Preparation and in vitro evaluation of tacrolimus-loaded ethosomes.
The main objective of the present work was to prepare and assess dermal delivery of tacrolimus-loaded ethosomes versus classic liposomes. Both delivery systems were characterized for particle size, polydispersity index, and entrapment efficiency (EE), by dynamic laser diffraction and ultrafiltration or dialysis methods, respectively. The results indicated that presence of ethanol in the formulations affected the particle size. In addition, ultrafiltration method was selected to determine EE due to relatively short period as compared with dialysis method. Ethosomes exhibited a significant higher EE and amount of drug in dermis in contrast to classic liposomes suggesting that ethosomes with higher entrapment capacity prompted more amount of tacrolimus to permeate through stratum corneum and reach the target of atopic dermatitis (AD). Physical stability was very well for tacrolimus-loaded ethosomes under storage condition (4 °C). Our results demonstrated that the ethosomal system might be a promising candidate for dermal delivery of tacrolimus for AD.
Institute of Medicinal Biotechnology, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China.
Guiling
G
Li
Chao
C
Fan
Xinru
X
Li
Yating
Y
Fan
Xiaoning
X
Wang
Mei
M
Li
Yan
Y
Liu
D000818:Animals; D004058:Diffusion; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D007166:Immunosuppressive Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D010743:Phospholipids / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012869:Skin Absorption / Q000502:physiology*; D016559:Tacrolimus / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*
D004337:Drug Carriers; D007166:Immunosuppressive Agents; D010743:Phospholipids; D016559:Tacrolimus