We evaluated the ability of microemulsions containing medium-chain glycerides as penetration enhancers to increase the transdermal delivery of lipophilic (progesterone) and hydrophilic (adenosine) model drugs as well as the effects of an increase in surfactant blend concentration on drug transdermal delivery. Microemulsions composed of polysorbate 80, medium-chain glycerides, and propylene glycol (1:1:1, w/w/w) as surfactant blend, myvacet oil as the oily phase, and water were developed. Two microemulsions containing different concentrations of surfactant blend but similar water/oil ratios were chosen; ME-lo contained a smaller concentration of surfactant than ME-hi (47:20:33 and 63:14:23 surfactant/oil/water, w/w/w). Although in vitro progesterone and adenosine release from ME-lo and ME-hi was similar, their transdermal delivery was differently affected. ME-lo significantly increased the flux of progesterone and adenosine delivered across porcine ear skin (4-fold or higher, p < 0.05) compared to progesterone solution in oil (0.05 +/- 0.01 microg/cm(2)/h) or adenosine in water (no drug was detected in the receptor phase). The transdermal flux of adenosine, but not of progesterone, was further increased (2-fold) by ME-hi, suggesting that increases in surfactant concentration represent an interesting strategy to enhance transdermal delivery of hydrophilic, but not of lipophilic, compounds. The relative safety of the microemulsions was assessed in cultured fibroblasts. The cytotoxicity of ME-lo and ME-hi was significantly smaller than sodium lauryl sulfate (considered moderate-to-severe irritant) at same concentrations (up to 50 microg/mL), but similar to propylene glycol (regarded as safe), suggesting the safety of these formulations.

译文

:我们评估了含有中链甘油酯作为渗透促进剂的微乳剂增加亲脂性(孕酮)和亲水性(腺苷)模型药物的透皮递送的能力,以及表面活性剂共混物浓度增加对药物透皮递送的影响。开发了由聚山梨酯80,中链甘油酯和丙二醇(1:1:1,w / w / w)作为表面活性剂共混物,肉豆蔻油作为油相和水组成的微乳液。选择了两种含有不同浓度的表面活性剂共混物但水/油比相似的微乳剂。 ME-lo所含表面活性剂的浓度低于ME-hi(47:20:33和63:14:23表面活性剂/油/水,w / w / w)。尽管从ME-lo和ME-hi释放体外孕酮和腺苷相似,但它们的透皮递送受到不同的影响。与油中的孕酮溶液(0.05 /-0.01 microg / cm(2)/ h)或腺苷溶液相比,ME-lo显着提高了跨猪耳皮肤输送的孕酮和腺苷的通量(4倍或更高,p <0.05)。水(在受体相中未检测到药物)。 ME-hi进一步增加了腺苷而不是孕酮的透皮通量(2倍),这表明表面活性剂浓度的增加代表了一种增强亲水性而不是亲脂性化合物透皮递送的有趣策略。在培养的成纤维细胞中评估了微乳液的相对安全性。在相同浓度(最高50 microg / mL)下,ME-lo和ME-hi的细胞毒性显着小于月桂基硫酸钠(被认为是中度至重度刺激物),但与丙二醇相似(被认为是安全的),表明这些配方的安全性。

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