Spanlastic-laden nanogel as a plausible platform for dermal delivery of bimatoprost with superior cutaneous deposition and hair regrowth efficiency in androgenic alopecia

IF 5.2 2区 医学 Q1 PHARMACOLOGY & PHARMACY
Bjad K. Almutairy , El-Sayed Khafagy , Mohammed F. Aldawsari , Abdullah Alshetaili , Hadil Faris Alotaibi , Amr Selim Abu Lila
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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.

Abstract Image

含有斯潘立德的纳米凝胶是一种用于皮肤输送比马前列素的合理平台,在雄激素性脱发中具有优异的皮肤沉积和生发效果
比马前列素(BIM)是一种前列腺素 F2α 类似物,最初被批准用于治疗青光眼和眼压过高。最近的研究强调了它促进毛发生长的潜力。这项研究的目的是质疑spanlastics(SL)作为一种基于表面活性剂的囊泡系统在促进BIM的皮肤输送以治疗脱发方面的潜力。研究人员采用乙醇注射法制备了以斯潘为主要囊泡成分、吐温为边缘活化剂的负载 BIM 的spanlastics(BIM-SLs)。通过 23 全因子设计对配制的 BIM-SL 进行了优化。对优化配方(F1)进行了夹持效率、表面电荷、囊泡大小和 12 小时后药物释放量(Q12h)的表征。优化配方(F1)具有较高的药物包埋效率(83.1 ± 2.1%)、适当的 zeta 电位(-19.9 ± 2.1 mV)、71.3 ± 5.3% 的 Q12h 值和 364.2 ± 15.8 nm 的囊泡尺寸,有利于药物的皮肤蓄积。此外,体内外皮肤沉积研究表明,与原始的 BIM 凝胶相比,将 BIM 包裹在基于 spanlastic 的纳米凝胶(BIM-SLG)中可增加 BIM 的皮肤沉积。此外,体内研究证实,与纯BIM凝胶相比,spanlastic囊泡能有效促进BIM的皮肤蓄积;BIM-SLG的AUC0-12h为888.05 ± 72.31 μg/mL.h,是纯BIM凝胶(AUC0-12h为382.86 ± 41.12 μg/mL.h)的两倍。有趣的是,在雄激素性脱发小鼠模型中,BIM-SLG 在刺激毛发再生方面的效果优于天真 BIM 凝胶和米诺地尔商用制剂。总之,spanlastic 囊泡可能是促进 BIM 皮肤给药治疗脱发的潜在平台。
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来源期刊
International Journal of Pharmaceutics: X
International Journal of Pharmaceutics: X Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
6.60
自引率
0.00%
发文量
32
审稿时长
24 days
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