Materials Science Centre, Indian Institute of Technology, Kharagpur, West Bengal 721302, India.
School of Medical Science and Technology, Indian Institute of Technology, Kharagpur, West Bengal 721302, India.
Colloids Surf B Biointerfaces. 2014 Apr 1;116:169-75. doi: 10.1016/j.colsurfb.2013.12.040. Epub 2013 Dec 30.
The present work focuses on the design of a drug delivery system for systemic, controlled release of the poorly soluble breast cancer drug, letrozole. The drug delivery system was prepared in two steps: a low density polyethylene (LDPE) substrate surface was grafted with maleic anhydride (MA) via solution grafting technique. Next, the grafted substrate was used to anchor a hydrophilic polymeric drug release system consisting of poly (vinyl alcohol) (PVA). The PVA anchored MA grafted LDPE (PVA/MA-g-LDPE) drug release system was used for the controlled release of letrozole. This system was characterized using ATR-FTIR spectrophotometry, surface profilometry, and scanning electron microscopy. Biocompatibility studies were also carried out. In vitro release studies of letrozole from the system were performed in distilled water and phosphate buffer saline (PBS) at 37°C. Release of ∼90% letrozole from hydrophilic PVA matrix was observed within a period of 35 days. A high correlation coefficient (R(2)=0.99) was seen between the release of letrozole in distilled water and PBS. Cytotoxicity studies using MTT colorimetric assay suggested that all samples were biocompatible. It is concluded that the letrozole delivery system appears to overcome the limitations associated with letrozole by providing enhanced drug dissolution rate, controlled release and improved bioavailability of the incorporated drug and, therefore, seems to have extended therapeutic effects.
本工作专注于设计一种药物传递系统,用于系统地、控制释放疏水性乳腺癌药物来曲唑。药物传递系统分两步制备:通过溶液接枝技术将马来酸酐(MA)接枝到低密度聚乙烯(LDPE)基底表面。接下来,将接枝基底用于锚定由聚乙烯醇(PVA)组成的亲水性聚合物药物释放系统。将 PVA 锚定的 MA 接枝 LDPE(PVA/MA-g-LDPE)药物释放系统用于来曲唑的控制释放。使用衰减全反射傅里叶变换红外光谱(ATR-FTIR)分光光度法、表面轮廓仪和扫描电子显微镜对该系统进行了表征。还进行了生物相容性研究。在 37°C 的蒸馏水中和磷酸盐缓冲盐水(PBS)中进行了该系统的来曲唑体外释放研究。在 35 天内观察到约 90%的来曲唑从亲水性 PVA 基质中释放。在蒸馏水中和 PBS 中,来曲唑的释放具有高相关系数(R²=0.99)。MTT 比色法细胞毒性研究表明所有样品均具有生物相容性。结论是,来曲唑传递系统似乎通过提供增强的药物溶解速率、控制释放和改善所包含药物的生物利用度来克服与来曲唑相关的限制,因此似乎具有延长的治疗效果。