Abdel-Bar Hend Mohamed, Abdel-Reheem Amal Youssef, Osman Rihab, Awad Gehanne A S, Mortada Nahed
Department of Pharmaceutics, National Organization of Drug Control and Research, Giza, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Int J Pharm. 2014 Dec 30;477(1-2):623-30. doi: 10.1016/j.ijpharm.2014.11.005. Epub 2014 Nov 6.
Injectable thermoreversible chitosan (CS)/β-glycerophosphate (β-GP) hydrogels were developed for prolonged localized delivery of cisplatin (Cis). The effects of formulation variables on the thermoreversible hydrogels preparation as well as the impact of drug incorporation method on Cis release were studied. Antitumor activity of Cis CS/β-GP thermoreversible hydrogels were evaluated against HCT-116 human colorectal cancer cells and MCF-7 human breast cancer cells. Incorporation of Cis to CS solution adjusted at pH 6.2 prior to hydrogel preparation deemed necessary to achieve a sustained release up to 4 days. Cis loaded CS/β-GP thermoreversible hydrogels showed enhanced antitumor activity with about 1.2 fold and 2.05 fold that of Cis solution against HCT-116 cancer cells and MCF-7 cancer cells respectively. The obtained enhanced antitumor activity elected this delivery system for further in vivo and toxicological investigations.
可注射的热可逆壳聚糖（CS）/β-甘油磷酸酯（β-GP）水凝胶被开发用于顺铂（Cis）的长期局部递送。研究了配方变量对热可逆水凝胶制备的影响以及药物掺入方法对顺铂释放的影响。评估了顺铂CS/β-GP热可逆水凝胶对HCT-116人结肠癌细胞和MCF-7人乳腺癌细胞的抗肿瘤活性。在制备水凝胶之前，将顺铂掺入pH值调至6.2的CS溶液中，这被认为是实现长达4天持续释放所必需的。负载顺铂的CS/β-GP热可逆水凝胶显示出增强的抗肿瘤活性，分别是顺铂溶液对HCT-116癌细胞和MCF-7癌细胞的抗肿瘤活性的约1.2倍和2.05倍。所获得的增强的抗肿瘤活性使该递送系统被选用于进一步的体内和毒理学研究。
