Department of Pharmaceutics, Bengal College of Pharmaceutical Sciences and Research, Durgapur 713212, West Bengal, India.
Saudi Pharm J. 2012 Oct;20(4):355-63. doi: 10.1016/j.jsps.2012.02.001. Epub 2012 Feb 21.
The present study deals with the development of transferosomal gel containing insulin by reverse phase evaporation method for painless insulin delivery for use in the treatment of insulin dependent diabetes mellitus. The effect of independent process variables like ratio of lipids (soya lecithin:cholesterol), ratio of lipids and surfactants, and ratio of surfactants (Tween 80:sodium deoxycholate) on the in vitro permeation flux (μg/cm(2)/h) of formulated transferosomal gels containing insulin through porcine ear skin was optimized using 2(3) factorial design. The optimal permeation flux was achieved as 13.50 ± 0.22 μg/cm(2)/h with drug entrapment efficiency of 56.55 ± 0.37% and average vesicle diameter range, 625-815 nm. The in vitro insulin permeation through porcine ear skin from these transferosomal gel followed zero-order kinetics (R (2) = 0.9232-0.9989) over a period of 24 h with case-II transport mechanism. The in vitro skin permeation of insulin from optimized transferosomal gel by iontophoretic influence (with 0.5 mA/cm(2) current supply) also provided further enhancement of permeation flux to 17.60 ± 0.03 μg/cm(2)/h. The in vivo study of optimized transferosomal gel in alloxan-induced diabetic rat has demonstrated prolonged hypoglycemic effect in diabetic rats over 24 h after transdermal administration.
本研究通过反相蒸发法开发了一种含有胰岛素的传递体凝胶，用于无痛胰岛素传递，以治疗胰岛素依赖型糖尿病。通过 2(3) 因子设计，优化了独立过程变量（如脂质（大豆卵磷脂：胆固醇）比例、脂质和表面活性剂比例以及表面活性剂（吐温 80：脱氧胆酸钠）比例）对含有胰岛素的传递体凝胶的体外渗透通量（μg/cm(2)/h）的影响。最优渗透通量为 13.50±0.22μg/cm(2)/h，药物包封效率为 56.55±0.37%，平均囊泡直径范围为 625-815nm。这些传递体凝胶中胰岛素通过猪耳皮的体外渗透在 24 小时内遵循零级动力学（R (2) = 0.9232-0.9989），具有 II 型传输机制。优化后的传递体凝胶经离子电渗影响（电流供应 0.5 mA/cm(2)）的体外皮肤渗透也使渗透通量进一步提高到 17.60±0.03μg/cm(2)/h。优化传递体凝胶在四氧嘧啶诱导的糖尿病大鼠中的体内研究表明，在经皮给药后 24 小时内，糖尿病大鼠的降血糖作用延长。
