Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via Savinio, Ed. Polifunzionale, 87036 Arcavacata di Rende, Italy.
Department of Chemistry and Chemical Technologies, University of Calabria, Via P. Bucci, Cubo 14/D, Rende (Cs), Italy.
Colloids Surf B Biointerfaces. 2019 Jan 1;173:623-631. doi: 10.1016/j.colsurfb.2018.10.041. Epub 2018 Oct 19.
The low efficacy of Acyclovir topical therapy is due to its physicochemical properties that limit the permeation across the stratum corneum. The goal of this research was to evaluate the ability of biodegradable surfactant, Brij97, to self-assembly in different types of colloid systems which can improve the Acyclovir permeation and accumulation at the target site (the basal epidermis). New Acyclovir formulation based on Brij97 have been analyzed in order to investigate the effect of drug encapsulation on the structure. After that, the in vitro percutaneous permeation of Acyclovir has been compared with that one of the commercial specialty Zovirax 5%. To estimate the potential of the new formulations proposed as topical delivery, it has been essential to quantify the Acyclovir in the skin layers. The results confirmed that the self-assembly of the surfactant in different nanosized structures improved the amount of permeated Acyclovir and the formation of intracutaneous drug reservoir. Furthermore, the different lipophilicity and structural organization of carriers based on Brij97 showed different influence on the promotion of permeation. The experimental data suggest that the designed carriers could be a valid alternative to improve the efficacy of the current antiviral therapy.
阿昔洛韦局部治疗效果不佳是由于其理化性质限制了其穿过角质层的渗透。本研究的目的是评估生物可降解表面活性剂 Brij97 自组装成不同胶体系统的能力，以提高目标部位（基底层表皮）的阿昔洛韦渗透和积累。为了研究药物包封对结构的影响，对基于 Brij97 的新阿昔洛韦制剂进行了分析。然后，将阿昔洛韦的体外经皮渗透与商业特效药 Zovirax 5%的渗透进行了比较。为了评估作为局部递药的新制剂的潜力，定量测定皮肤各层中的阿昔洛韦是必不可少的。结果证实，表面活性剂在不同纳米结构中的自组装提高了渗透的阿昔洛韦的量，并形成了皮内药物储库。此外，基于 Brij97 的载体的不同亲脂性和结构组织对促进渗透有不同的影响。实验数据表明，所设计的载体可以作为提高现有抗病毒治疗效果的有效替代方法。
