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目的研究羧基化碳纳米管负载鬼臼毒素(PPT-CNTs-COOH)的制备以及体外透皮的特性。方法采用冷冻球磨法制备PPT-CNTs-COOH;采用红外、紫外、X-衍射、热重分析对其进行表征,并采用HPLC测定负载物中鬼臼毒素的含量;采用体外Franze扩散池法测定药物透皮速率;采用家兔的皮肤刺激性实验评价药物皮肤刺激性。结果 PPT-CNTs-COOH中鬼臼毒素的含量为58.0μg·mg~(-1);PPT凝胶的透皮速率为7.08μg·cm~(-2)·h~(-1),而PPT-CNTs-COOH凝胶的为3.03μg·cm~(-2)·h~(-1),PPT-CNTs-COOH凝胶的皮肤滞留量为3.04μg·cm~(-2),PPT凝胶为1.52μg·cm~(-2);PPT-CNTs-COOH凝胶涂药24 h内表现为轻度刺激性,48 h后刺激性逐渐降低,72 h后刺激性消失。结论 PPT-CNTs-COOH体外透皮具有显著缓释效果,皮肤滞留量高,利于局部透皮给药治疗。
Objective To study the preparation of carboxylated carbon nanotubes loaded podophyllotoxin (PPT-CNTs-COOH) and its in vitro transdermal properties. Methods PPT-CNTs-COOH was prepared by the free-cooling milling method. The structure of PPT-CNTs-COOH was characterized by IR, UV, X-ray diffraction and thermogravimetric analysis. The content of podophyllotoxin was determined by HPLC. Transdermal rate; Rabbit skin irritation test to evaluate drug skin irritation. Results The content of podophyllotoxin in PPT-CNTs-COOH was 58.0 μg · mg -1, the transdermal rate of PPT gel was 7.08 μg · cm -2 · h -1, The skin retention of PPT-CNTs-COOH gel was 3.04 μg · cm -2 for the -CNTs-COOH gel, 3.03 μg · cm -2 -2 h -1 for PPT-CNTs-COOH gel, 1.52μg · cm -2. PPT-CNTs-COOH gel showed mild irritation within 24 h and irritation gradually decreased after 48 h, but disappeared after 72 h. Conclusion PPT-CNTs-COOH in vitro transdermal delivery has a significant sustained release effect, high skin retention, which is conducive to local transdermal drug delivery.