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(123.4±1.9)nm；在12 h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。
Abstract
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 TPSLN formulations were assessed by an in vitro permeation technique using modified Franzdiffusion 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 inflammotory 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.
关键词
雷公藤内酯醇 /
固体脂质纳米粒 /
经皮渗透 /
抗炎作用
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Key words
triptolide /
solid lipid nanoparticle /
transdermal absorption /
anti inflammatory activity
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参考文献
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脚注
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基金
国家“863”计划(2001AA218051)及“十五”科技攻关(2001BA310A07)资助项目
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