Document Detail


Microemulsions for topical delivery of estradiol.
MedLine Citation:
PMID:  12623186     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Estradiol has been widely used for the treatment of hormonal insufficiencies. Due to its extensive first pass metabolism after oral administration, transdermal administration of estradiol in gels and emulsions has been used to improve its bioavailability, prolong activity and to optimize metabolic profile. The purpose of this study was to investigate microemulsions as delivery systems for estradiol. Various o/w microemulsions were used to deliver estradiol across human abdominal skin in vitro. Trasdermal flux of estradiol was determined using Franz-type diffusion cells and the samples were analyzed by high-performance liquid chromatography (HPLC). The permeation data showed that microemulsion formulations increased estradiol flux 200-700-fold over the control, but permeability coefficients were decreased by 5-18 times. The superior transdermal flux of estradiol was due to 1500-fold improvement in solubilization of estradiol by microemulsions. The results suggest that microemulsions are potential vehicles for improved topical delivery of estradiol.
Authors:
S Peltola; P Saarinen-Savolainen; J Kiesvaara; T M Suhonen; A Urtti
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Publication Detail:
Type:  In Vitro; Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  254     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2003 Mar 
Date Detail:
Created Date:  2003-03-07     Completed Date:  2003-09-22     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  99-107     Citation Subset:  IM    
Copyright Information:
Copyright 2002 Elsevier Science B.V.
Affiliation:
Department of Pharmaceutics, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland.
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MeSH Terms
Descriptor/Qualifier:
Adjuvants, Pharmaceutic / pharmacology
Administration, Cutaneous
Chromatography, High Pressure Liquid
Drug Stability
Emulsions / chemistry*
Estradiol / administration & dosage*,  chemistry,  pharmacokinetics
Ethanol / pharmacology
Humans
Particle Size
Permeability
Skin Absorption
Solubility
Chemical
Reg. No./Substance:
0/Adjuvants, Pharmaceutic; 0/Emulsions; 50-28-2/Estradiol; 64-17-5/Ethanol

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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