Acyclovir is an acyclic purine nucleoside analog that is highly effective in inhibiting the herpes simplex virus. However, topical acyclovir has poor efficacy because of its low skin permeability. This study aimed to develop an acyclovir gel plaster containing sponge spicules (AGP-SS) to achieve synergistic improvements in skin absorption and deposition of acyclovir. The process of preparing the gel plaster was optimized by orthogonal experiments, while the composition of the formulation was optimized using the Plackett-Burman and Box–Behnken experimental designs. The selected formula was tested for physical properties, in vitro release, stability, ex vivo permeation, skin irritation, and pharmacokinetics. The optimized formulation exhibited good physical characteristics. In vitro release and ex vivo permeation studies showed that acyclovir release from AGP-SS was dominated by diffusion with significantly higher skin permeation (20.00 ± 1.07 μg/cm²) than that of the controls (p < 0.05). Dermatopharmacokinetic analyses revealed that the maximum concentration (78.74 ± 11.12 μg/g), area under the curve (1091.81 ± 29.05 μg/g/h) and relative bioavailability (197.12) of AGP-SS were higher than those of the controls. Therefore, gel plaster containing sponge spicules show potential for development as transdermal delivery systems to achieve higher skin absorption and deposition of acyclovir, especially in deep skin layers.

阿昔洛韦是一种无环嘌呤核苷类似物，对抑制单纯疱疹病毒非常有效。然而，外用阿昔洛韦因其皮肤渗透性低而疗效较差。本研究旨在开发一种含有海绵针的阿昔洛韦凝胶膏药（AGP-SS），以协同改善阿昔洛韦的皮肤吸收和沉积。通过正交实验优化了凝胶膏药的制备过程，同时使用 Plackett-Burman 和 Box-Behnken 实验设计优化了配方的组成。对所选配方的物理性质、体外释放、稳定性、离体渗透、皮肤刺激和药代动力学进行了测试。优化后的配方表现出良好的物理特性。体外释放和离体渗透研究表明，AGP-SS 中阿昔洛韦的释放以扩散为主，皮肤渗透性 (20.00 ± 1.07 μg/cm ² ) 显着高于对照组 ( p  < 0.05)。皮肤药代动力学分析显示，AGP-SS的最大浓度（78.74±11.12μg/g）、曲线下面积（1091.81±29.05μg/g/h）和相对生物利用度（197.12）均高于对照组。因此，含有海绵针的凝胶膏药显示出作为透皮给药系统的开发潜力，以实现阿昔洛韦更高的皮肤吸收和沉积，特别是在深层皮肤层。