时后，分别从 2%（w/v）的 BE 和 BE-PAMAM 溶液中释放出约 80%和 60%的紫杉醇。
