Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.
J Pharm Sci. 2010 Aug;99(8):3533-41. doi: 10.1002/jps.22104.
The pMEL34 was loaded in elastic cationic niosomes (Tween61/Cholesterol/DDAB at 1:1:0.5 molar ratio) by chloroform film method with sonication and rehydrated with 25% ethanol. The amount of pMEL34 was determined by gel electrophoresis and gel documentation. The maximum loading of pMEL34 in elastic cationic niosomes was 150 microg/16 mg of the niosomal compositions. At 8 weeks, the remaining plasmid in the elastic niosomes kept at 4 +/- 2 degrees C, 27 +/- 2 degrees C were 49.75% and 38.57%, respectively, whereas at 45 +/- 2 degrees C, all plasmids were degraded. For transdermal absorption through rat skin investigated by Franz diffusion cells at 6 h, the fluxes of pMEL34 loaded in elastic and nonelastic niosomes in viable epidermis and dermis (VED) were 0.022 +/- 0.00 and 0.017 +/- 0.01 microg/cm(2)/h, respectively, whereas only pMEL34 loaded in elastic cationic noisome was observed in the receiver solution. The pMEL34 loaded in elastic cationic niosomes showed the highest tyrosinase gene expression demonstrating higher tyrosinase activity than the free and the loaded plasmid in nonelastic niosomes of about four times. This study has suggested the potential application of elastic cationic niosomes as an efficient topical delivery for tyrosinase gene in vitiligo therapy.
pMEL34 通过氯仿膜法加载到弹性阳离子脂双层体(摩尔比为 1:1:0.5 的 Tween61/胆固醇/DDAB)中,并用超声处理和再水化 25%乙醇。pMEL34 的量通过凝胶电泳和凝胶文档确定。弹性阳离子脂双层体中 pMEL34 的最大载药量为 150μg/16mg 脂双层体组合物。在 4°C ± 2°C、27°C ± 2°C 下保存 8 周时,弹性脂双层体中剩余的质粒分别保持 49.75%和 38.57%,而在 45°C ± 2°C 时,所有质粒均降解。通过 Franz 扩散细胞在 6 小时研究经皮透过大鼠皮肤,在活表皮和真皮(VED)中,弹性和非弹性脂双层体中负载的 pMEL34 的通量分别为 0.022 ± 0.00 和 0.017 ± 0.01μg/cm2/h,而只有弹性阳离子脂双层体中负载的 pMEL34 被观察到在接收溶液中。负载在弹性阳离子脂双层体中的 pMEL34 显示出最高的酪氨酸酶基因表达,表现出比非弹性脂双层体中负载和游离质粒高约四倍的酪氨酸酶活性。这项研究表明,弹性阳离子脂双层体作为一种有效的局部传递系统,具有在白癜风治疗中传递酪氨酸酶基因的潜力。
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