Mishra Brahmeshwar, Padaliya Ravi, Patel Ravi R
a Department of Pharmaceutics , Indian Institute of Technology (Banaras Hindu University ), Varanasi , India.
Artif Cells Nanomed Biotechnol. 2017 May;45(3):522-534. doi: 10.3109/21691401.2016.1163714. Epub 2016 Mar 26.
The objective of the present study was to formulate and optimize exemestane (EXM) encapsulated vitamin E-TPGS-poly-ɛ-caprolactone based polymeric nanoparticles (TPGS-PCLNPs) for enhancing its anticancer efficacy. The 2 factorial design was employed to investigate the combined influence of formulation and process variables on properties of TPGS-PCLNPs, prepared by nanoprecipitation method. The physicochemical characterization revealed the encapsulation of EXM in amorphous form without any interaction inside spherical shaped TPGS-PCLNPs. In vitro cytotoxicity study on MCF-7 breast cancer cells exhibited enhanced cytotoxicity of EXM by encapsulating in TPGS-PCLNPs. The TPGS-PCLNPs can serve as potential delivery vehicle for EXM to improve its therapeutic efficacy.
本研究的目的是制备并优化基于维生素E-TPGS-聚-ε-己内酯的依西美坦（EXM）包封聚合物纳米粒（TPGS-PCLNPs），以增强其抗癌功效。采用二因素设计研究配方和工艺变量对通过纳米沉淀法制备的TPGS-PCLNPs性质的综合影响。物理化学表征显示EXM以无定形形式包封在球形TPGS-PCLNPs内部且无任何相互作用。对MCF-7乳腺癌细胞的体外细胞毒性研究表明，将EXM包封在TPGS-PCLNPs中可增强其细胞毒性。TPGS-PCLNPs可作为EXM的潜在递送载体，以提高其治疗效果。
