Gao Meng, Xu Hong, Zhang Chenghong, Liu Kexin, Bao Xu, Chu Qiuchen, He Yan, Tian Yan
Department of Pharmaceutics, College of Pharmacy .
Drug Dev Ind Pharm. 2014 Nov;40(11):1557-64. doi: 10.3109/03639045.2013.838579. Epub 2013 Sep 23.
This paper describes the development and optimization of curcumin thermosensitive hydrogels (CTH), a kind of gel injection for intratumoral injection treatment.
Aimed at increasing the content and stability of effective components, an optimal formulation of CTH was chosen based on the results from orthogonal tests and the optimal pH was determined by stability test. To investigate the hydrogels drug release in vitro, residence time by RP-HPLC and therapeutic effects on ascitic hepatocarcinoma cell strain with high metastasis potential in lymphatic system (HCA-F) solid tumors in mice.
The selected optimal formulation of CTH was: 0.2% curcumin, 20% poloxamer 407, 4% poloxamer 188, 8% polyethylene glycol 400, 12% 1,2-propanediol and pH was 6.0. The drug release determined by RP-HPLC fit to the Higuchi model. The residence time of CTH was longer than the curcumin suspensions. Intratumoral injection of the CTH can effectively inhibit the growth of HCA-F solid tumors in mice.
The CTH prepared in this test demonstrates proper gel temperature and viscosity. It improves the solubility of curcumin with a relatively long period of drug release in vitro and residence time. Intratumoral injection of the CTH can effectively inhibit the growth of HCA-F solid tumors in mice.
本文描述了姜黄素热敏水凝胶（CTH）的研发与优化，CTH是一种用于瘤内注射治疗的凝胶注射剂。
为提高有效成分的含量和稳定性，基于正交试验结果选择CTH的最佳配方，并通过稳定性试验确定最佳pH值。通过反相高效液相色谱法（RP-HPLC）研究水凝胶在体外的药物释放、滞留时间，以及对具有高淋巴系统转移潜能的腹水肝癌细胞株（HCA-F）小鼠实体瘤的治疗效果。
所选CTH的最佳配方为：0.2%姜黄素、20%泊洛沙姆407、4%泊洛沙姆188、8%聚乙二醇400、12% 1,2-丙二醇，pH值为6.0。RP-HPLC测定的药物释放符合 Higuchi 模型。CTH的滞留时间长于姜黄素悬浮液。瘤内注射CTH可有效抑制小鼠HCA-F实体瘤的生长。
本试验制备的CTH具有合适的凝胶温度和粘度。它提高了姜黄素的溶解度，在体外具有较长的药物释放期和滞留时间。瘤内注射CTH可有效抑制小鼠HCA-F实体瘤的生长。
