期刊
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
卷 39, 期 1-3, 页码 90-96出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.ejps.2009.10.016
关键词
Liposomes; Ultradeformable; Skin; Topical; Transdermal; Calcein
资金
- CNPq [472032/2004-6, 307726/2006-1, 501181/2007-5]
- FAPEMIG [REDE 2825/05, REDE 221/08]
Whether ultradeformable vesicles pass intact through the stratum corneum and can promote the transdermal absorption of any substance remain open questions. This paper presents different experimental approaches, based on the use of calcein as hydrophilic fluorescent market, to probe the physicochemical and pharmacokinetic characteristics of these vesicles. Ultradeformable membranes made from natural phosphatidylcholine and sodium cholate were found to be highly permeable to calcein, as a result of the permeabilizing effects of sodium cholate and ethanol. In vitro skin permeation and in vivo transdermal (percutaneous) absorption Studies were performed using hairless mice. Both studies indicated that deformable vesicles reduce the transdermal flux of calcein, when compared to a solution containing or not sodium cholate and ethanol. The data support the model that the transdermal absorption of calcein from deformable vesicles is controlled by the release of the drug from the formulation deposited onto the skin surface. Importantly, fluorescence measurements of the receptor fluid of the Franz diffusion cell after addition of Co2+ quencher revealed that permeated calcein exists essentially under the non-encapsulated form. In conclusion, our results argue against the model that deformable vesicles would carry hydrophilic drugs across the skin and act as a Sustained release system in deep tissues. (C) 2009 Elsevier B.V. All rights reserved.
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