Abdulbaqi Ibrahim M, Darwis Yusrida, Assi Reem Abou, Khan Nurzalina Abdul Karim
School of Pharmaceutical Sciences, Universiti Sains Malaysia, Minden, Penang, Malaysia.
Drug Des Devel Ther. 2018 Apr 9;12:795-813. doi: 10.2147/DDDT.S158018. eCollection 2018.
Colchicine is used for the treatment of gout, pseudo-gout, familial Mediterranean fever, and many other illnesses. Its oral administration is associated with poor bioavailability and severe gastrointestinal side effects. The drug is also known to have a low therapeutic index. Thus to overcome these drawbacks, the transdermal delivery of colchicine was investigated using transethosomal gels as potential carriers.
Colchicine-loaded transethosomes (TEs) were prepared by the cold method and statistically optimized using three sets of 24 factorial design experiments. The optimized formulations were incorporated into Carbopol 940 gel base. The prepared colchicine-loaded transethosomal gels were further characterized for vesicular size, dispersity, zeta potential, drug content, pH, viscosity, yield, rheological behavior, and ex vivo skin permeation through Sprague Dawley rats' back skin.
The results showed that the colchicine-loaded TEs had aspherical irregular shape, nanometric size range, and high entrapment efficiency. All the formulated gels exhibited non-Newtonian plastic flow without thixotropy. Colchicine-loaded transethosomal gels were able to significantly enhance the skin permeation parameters of the drug in comparison to the non-ethosomal gel.
These findings suggested that the transethosomal gels are promising carriers for the transdermal delivery of colchicine, providing an alternative route for drug administration.
秋水仙碱用于治疗痛风、假性痛风、家族性地中海热及许多其他疾病。其口服给药生物利用度低，且伴有严重的胃肠道副作用。该药物还具有较低的治疗指数。因此，为克服这些缺点，研究了以转乙缩醛磷脂体凝胶作为潜在载体进行秋水仙碱的透皮给药。
采用冷法制备载秋水仙碱的转乙缩醛磷脂体（TEs），并使用三组24析因设计实验进行统计学优化。将优化后的制剂加入卡波姆940凝胶基质中。对所制备的载秋水仙碱转乙缩醛磷脂体凝胶进一步进行囊泡大小、分散度、ζ电位、药物含量、pH值、粘度、产率、流变学行为以及通过斯普拉格-道利大鼠背部皮肤的离体皮肤渗透特性表征。
结果表明，载秋水仙碱的转乙缩醛磷脂体呈非球形不规则形状，尺寸在纳米范围内，包封率高。所有配制的凝胶均表现出非牛顿塑性流动且无触变性。与非乙缩醛磷脂体凝胶相比，载秋水仙碱转乙缩醛磷脂体凝胶能够显著提高药物的皮肤渗透参数。
这些研究结果表明，转乙缩醛磷脂体凝胶是秋水仙碱透皮给药的有前景的载体，为药物给药提供了一条替代途径。
