PDF(Pubmed)
Abstract：
Bimatoprost (BIM) is a prostaglandin F2α analogs originally approved for the treatment of glaucoma and ocular hypertension. Recent studies have highlighted its potential to boost hair growth. The objective of this investigation is to challenge the potential of spanlastics (SLs) as a surfactant-based vesicular system for promoting the cutaneous delivery of BIM for the management of alopecia. BIM-loaded spanlastics (BIM-SLs), composed of Span as the main vesicle component and Tween as the edge activator, were fabricated by ethanol injection method. The formulated BIM-SLs were optimized by 23 full factorial design. The optimized formula (F1) was characterized for entrapment efficiency, surface charge, vesicle size, and drug release after 12 h (Q12h). The optimized formula (F1) exhibited high drug entrapment efficiency (83.1 ± 2.1%), appropriate zeta potential (-19.9 ± 2.1 mV), Q12h of 71.3 ± 5.3%, and a vesicle size of 364.2 ± 15.8 nm, which favored their cutaneous accumulation. In addition, ex-vivo skin deposition studies revealed that entrapping BIM within spanlastic-based nanogel (BIM-SLG) augmented the dermal deposition of BIM, compared to naïve BIM gel. Furthermore, in vivo studies verified the efficacy of spanlastic vesicles to boost the cutaneous accumulation of BIM compared to naive BIM gel; the AUC0-12h of BIM-SLG was 888.05 ± 72.31 μg/mL.h, which was twice as high as that of naïve BIM gel (AUC0-12h 382.86 ± 41.12 μg/mL.h). Intriguingly, BIM-SLG outperforms both naïve BIM gel and commercial minoxidil formulations in stimulating hair regrowth in an androgenetic alopecia mouse model. Collectively, spanlastic vesicles might be a potential platform for promoting the dermal delivery of BIM in managing alopecia.
摘要：
比马前列素(BIM)是最初被批准用于治疗青光眼和高眼压症的前列腺素F2α类似物。最近的研究强调了它促进头发生长的潜力。这项研究的目的是挑战作为基于表面活性剂的囊泡系统促进BIM皮肤输送以治疗脱发的潜力。BIM加载的asanlasics(BIM-SL),由Span作为主要囊泡成分和Tween作为边缘激活剂组成，采用乙醇注射法制备。通过23个全因子设计对配方BIM-SL进行了优化。对优化配方(F1)的包封率进行了表征，表面电荷,囊泡大小，和药物释放后12h（Q12h）。优化配方（F1）具有较高的药物包封率（83.1±2.1％），适当的zeta电位（-19.9±2.1mV），Q12h为71.3±5.3%，囊泡尺寸为364.2±15.8nm，这有利于它们的皮肤积累。此外,体外皮肤沉积研究表明，将BIM包埋在基于弹性的纳米凝胶（BIM-SLG）中可增强BIM的皮肤沉积，与幼稚的BIM凝胶相比。此外，体内研究证实,与原始BIM凝胶相比,弹性囊泡促进BIM皮肤积聚的功效;BIM-SLG的AUC0-12h为888.05±72.31μg/mL。h,这是初始BIM凝胶的两倍(AUC0-12h382.86±41.12μg/mL。h).有趣的是，BIM-SLG在刺激雄激素性脱发小鼠模型中的毛发再生方面优于原始BIM凝胶和商业米诺地尔制剂。总的来说，在治疗脱发时，弹性囊泡可能是促进BIM皮肤递送的潜在平台。
