Almutairy Bjad K, Khafagy El-Sayed, Aldawsari Mohammed F, Alshetaili Abdullah, Alotaibi Hadil Faris, Lila Amr Selim Abu
Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-kharj 11942, Saudi Arabia.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.
Int J Pharm X. 2024 Mar 26;7:100240. doi: 10.1016/j.ijpx.2024.100240. eCollection 2024 Jun.
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 2 full factorial design. The optimized formula (F1) was characterized for entrapment efficiency, surface charge, vesicle size, and drug release after 12 h (Q). The optimized formula (F1) exhibited high drug entrapment efficiency (83.1 ± 2.1%), appropriate zeta potential (-19.9 ± 2.1 mV), Q of 71.3 ± 5.3%, and a vesicle size of 364.2 ± 15.8 nm, which favored their cutaneous accumulation. In addition, 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, studies verified the efficacy of spanlastic vesicles to boost the cutaneous accumulation of BIM compared to naive BIM gel; the AUC of BIM-SLG was 888.05 ± 72.31 μg/mL.h, which was twice as high as that of naïve BIM gel (AUC 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.
比马前列素(BIM)是一种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。最近的研究突出了其促进头发生长的潜力。本研究的目的是挑战Spanlastics(SLs)作为一种基于表面活性剂的囊泡系统促进BIM经皮递送以治疗脱发的潜力。以司盘为主要囊泡成分、吐温为边缘活化剂制备了载有BIM的Spanlastics(BIM-SLs),采用乙醇注入法。通过二因素全因子设计对制备的BIM-SLs进行优化。对优化配方(F1)进行包封率、表面电荷、囊泡大小和12小时后药物释放量(Q)的表征。优化配方(F1)表现出较高的药物包封率(83.1±2.1%)、合适的ζ电位(-19.9±2.1mV)、Q值为71.3±5.3%以及囊泡大小为364.2±15.8nm,这有利于其在皮肤的蓄积。此外,皮肤沉积研究表明,与单纯的BIM凝胶相比,将BIM包裹在基于Spanlastics的纳米凝胶(BIM-SLG)中可增加BIM的真皮沉积。此外,研究证实与单纯的BIM凝胶相比,Spanlastics囊泡可促进BIM在皮肤的蓄积;BIM-SLG的曲线下面积(AUC)为888.05±72.31μg/mL·h,是单纯BIM凝胶(AUC 382.86±41.12μg/mL·h)的两倍。有趣的是,在雄激素性脱发小鼠模型中,BIM-SLG在促进毛发生长方面优于单纯的BIM凝胶和市售米诺地尔制剂。总的来说,Spanlastics囊泡可能是促进BIM经皮递送治疗脱发的潜在平台。