Mohammadi Mojdeh, Elahimehr Zohreh, Mahboobian Mohammad Mehdi
Department of Pharmacology & Toxicology, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Curr Eye Res. 2021 Nov;46(11):1646-1652. doi: 10.1080/02713683.2021.1929328. Epub 2021 May 25.
The main goal of the present work was to develop and evaluate nanoemulsions (NEs) containing acyclovir (ACV) for ophthalmic drug delivery. Firstly, component screening was performed by determining ACV solubility in various oils, surfactants, and co-surfactants. Different NE formulations were developed based on pseudo-ternary phase diagrams, and physicochemical assets were evaluated. Selected formulations were subjected to the drug release efficacy, stability studies, and ex-vivo trans-corneal permeation test. The safety of NEs was investigated by the modified Draize test and hen's egg test-chorioallantoic membrane (HET-CAM). Based on the solubility studies, Tween 20, Triacetin, and TramsectolP were chosen to prepare NE formulations. Developed NEs showed desirable physiochemical properties, including a droplet size of less than 15 nm. Selected formulations (F1 and F2) exhibited a sustained drug release pattern compared to the control group ( < .001). ACV penetration from F1 and F2 to the excised bovine cornea was 2.85 and 2.9-fold more than the control, respectively. Furthermore, HET-CAM and modified Draize test confirmed that F1 and F2 were safe for ocular administration. Present investigation revealed that ACV-loaded NEs could be effective, and safe platform for ophthalmic delivery of ACV.
本研究的主要目标是开发和评估用于眼科药物递送的含阿昔洛韦（ACV）的纳米乳剂（NEs）。首先，通过测定阿昔洛韦在各种油、表面活性剂和助表面活性剂中的溶解度进行成分筛选。基于伪三元相图开发了不同的纳米乳剂配方，并对其物理化学性质进行了评估。对选定的配方进行药物释放效果、稳定性研究和离体角膜渗透试验。通过改良的Draize试验和鸡胚绒毛尿囊膜试验（HET-CAM）研究纳米乳剂的安全性。基于溶解度研究，选择吐温20、三醋精和反式茴香脑来制备纳米乳剂配方。所开发的纳米乳剂表现出理想的物理化学性质，包括液滴尺寸小于15nm。与对照组相比，选定的配方（F1和F2）呈现出持续的药物释放模式（<0.001）。阿昔洛韦从F1和F2渗透到切除的牛角膜中的量分别比对照组高2.85倍和2.9倍。此外，HET-CAM和改良的Draize试验证实F1和F2用于眼部给药是安全的。目前的研究表明，载阿昔洛韦的纳米乳剂可能是一种有效且安全的阿昔洛韦眼科递送平台。
