a Department of Pharmaceutics, College of Pharmacy , King Saud University , Riyadh , Saudi Arabia.
b Pharmaceutical Sciences Department, College of Pharmacy , King Saud bin Abdulaziz University for Health Sciences, King Abdullah International Medical Research Center, Ministry of National Guard, Health Affairs , Riyadh , Saudi Arabia.
Pharm Dev Technol. 2018 Oct;23(8):787-793. doi: 10.1080/10837450.2017.1330345. Epub 2017 May 26.
The objective of the current study was to formulate the eprosartan mesylate loaded transfersomes using different proportions of Phospholipon 90 G and Tween 80 (95-75:5-25% w/w). The prepared transfersomes were characterized for their vesicles size, shape, polydispersity index, zeta potential, entrapment efficiency, in vitro skin permeation, confocal laser scanning microscopy, and in vivo skin irritation. Results revealed that the formulated transfersomes were negatively charged, spherical unilamellar structure of 71.18-85.66 nm with entrapment efficiency of 83.00-88.19%, and presented transdermal flux of 1.78-5.02 μg/cm/h across rat skin. Confocal laser scanning microscopy confirmed that the formulated rhodamine 6 G loaded transfersomes could penetrate deeply and uniformly into rat skin. Additionally, in vivo skin irritation studies revealed that the prepared transfersomes were devoid of any skin irritation potential (erythema and edema). Results of this study revealed that the transfersomes prepared with Tween 80 could be used to enhance the transdermal delivery of eprosartan mesylate. In conclusion, transdermal transfersomes formulation may prove to be an encouraging drug carrier for eprosartan mesylate and other actives, particularly owing to their simple formulation and unsophisticated scale-up methods.
本研究的目的是用不同比例的 Phospholipon 90G 和 Tween 80（95-75:5-25%w/w）来制备甲磺酸依普罗沙坦的传递体。对制备的传递体进行了粒径、形态、多分散指数、Zeta 电位、包封效率、体外皮肤渗透、共聚焦激光扫描显微镜和体内皮肤刺激性评价。结果表明，所制备的传递体带负电荷，为 71.18-85.66nm 的球形单层结构，包封效率为 83.00-88.19%，在大鼠皮肤中的透皮通量为 1.78-5.02μg/cm/h。共聚焦激光扫描显微镜证实，所制备的罗丹明 6G 负载传递体能够深入且均匀地渗透到大鼠皮肤中。此外，体内皮肤刺激性研究表明，所制备的传递体没有任何皮肤刺激性（红斑和水肿）。本研究结果表明，用 Tween 80 制备的传递体可用于增强甲磺酸依普罗沙坦的透皮递送。总之，经皮传递体制剂可能被证明是甲磺酸依普罗沙坦和其他活性剂的有前途的药物载体，特别是由于其简单的制剂和不复杂的放大方法。
