Balakrishnan Prabagar, Shanmugam Srinivasan, Lee Won Seok, Lee Won Mo, Kim Jong Oh, Oh Dong Hoon, Kim Dae-Duk, Kim Jung Sun, Yoo Bong Kyu, Choi Han-Gon, Woo Jong Soo, Yong Chul Soon
College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.
Int J Pharm. 2009 Jul 30;377(1-2):1-8. doi: 10.1016/j.ijpharm.2009.04.020. Epub 2009 Apr 24.
Niosomes have been reported as a possible approach to improve the low skin penetration and bioavailability characteristics shown by conventional topical vehicle for minoxidil. Niosomes formed from polyoxyethylene alkyl ethers (Brij) or sorbitan monoesters (Span) with cholesterol molar ratios of 0, 1 and 1.5 were prepared with varying drug amount 20-50mg using thin film-hydration method. The prepared systems were characterized for entrapment efficiency, particle size, zeta potential and stability. Skin permeation studies were performed using static vertical diffusion Franz cells and hairless mouse skin treated with either niosomes, control minoxidil solution (propylene glycol-water-ethanol at 20:30:50, v/v/v) or a leading topical minoxidil commercial formulation (Minoxyl). The results showed that the type of surfactant, cholesterol and incorporated amount of drug altered the entrapment efficiency of niosomes. Higher entrapment efficiency was obtained with the niosomes prepared from Span 60 and cholesterol at 1:1 molar ratio using 25mg drug. Niosomal formulations have shown a fairly high retention of minoxidil inside the vesicles (80%) at refrigerated temperature up to a period of 3 months. It was observed that both dialyzed and non-dialyzed niosomal formulations (1.03+/-0.18 to 19.41+/-4.04%) enhanced the percentage of dose accumulated in the skin compared to commercial and control formulations (0.11+/-0.03 to 0.48+/-0.17%) except dialyzed Span 60 niosomes. The greatest skin accumulation was always obtained with non-dialyzed vesicular formulations. Our results suggest that these niosomal formulations could constitute a promising approach for the topical delivery of minoxidil in hair loss treatment.
已报道囊泡可作为一种可能的方法,用于改善米诺地尔传统局部给药载体所表现出的皮肤渗透性低和生物利用度差的特性。使用薄膜水化法,以聚氧乙烯烷基醚(Brij)或脱水山梨醇单酯(Span)与胆固醇的摩尔比为0、1和1.5,制备了含药量在20 - 50mg之间变化的囊泡。对所制备的体系进行包封率、粒径、zeta电位和稳定性表征。使用静态垂直扩散弗兰兹池和用囊泡、对照米诺地尔溶液(丙二醇 - 水 - 乙醇,体积比为20:30:50)或领先的局部米诺地尔商业制剂(Minoxyl)处理的无毛小鼠皮肤进行皮肤渗透研究。结果表明,表面活性剂类型、胆固醇和药物掺入量改变了囊泡的包封率。使用25mg药物,以摩尔比1:1由Span 60和胆固醇制备的囊泡获得了更高的包封率。在冷藏温度下长达3个月的时间内,囊泡制剂显示米诺地尔在囊泡内的保留率相当高(80%)。观察到,与商业制剂和对照制剂(0.11±0.03至0.48±0.17%)相比,除了透析后的Span 60囊泡外,透析和未透析的囊泡制剂(1.03±0.18至19.41±4.04%)均提高了皮肤中累积剂量的百分比。最大的皮肤累积量总是在未透析的囊泡制剂中获得。我们的结果表明,这些囊泡制剂可能构成一种有前景的米诺地尔局部给药方法,用于脱发治疗。