Almehmady Alshaimaa M, Ali Sarah A
Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Department of Oral Diagnostic Sciences, Faculty of Dentistry, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
Pharmaceutics. 2021 May 7;13(5):669. doi: 10.3390/pharmaceutics13050669.
The exponentially mounting cases of herpes simplex virus infection or cold sores have become a serious global concern. Acyclovir (ACV) and garlic oil (GO)-loaded lipid nanocarrier could be a promising therapeutic approach in alleviating cold sores, as well as limiting the biopharmaceutical constraints associated with ACV absorption and therapeutic efficacy. Therefore, the objective of the current research study was to formulate an ACV-GO self-nanoemulsifying drug delivery system (ACV-GO-SNEDDS) as transdermal films. The prepared SNEDDS was optimized using an experimental mixture design. The optimized ACV-GO SNEDDS was loaded in transdermal film and was evaluated for ex vivo skin permeation and in vivo pharmacokinetic prospects. An optimized ACV-GO SNEDDs formulation constituted of 10.4% () of GO, 64.8% () of surfactant mixture (Tween 20-Span 20); 24.8%() of co-surfactant (Propylene glycol), and 200mg of ACV, respectively, were prepared and characterized for particle size (Y). The observed globule size of the optimized ACV-GO SNEDDS is 170 ± 13.45 nm. The results of stability studies indicated that the stability index of optimized ACV-GO-SNEDDS was more than 92 ± 3%. This optimized ACV-GO SNEDDS was loaded in hydroxypropyl cellulose transdermal film. The outcome of the ex vivo skin permeation study demonstrated a 2.3-fold augmented permeation of ACV from the optimized ACV-GO SNEDDS HPC transdermal film in comparison to the raw ACV transdermal film. There was a 3-fold increase in the relative bioavailability of the optimized ACV-GO SNEDDS transdermal film compared to the raw ACV-HPC film. The study findings confirmed that the ACV-GO SNEDDS transdermal film exhibited excellent potential to enhance the bioavailability of ACV.
单纯疱疹病毒感染或唇疱疹病例呈指数级增长，已成为全球严重关切的问题。负载阿昔洛韦（ACV）和大蒜油（GO）的脂质纳米载体可能是缓解唇疱疹以及限制与ACV吸收和治疗效果相关的生物制药限制的一种有前景的治疗方法。因此，当前研究的目的是制备一种阿昔洛韦-大蒜油自纳米乳化药物递送系统（ACV-GO-SNEDDS）作为透皮膜。使用实验混合物设计对制备的SNEDDS进行优化。将优化后的ACV-GO SNEDDS负载到透皮膜中，并对其进行体外皮肤渗透和体内药代动力学前景评估。制备了一种优化的ACV-GO SNEDDs制剂，分别由10.4%（）的GO、64.8%（）的表面活性剂混合物（吐温20-司盘20）、24.8%（）的助表面活性剂（丙二醇）和200mg的ACV组成，并对其粒径（Y）进行了表征。优化后的ACV-GO SNEDDS的观察到的球粒大小为170±13.45nm。稳定性研究结果表明，优化后的ACV-GO-SNEDDS的稳定性指数超过92±3%。这种优化后的ACV-GO SNEDDS被负载到羟丙基纤维素透皮膜中。体外皮肤渗透研究结果表明，与未加工的ACV透皮膜相比，优化后的ACV-GO SNEDDS HPC透皮膜中ACV的渗透增加了2.3倍。与未加工的ACV-HPC膜相比，优化后的ACV-GO SNEDDS透皮膜的相对生物利用度提高了3倍。研究结果证实，ACV-GO SNEDDS透皮膜具有提高ACV生物利用度的优异潜力。
