Department of Pharmaceutics, East West College of Pharmacy, Bangalore 560 091, Karnataka, India.
Saudi Pharm J. 2013 Jan;21(1):85-91. doi: 10.1016/j.jsps.2011.12.002. Epub 2012 Jan 5.
The objective of this study was to develop paclitaxel (PTX) loaded poly(ε-caprolactone) (PCL) based tiny implants. β-Cyclodextrin (β-CD) and polyethylene glycol (PEG 6000) were used to enhance solubility and release of the drug in the phosphate buffer saline pH 7.4. Implants were evaluated in terms of color, shape, thickness, surface area, weight, drug content. Developed implants were characterized for their surface morphology (SEM analysis), drug physical state by thermal analysis (DSC studies), crystalline nature (XRD studies) and drug excipients compatibility (FT-IR spectroscopy). Macroscopically all the tiny implants were white in color and cylindrical in shape with smooth surfaces. PTX was entrapped within implants in the polymeric amorphous form. In vitro drug release studies showed prolonged and controlled release of PTX with zero order and Korsmeyer-Peppas model being exhibited. Excipients and method of preparation did not affect chemical stability of PTX.
本研究旨在开发紫杉醇（PTX）负载的聚己内酯（PCL）基微小植入物。β-环糊精（β-CD）和聚乙二醇（PEG 6000）被用于提高药物在磷酸盐缓冲盐水 pH 7.4 中的溶解度和释放度。植入物的颜色、形状、厚度、表面积、重量和药物含量等方面进行了评价。所开发的植入物通过扫描电子显微镜分析（SEM 分析）对其表面形态、热分析（DSC 研究）研究药物物理状态、结晶性质（XRD 研究）和药物赋形剂相容性（FT-IR 光谱学）进行了表征。宏观上，所有微小植入物均为白色，呈圆柱形，表面光滑。PTX 以无定形聚合物的形式包埋在植入物中。体外药物释放研究表明，PTX 呈零级和 Korsmeyer-Peppas 模型的持续和控制释放。赋形剂和制备方法不会影响 PTX 的化学稳定性。
