Rakesh R, Anoop K R
Department of Pharmaceutics, Amrita School of Pharmacy, Amrita Vishwa Vidyapeetham University, Health Sciences Campus, Kochi, Kerala, India.
J Pharm Bioallied Sci. 2012 Oct;4(4):333-40. doi: 10.4103/0975-7406.103274.
The current study was aimed to investigate the feasibility of transdermal delivery of cromolyn sodium using a novel lipid vesicular carrier, ethosomes.
Ethosomes of cromolyn sodium was prepared, optimized, and characterized for vesicle shape, vesicle size and size distribution, zeta potential, entrapment efficiency, in vitro drug release, in vitro skin permeation, in vitro skin deposition and vesicle stability. Histological examination of porcine ear skin treated with optimized ethosomal formulation was performed to study the change of skin morphologies.
The optimized cromolyn sodium ethosomes showed reasonable entrapment efficiency (49.88±1.84%), optimum nanometric size range (133.8 ± 7.5 nm), and high zeta potential (-69.82 ± 1.2 mV). In vitro drug release studies of optimized ethosomal formulation through cellophane membrane showed an enhanced and sustained delivery of drug compared to conventional liposomes, hydroethanolic, (45% v/v) and phosphate buffer saline PBS pH 7.4 drug solutions. The optimized ethosomal formulation showed significantly-enhanced transdermal flux (18.49 ± 0.08 mg/cm(2)/h) across porcine ear skin as compared to liposome (1.80 ± 0.12 mg/cm(2)/h), hydroethanolic drug solution (4.45 ± 0.71 mg/cm(2)/h), and PBS pH 7.4 drug solution (1.18 ± 0.35 mg/cm(2)/h). Moreover, ethosomal formulation showed better skin drug deposition (10.28 ± 0.67%) and shortest lag time (0.11 ± 0.09 h) for cromolyn sodium.
Our significant results suggest that ethosomes can be a promising tool for transdermal delivery of cromolyn sodium.
本研究旨在探讨使用新型脂质囊泡载体乙醇脂质体经皮递送色甘酸钠的可行性。
制备、优化色甘酸钠乙醇脂质体，并对其囊泡形状、囊泡大小和大小分布、ζ电位、包封率、体外药物释放、体外皮肤渗透、体外皮肤沉积和囊泡稳定性进行表征。对用优化后的乙醇脂质体制剂处理的猪耳皮肤进行组织学检查，以研究皮肤形态的变化。
优化后的色甘酸钠乙醇脂质体显示出合理的包封率（49.88±1.84%）、最佳的纳米尺寸范围（133.8±7.5nm）和高ζ电位（-69.82±1.2mV）。与传统脂质体、氢乙醇溶液（45%v/v）和pH 7.4的磷酸盐缓冲盐水（PBS）药物溶液相比，优化后的乙醇脂质体制剂通过玻璃纸膜进行的体外药物释放研究显示药物递送增强且持续。与脂质体（1.80±0.12mg/cm²/h）、氢乙醇药物溶液（4.45±0.71mg/cm²/h）和pH 7.4的PBS药物溶液（1.18±0.35mg/cm²/h）相比，优化后的乙醇脂质体制剂在猪耳皮肤上显示出显著增强的透皮通量（18.49±0.08mg/cm²/h）。此外，乙醇脂质体制剂对色甘酸钠显示出更好的皮肤药物沉积（10.28±0.67%）和最短的滞后时间（0.11±0.09h）。
我们的重要结果表明，乙醇脂质体可能是经皮递送色甘酸钠的一种有前景的工具。
