School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
Drug Dev Ind Pharm. 2013 Aug;39(8):1187-96. doi: 10.3109/03639045.2012.704042. Epub 2012 Jul 17.
Here we report the application of solid dispersion (SD) technique to improve paclitaxel (PTX) release from poly(ϵ-caprolactone) (PCL)-based film. Paclitaxel solid dispersions (SDs) with either poloxamer188 (PXM) or polyethylene glycol (PEG) were successfully prepared by a melting method and then incorporated into PCL films, which were characterized by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and In vitro drug release/dissolution studies. It was found that PTX was faster released from the SDs than the corresponding physical mixtures (PMs) or PTX alone. For the PCL films with almost the same PTX loading, drug release from films containing SDs was remarkably faster than that from the film directly incorporated with PTX particles, and the films containing SDs with PXM exhibited a faster drug release than those with PEG. An increase In the content of PXM had no significant influence on PTX release from the films containing SDs. Incorporation of a higher content of SDs led to slower drug release from PCL films, indicating that PTX loading had a dominating effect on drug release. Through this study, we demonstrated the feasibility of the application of SD technique on the improvement of PTX release from PCL films and offered some beneficial information on modulating drug release behavior by changing the compositions and contents of the SDs-loaded PCL films.
在这里,我们报告了固体制备(SD)技术在改善紫杉醇(PTX)从聚(ε-己内酯)(PCL)基膜中释放的应用。通过熔融法成功制备了泊洛沙姆 188(PXM)或聚乙二醇(PEG)的紫杉醇固体分散体(SD),并将其掺入 PCL 膜中,通过扫描电子显微镜(SEM)、X 射线衍射(XRD)、差示扫描量热法(DSC)和体外药物释放/溶解研究进行了表征。结果发现,SD 中的 PTX 比相应的物理混合物(PM)或单独的 PTX 释放得更快。对于具有几乎相同 PTX 负载的 PCL 膜,含有 SD 的膜中的药物释放明显快于直接掺入 PTX 颗粒的膜,并且含有 PXM 的 SD 的膜的药物释放快于含有 PEG 的 SD。PXM 含量的增加对含有 SD 的膜中 PTX 的释放没有显著影响。掺入更高含量的 SD 导致 PCL 膜中药物释放更慢,表明 PTX 负载对药物释放具有主导作用。通过这项研究,我们证明了 SD 技术在改善 PCL 膜中 PTX 释放方面的应用的可行性,并提供了一些有益的信息,即通过改变 SD 负载 PCL 膜的组成和含量来调节药物释放行为。