微针辅助左旋肉碱水凝胶制剂体内外经皮渗透性评价  

In vitro and in vivo transdermal evaluation of L-carnitine gel assisted by functional microneedle arrays

作　　者：张锁慧[1] 邱玉琴[1] 高云华[1] 

机构地区：[1]中国科学院理化技术研究所光化学转换和功能材料重点实验室,北京100190

出　　处：《中国新药杂志》2013年第19期2309-2313,共5页Chinese Journal of New Drugs

摘　　要：目的：探讨微针经皮给药系统对强亲水性药物左旋肉碱经皮渗透性的影响。方法：选择改良的Franze扩散池，采用针高150μm的实心硅微针阵列作用于猪耳朵皮肤进行体外经皮实验评价。制备卡波姆水凝胶作为左旋肉碱的给药载体，并与市售的左旋肉碱外用制剂进行渗透性比较。体内试验考察了大鼠贴敷左旋肉碱凝胶贴片6h血液以及皮肤中的药物浓度变化。结果：左旋肉碱微针体外累积渗透量较被动扩散提高了30倍。浓度为0．5％的卡波姆980水凝胶作为左旋肉碱药物载体，经皮渗透性优于市售制剂。体内试验表明，左旋肉碱经微针促渗后可进入体循环，在给药的1～6h期间血液以及皮肤中药物浓度保持平稳。结论：微针经皮给药系统能够有效地促进左旋肉碱的经皮渗透性，从而实现缓控释效果。Objective： To evaluate the characteristics of permeability of high hydrophilic drug L-carnitine （LC） by functional mieroneedle arrays （FMA） intradermal delivery system. Methods： In vitro study was designed to investigate permeability of LC across porcine ear skin by using solid silicon microneedles with 150 μm height in an improved Franze type diffusion cell. The carbomer hydrogel was prepared as LC carrier, and compared skin per- meability with commercially formulations. In vivo studies were performed to observe plasma and skin concentrations after applied LC patch on SD rats for 6 h. Results： The permeability of LC was enhanced about 30 times compared with passive diffusion. When 0.5% earbomer 980 hydrogel was used as LC carrier, pereutaneous release was better than commercially formulations. In vivo study showed that LC transport from skin into systemic circulation assisted by FMA. The plasma and skin concentration of LC was stable over administration period of 1 - 6 h. Conclusion： FMA delivery system can enhance the permeability of LC, and achieve controlled release effect.

关 键 词：微针经皮给药 左旋肉碱 水凝胶 血药浓度 

分 类 号：R943.43[医药卫生—药剂学]