In vitro skin permeation of estradiol from various proniosome formulations.
The skin permeation of estradiol from various proniosome gel formulations across excised rat skin was investigated in vitro. The encapsulation efficiency and size of niosomal vesicles formed from proniosomes upon hydration were also characterized. The encapsulation (%) of proniosomes with Span surfactants showed a very high value of about 100%. Proniosomes with Span 40 and Span 60 increased the permeation of estradiol across skin. Both penetration enhancer effect of non-ionic surfactant and vesicle-skin interaction may contribute to the mechanisms for proniosomes to enhance estradiol permeation. Niosome suspension (diluted proniosomal formulations) and proniosome gel showed different behavior in modulating transdermal delivery of estradiol across skin. Presence or absence of cholesterol in the lipid bilayers of vesicles did not reveal difference in encapsulation and permeation of the associated estradiol. The types and contents of non-ionic surfactant in proniosomes are important factors affecting the efficiency of transdermal estradiol delivery.
Fang
J Y
JY
School of Pharmacy, Kaohsiung Medical University, 100 Shih-Chuan 1st Road, 807, Kaohsiung, Taiwan.
Yu
S Y
SY
Wu
P C
PC
Huang
Y B
YB
Tsai
Y H
YH
D002482:Cellulose; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding; D004958:Estradiol / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008567:Membranes, Artificial; D008861:Microsomes; D010316:Particle Size; D010713:Phosphatidylcholines; D010743:Phospholipids; D012869:Skin Absorption / Q000502:physiology*; D013501:Surface-Active Agents
D008567:Membranes, Artificial; D010713:Phosphatidylcholines; D010743:Phospholipids; D013501:Surface-Active Agents; D004958:Estradiol; D002482:Cellulose