| Effect of fatty acids on the transdermal delivery of donepezil: In vitro and in vivo evaluation. | |
| | |
MedLine Citation:
|
PMID: 22037444 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
|
The effect of fatty acids on the skin permeation of donepezil base (DPB) and its hydrochloride salt (DPH) were studied in vitro using hairless mouse and human cadaver skin. DPB and DPH were solubilized in propylene glycol (PG) containing 1% (w/v) fatty acid, after which the in vitro permeation through hairless mouse skin and human cadaver skin were evaluated using Keshary-Chien diffusion cells. The optimized formulation obtained from the in vitro study was then tested in rats for an in vivo pharmacokinetic study. The relative in vitro skin permeation rate of donepezil (DP) through the hairless mouse skin showed a parabolic relationship with increased carbon length of the fatty acid enhancers. Among the fatty acids tested, oleic acid for DPB and palmitoleic acid for DPH showed the highest enhancing effect, respectively. Both the permeation rates of DPB and DPH evaluated in human cadaver skin were in good correlation with those in hairless mouse skin, regardless of the presence of fatty acids. This suggests that the mouse skin model serves as a useful in vitro system that satisfactorily represents the characteristics of the human skin. Moreover, based on the in vitro results, the optimal formulation that could maintain the human plasma concentration of 50ng/mL was determined to be 10mg DP with 1% (w/v) enhancer. When the DP transdermal formulations were applied to the abdominal skin of rats (2.14cm(2)), the C(ss) was maintained for 48h, among which the highest value of 52.21±2.09ng/mL was achieved with the DPB formulation using oleic acid. These results showed that fatty acids could enhance the transdermal delivery of DP and suggested the feasibility of developing a novel transdermal delivery system for clinical use. |
| | |
Authors:
|
Joonho Choi; Min-Koo Choi; Suk-Jae Chung; Chang-Koo Shim; Dae-Duk Kim |
Related Documents
:
|
7328564 - Demonstration of chemotactic factor in human gout: further characterization of occurren... 17105494 - Characterization of several amino acid transports and glutamine metabolism in molt4 hum... 2880834 - Dl-7-azatryptophan and citrulline metabolism in the cyanobacterium anabaena sp. strain 1f. 17713594 - A role for excitatory amino acids in diabetic eye disease. 11405664 - A new receptor molecule for lysine and histidine in water: strong binding of basic amin... 3128624 - Acid-base regulation following acute acidosis in seawater-adapted rainbow trout, salmo ... |
Publication Detail:
|
Type: JOURNAL ARTICLE Date: 2011-10-20 |
Journal Detail:
|
Title: International journal of pharmaceutics Volume: - ISSN: 1873-3476 ISO Abbreviation: - Publication Date: 2011 Oct |
Date Detail:
|
Created Date: 2011-10-31 Completed Date: - Revised Date: - |
Medline Journal Info:
|
Nlm Unique ID: 7804127 Medline TA: Int J Pharm Country: - |
Other Details:
|
Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
|
Copyright © 2011. Published by Elsevier B.V. |
Affiliation:
|
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, South Korea. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
|
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Oxidized phospholipid based pH sensitive micelles for delivery of anthracyclines to resistant leukem...
Next Document: Optimized dextran-polyethylenimine conjugates are efficient non-viral vectors with reduced cytotoxic...