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Nanoemulsion as a potential transdermal carrier for poorly water soluble antifungal drug Itraconazole

机译:纳米乳作为水溶性差的抗真菌药物伊曲康唑的潜在透皮载体

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The objective of our study was to design a novel nanoemulsion system of broad spectrum antifungal agent Itraconazole for its sustained and prolong action without using any additional permeation enhancer. Pseudoternary phase diagrams were constructed, and various naoemulsion formulations were prepared using combination of IPM and Olive oil (1:1) as oil, Tween 20 as a surfactant and Transcutol P® as a cosurfactant. Developed formulations were subjected to thermodynamic stability test. All the nanoemulsion formulations has small droplet size (<90 nm), uniform size distribution (PI, < 0.227) and low viscosity (<160 mP). The results showed that the droplet size and viscosity of nanoemulsion decreases with the decrease in the concentration of surfactant, whereas transdermal flux was increased. The optimized formulation, which contained Olive oil +IPM (1:1) (8 % w/w), 22% w/w Smix (Tween 20 +Transcutol P®) and water (70 % w/w) showed significant increase (P < 0.01) in the transdermal flux (0.1512±0.083 mg h~(-1) cm~(-2)). Furthermore, for the optimized formulation antifungal activity study was conducted. The result showed that prepared formula exhibited better antimicrobial activity, and can be a promising carrier for the transdermal delivery of Itraconazole for prolonged period along with reduced side effects, and offers a novel means for the treatment of fungal infections like blastomycosis, histoplasmosis, onychomycosis etc.
机译:我们研究的目的是设计一种新型的广谱抗真菌剂伊曲康唑的纳米乳液系统,该系统具有持续和延长的作用,而无需使用任何其他的渗透促进剂。构造了伪三元相图,并使用IPM和橄榄油(1:1)作为油,吐温20作为表面活性剂和TranscutolP®作为辅助表面活性剂的组合制备了各种乳液乳液配方。所开发的制剂经受热力学稳定性测试。所有的纳米乳液配方均具有较小的液滴尺寸(<90 nm),均匀的尺寸分布(PI,<0.227)和低粘度(<160 mP)。结果表明,随着表面活性剂浓度的降低,纳米乳液的液滴尺寸和粘度减小,而透皮通量增加。优化的配方包含橄榄油+ IPM(1:1)(8%w / w),22%w / w的Smix(Tween 20 + TranscutolP®)和水(70%w / w),显示出显着的增加(透皮通量(0.1512±0.083 mg h〜(-1)cm〜(-2))中的P <0.01)。此外,为了优化制剂,进行了抗真菌活性研究。结果表明,所制备的配方具有较好的抑菌活性,可以作为伊曲康唑经皮给药的有前途的载体,且副作用减少,为治疗真菌感染如芽孢杆菌病,组织胞浆菌病,灰指甲病等提供了一种新颖的手段。 。

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