N-三甲基壳聚糖对塞来昔布脂质体体外透皮促进作用考察

目的 对季铵化程度为60％的N-三甲基壳聚糖（TMC60）促进塞来昔布脂质体（CLXL）透皮吸收的作用进行体外研究.方法 采用薄膜分散-高压均质法制备CLXL,并分别制成TMC60包衣和物理混合物;对TMC60包衣前后脂质体的形态、粒径、Zeta电位及包封率进行了比较;以氮酮为阳性对照,采用Franz扩散池法,对CLXL 、TMC60包衣CLXL、TMC60与CLXL物理混合物穿透小鼠离体皮肤的累积量及速率进行考察.结果 TMC60包衣后,形态上呈现明显包衣层,粒径增大,Zeta电位由负转正,而包封率无明显变化;体外透皮试验结果表明,与CLXL相比,TMC60包衣CLXL、TMC60与CLXL物理混合物、氮酮与CLXL物理混合物的透皮渗透量及透皮速率均显著增加（P＜0.05）,且以TMC60与CLXL物理混合物促进作用较强,与氮酮CXCL物理混合物的促进作用差异无统计学意义（P＞0.05）.结论 TMC60可显著促进CLXL的体外透皮效果,且以TMC60与CLXL物理混合物的促进作用较好.

Study on transdermal enhancement of N-trimethyl chitosan on celecoxib liposomes in vitro

Objective To study the transdermal enhancement of N-trimethyl chitosan with quaternization degree of 60% （TMC60） on celecoxib liposomes （CLXL） in vitro. Methods CLXL were prepared with TMC60-eoating or TMC60-mixing. The morphology, size,Zeta potential and entrapment efficiency of CLXL after TMC60-coating were observed. Azone as the positive control, the in vitro transdermal penetration of CLXL, TMC60-coated CLXL and the mixture of TMC60 and CLXL was studied by using Franz diffusion cells. Results After TMC60-coating, the morphology showed notable coating layer with increased size, positive charge and intact entrapment efficiency. Compared with CLXL, TMC60-coated CLXL, the mixture of TMC60 and CLXL and the mixture of Azone and CLXL all exhibited enhanced accumulative transdermal penetration amount and rate （ P 〈 0.05 ） , and the mixture of TMC60 and CLXL showed better enhancement than TMC60-coated CLXL with no significant difference from the mixture of Azone and CLXL （ P 〉 O. 05 ）. Conclusion TMC60 shows promising enhancement on the transderInal penetration of CLXL, and the mixture is better than the coating.