a Department of Pharmaceutics , College of Pharmacy, Gulf Medical University , Ajman , UAE and.
b Department of Pharmaceutical Sciences , College of Clinical Pharmacy, King Faisal University , Al-Ahsa , KSA.
J Liposome Res. 2017 Dec;27(4):283-292. doi: 10.1080/08982104.2016.1224897. Epub 2016 Sep 26.
Niosomes suggest a versatile vesicle delivery system with possible transport of drugs via topical route for skin delivery. The aim of the present research was to optimize niosome gel formulation of acyclovir and to evaluate in both in vitro and in vivo rabbit model. Niosome formulations were formulated by coacervation phase separation technique with different ratios of nonionic surfactants, phospholipids and cholesterol using 3 factorial design. Altering the surfactant concentration has influenced the drug entrapment, but not vesicle size. At high surfactant combinations, the acyclovir release from niosomes was strongly influenced by cholesterol:lecithin ratio. Ex vivo drug permeation data indicate substantial difference in flux values and was influenced by the niosome composition. Ex vivo studies using formulation (B) for drug deposition indicate greater amount of niosome being diffused into the skin layers and formed a depot, compared to commercial acyclovir cream (control). Two distinct dermatopharmacokinetic profiles were observed, in vivo, for niosome gel formulation (B) and control, which were analog to the profiles observed with ex vivo deposition studies. In vivo plasma drug level suggests low systemic exposure of acyclovir (C: 9.44 ± 2.27 ng/mL and 14.54 ± 3.11 ng/mL for niosome formulation and control, respectively). Comparison of kinetic data of acyclovir in the stratum corneum and plasma signifies that the niosome formulation forms a depot in the epidermis or dermis region. This study concludes that the niosome gel formulation (B) could be a viable vesicular system for an impressive transdermal delivery of acyclovir by topical application.
毫微囊体提供了一种多功能的囊泡给药系统，可通过局部途径将药物递送至皮肤，用于皮肤给药。本研究的目的是优化阿昔洛韦毫微囊体凝胶制剂，并在体外和体内兔模型中进行评估。毫微囊体制剂采用凝聚相分离技术，通过 3 因素设计，用不同比例的非离子表面活性剂、磷脂和胆固醇进行配方。改变表面活性剂浓度会影响药物包封率，但不会影响囊泡大小。在高表面活性剂组合下，阿昔洛韦从毫微囊体中的释放受胆固醇：卵磷脂比例的强烈影响。体外药物渗透数据表明，通量值存在显著差异，并且受毫微囊体组成的影响。使用制剂（B）进行药物沉积的离体研究表明，与市售阿昔洛韦乳膏（对照）相比，更多的毫微囊体扩散到皮肤层并形成一个储库。体内，毫微囊体凝胶制剂（B）和对照均观察到两种不同的皮肤药代动力学特征，与离体沉积研究中观察到的特征相似。体内血浆药物水平表明阿昔洛韦的全身暴露水平较低（C：毫微囊体制剂和对照分别为 9.44 ± 2.27 ng/mL 和 14.54 ± 3.11 ng/mL）。阿昔洛韦在角质层和血浆中的动力学数据比较表明，毫微囊体制剂在表皮或真皮区域形成一个储库。本研究得出结论，毫微囊体凝胶制剂（B）可能是一种可行的囊泡系统，可通过局部应用实现阿昔洛韦的令人印象深刻的经皮递药。
