维A酸泡囊凝胶剂的体外透皮扩散试验

Study on transdermal diffusion of retinoic acid in niosomal gels in vitro

目的:研究自制维A酸泡囊凝胶剂的体外透皮扩散率及皮肤内的蓄积量。方法:以酸性异丙醇为溶剂,用分光光度法在波长352nm处测定维A酸,采用离体鼠皮透皮扩散试验方法,测定维A酸泡囊凝胶对小鼠皮透皮扩散率及皮外残留量,并以市售乳膏等作对照。结果:测定方法的回收率为(99.01±0.77)%,含量为标示量的98%～99%。泡囊凝胶的透皮扩散率和皮外残留量均显著低于乳膏(分别为P<0.005,P<0.001),在皮肤内蓄积量却显著高于乳膏(P<0.001)。结论:维A酸的测定方法可靠,其泡囊凝胶药物主要蓄积于皮肤内,利于提高对皮肤病的疗效和降低全身毒性。

OBJECTIVE To study the transdermal diffusion rate and the drug amount retained in skin of self-prepared retinoic acid niosomal gels in vitro. METHODS Retinoie acid was determined by spectrophotometry at 352 nm using acidic isopropyl alcohol as the solvent;and transdermal diffusion through mouse skin and drug residue on the skin were measured with retinoie acid gels and commercial retinoic acid cream as controls in vitro. RESULTS Mean recovery of the assay method was （99. 01 ± 0. 77） % and the drug content was 98% - 990% of the labeled amount. Transdermal diffusion rate and residual rate on the skin of the niosornal gels were significantly lower than those of the cream（P〈0. 005 and P〈0. 001 ）,however, the niosotnal gels showed significantly higher drug amount retained in the skin（P〈0. 001）. CONCLUSION The assay method was reliable,and the niosomal gels showed good capacity to retain drug in the skin, which indicates the niosomal gels might enhance therapeutic efficiency against skin diseases and reduce systemic adverse reaction.