摘要
目的 研究固体脂质纳米粒 (SLN)作为雷公藤内酯醇 (TP)载体的经皮渗透及抗炎活性。方法 热熔分散法制备雷公藤内酯醇固体脂质纳米粒 (TP SLN) ,采用改进的Franz扩散池体外渗透实验 ,比较了不同组成的SLN体系的经皮渗透作用 ,研究了它们对Freund’s完全佐剂所致的大鼠佐剂性关节炎的治疗作用。结果 不同的脂质、乳化剂和辅助乳化剂都能制得稳定的SLN体系 ,最小粒径可达 ( 12 3.4± 1.9)nm ;在 12h内累计透皮吸收百分率以处方B最高 ,达到了 78.5 % ,而普通溶液为 32 .4 % ,TP SLN局部给药对Freund’s完全佐剂所致的佐剂性关节炎有较强的治疗作用 ,SLN的粒径越小 ,抗炎活性越强。结论 TP SLN作为透皮给药 ,可以延缓药物的释放 ,提高药物疗效 ,降低药物不良反应。
OBJECTIVE: To study the preparation of triptolide loaded solid lipid nanoparticle for transdermal delivery and its anti-inflammatory activity. METHODS: Triptolide loaded solid lipid nanoparticle was prepared by hot melting dispersion technique. The transdermal delivery effects of different TP-SLN formulations were assessed by an in vitro permeation technique using modified Franz-diffusion cells. The anti-inflammatory activity for complete Freund's adjuvant (CFA) induced arthritis was investigated in rats. RESULTS: Stable SLN systems were obtained by different lipids, emulsifiers and co-emulsifiers. The smallest particle size was (123.4 ± 1. 9) nm. The cumulative transdermal absorption fraction during 12h of the formulation B was 78.5%, whereas that of the conventional solution was 32.4%. In addition, the smaller the particle size was, the stronger the anti-inflammatory activity was. CONCLUSION: Solid lipid nanoparticle as topical transdermal delivery system may play a role to control drug release, increase drug effects and decrease side effects.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2003年第11期854-857,共4页
Chinese Pharmaceutical Journal
基金
国家"8 63"计划 (2 0 0 1AA2 180 5 1)
"十五"科技攻关(2 0 0 1BA3 10A0 7)资助项目
