Cao Pengxiao, Jeyabalan Jeyaprakash, Aqil Farrukh, Ravoori Srivani, Gupta Ramesh C, Vadhanam Manicka V
Department of Pharmacology and Toxicology, University of Louisville, Louisville, Kentucky, 40202.
J Pharm Sci. 2014 Mar;103(3):945-51. doi: 10.1002/jps.23864. Epub 2014 Jan 24.
Polymeric implants (millirods) have been tested for local delivery of chemotherapeutic agents in cancer treatment. Modeling of drug release profiles is critical as it may provide theoretical insights on rational implant design. In this study, a biodegradable poly (ε-caprolactone) (PCL) polymeric implant delivery system was tested to deliver green tea polyphenols (GTPs), both in vitro and in vivo. Factors including polymer compositions, supplements, drug loads, and surface area of implants were investigated. Our data showed that GTPs were released from PCL implants continuously for long durations, and drug load was the main determining factor of GTPs release. Furthermore, rates of in vitro release and in vivo release in the rat model followed similar kinetics for up to 16 months. A mathematical model was deduced and discussed. GTP implants have the potential to be used systemically and locally at the tumor site as an alternative strategy.
聚合物植入物（微棒）已在癌症治疗中用于局部递送化疗药物进行了测试。药物释放曲线的建模至关重要，因为它可为合理的植入物设计提供理论见解。在本研究中，测试了一种可生物降解的聚（ε-己内酯）（PCL）聚合物植入物递送系统在体外和体内递送绿茶多酚（GTPs）的情况。研究了包括聚合物组成、添加剂、药物负载量和植入物表面积等因素。我们的数据表明，GTPs从PCL植入物中持续长时间释放，药物负载量是GTPs释放的主要决定因素。此外，在大鼠模型中，体外释放速率和体内释放速率在长达16个月的时间内遵循相似的动力学。推导并讨论了一个数学模型。GTP植入物有潜力作为一种替代策略在肿瘤部位进行全身和局部应用。
