Document Detail

Skin delivery of oestradiol from lipid vesicles: importance of liposome structure.
MedLine Citation:
PMID:  11012000     Owner:  NLM     Status:  MEDLINE    
The aim of this study was to investigate the importance of liposome structure in oestradiol skin delivery as a tool for understanding the delivery mechanism from lipid vesicles. Liposomes of phosphatidylcholine (PC) (1), PC, sodium cholate; 86:14 w/w (II), PC, Span 80; 86.7:13.3 w/w (III) and PC, oleic acid: 84:16 w/w (IV) with 1 mg/ml radiolabelled drug were prepared. Saturated radiolabelled oestradiol solutions containing the components of I-IV were separately prepared in 90% w/w propylene glycol in water. In addition, saturated solutions containing cholate, Span, oleic acid and ethanol at the same concentrations used in vesicles were formulated. Oestradiol permeation through human epidermis was studied. Formulations I-IV increased oestradiol flux by 8.6, 17, 17 and 13-fold when used as vesicles compared with control and by 2.9. 4.0, 4.7 and 6.9-fold when used in solution with drug. Testing individual components in solution, relative fluxes were 2.9, 0.87, 1.1, 2.9 and 1.1 for PC, cholate. Span, oleic acid and 7% ethanol, respectively. Accordingly, it is important to prepare phospholipids as vesicles for efficient oestradiol skin delivery even after inclusion of oleic acid. Penetration enhancement is not the main mechanism for improved flux. Liposome components in solution have additive effect with a possible synergism in some cases.
G M El Maghraby; A C Williams; B W Barry
Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  204     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2000 Aug 
Date Detail:
Created Date:  2001-01-09     Completed Date:  2001-01-09     Revised Date:  2004-11-17    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  159-69     Citation Subset:  IM    
Drug Delivery Group, Postgraduate Studies in Pharmaceutical Technology, The School of Pharmacy, University of Bradford, UK.
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MeSH Terms
Chemistry, Pharmaceutical
Epidermis / metabolism*
Estradiol / pharmacokinetics*
Middle Aged
Skin Absorption / drug effects*,  physiology
Reg. No./Substance:
0/Liposomes; 50-28-2/Estradiol

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

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