Bonde Smita, Mavani Nisarg, Bonde Chandrakant
SVKM's NMIMS, School of Pharmacy and Technology Management, Shirpur Campus, Maharashtra, India.
Curr Drug Deliv. 2018;15(3):397-405. doi: 10.2174/1567201814666171013150938.
The conventional acyclovir topical therapy has a low efficacy, due to the lack of penetration of a sufficient amount of drug to the target site.
The aim of this work was to formulate and optimize organogel containing acyclovir to enhance the penetration and retention time of acyclovir in the basal epidermis, site of Herpes simplex virus infections.
Microemulsion based organogel containing acyclovir was developed using the combination of surfactants, polar and nonpolar solvents. To investigate the microemulsion and gelling region, titration was carried out and pseudoternary phase diagram was constructed. The formulation was optimized by using 3-factor, 3-level, Box-Behnken design. Response surface plots were constructed for various response variables, viz. % drug permeation, viscosity and spreadability. The optimized formulation was searched utilizing overlay plots and desirability of the response. The optimized formulation was further characterized for microscopy, pH, ex-vivo permeation etc. Ex-vivo skin permeation showed first order drug diffusion through the skin and was found being stable upto 8 hrs.
In case of developed organogel formulation, significantly higher amount of acyclovir was observed to be retained in the skin, as compared to retention observed with the conventional cream.
The results show that the ACV organogel penetrates into the skin and form the reservoir that can slowly release the drug for a longer period and may control viral growth more effectively.
传统的阿昔洛韦局部治疗疗效较低，原因是缺乏足够量的药物渗透到靶部位。
本研究旨在制备并优化含阿昔洛韦的有机凝胶，以提高阿昔洛韦在单纯疱疹病毒感染部位——基底表皮中的渗透及滞留时间。
采用表面活性剂、极性和非极性溶剂组合，开发了含阿昔洛韦的基于微乳液的有机凝胶。通过滴定法研究微乳液和凝胶化区域，并构建伪三元相图。采用三因素三水平的Box-Behnken设计对制剂进行优化。针对不同的响应变量，即药物渗透百分比、粘度和铺展性，构建响应面图。利用叠加图和响应的合意性搜索优化制剂。对优化后的制剂进行显微镜检查、pH值、体外渗透等进一步表征。体外皮肤渗透显示药物通过皮肤呈一级扩散，且在8小时内保持稳定。
与传统乳膏相比，所开发的有机凝胶制剂在皮肤中的阿昔洛韦滞留量显著更高。
结果表明，阿昔洛韦有机凝胶可渗透到皮肤中并形成储库，能够长时间缓慢释放药物，可能更有效地控制病毒生长。
