Formulation and characterization of Phospholipon 90G and tween 80 based transfersomes for transdermal delivery of eprosartan mesylate

被引:81
作者
Ahad, Abdul [1 ]
Al-Saleh, Abdulmohsen A. [1 ]
Al-Mohizea, Abdullah M. [1 ]
Al-Jenoobi, Fahad I. [1 ]
Raish, Mohammad [1 ]
Yassin, Alaa Eldeen B. [2 ]
Alam, Mohd Aftab [1 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmaceut, POB 2457, Riyadh 11451, Saudi Arabia
[2] King Saud bin Abdulaziz Univ Hlth Sci, King Abdullah Int Med Res Ctr, Minist Natl Guard, Pharmaceut Sci Dept,Coll Pharm,Hlth Affairs, Riyadh, Saudi Arabia
关键词
Transfersomes; hypertension; skin; stratum corneum; lipid based formulation; IN-VITRO CHARACTERIZATION; RECEPTOR BLOCKERS; SKIN; LIPOSOMES; OPTIMIZATION; PERMEATION; SAFETY; SUBSTANCES; STABILITY; VESICLES;
D O I
10.1080/10837450.2017.1330345
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
The objective of the current study was to formulate the eprosartan mesylate loaded transfersomes using different proportions of Phospholipon((R)) 90G and Tween((R)) 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 71.18-85.66nm with entrapment efficiency of 83.00-88.19%, and presented transdermal flux of 1.78-5.02g/cm(2)/h across rat skin. Confocal laser scanning microscopy confirmed that the formulated rhodamine 6G 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((R)) 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.
引用
收藏
页码:787 / 793
页数:7
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