Linked Life Data

20060457

Source:http://linkedlifedata.com/resource/pubmed/id/20060457

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
1-2
pubmed:dateCreated
2010-2-22
pubmed:abstractText
The purpose of the present study was to develop and optimize the microemulsion based transdermal therapeutic system for lacidipine (LCDP), a poorly water soluble and low bioavailable drug. The pseudo-ternary phase diagrams were developed for various microemulsion formulations composed of isopropyl myristate, Tween 80 and Labrasol. The microemulsion was optimized using a three-factor, three-level Box-Behnken design, the independent variables selected were isopropyl myristate, surfactant mixture (Tween 80 and Labrasol) and water; dependent variables (responses) were cumulative amount permeated across rat abdominal skin in 24h (Q(24); Y(1)), flux (Y(2)), and lag time (Y(3)). Mathematical equations and response surface plots were used to relate the dependent and independent variables. The regression equations were generated for responses Y(1), Y(2) and Y(3). The statistical validity of the polynomials was established, and optimized formulation factors were selected by feasibility and grid search. Validation of the optimization study with 10 confirmatory runs indicated high degree of prognostic ability of response surface methodology. The gel of optimized formulation (ME-OPT) showed a flux of 43.7microgcm(-2)h(-1), which could meet the target flux (12.16microgcm(-2)h(-1)). The bioavailability studies in rabbits showed that about 3.5 times statistically significant (p<0.05) improvement in bioavailability, after transdermal administration of microemulsion gel compared to oral suspension. The ex vivo-in vivo correlation was found to have biphasic pattern and followed type A correlation. Microemulsion based transdermal therapeutic system of LCDP was developed and optimized using Box-Behnken statistical design and could provide an effective treatment in the management of hypertension.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
pubmed:status
MEDLINE
pubmed:month
Mar
pubmed:issn
1873-3476
pubmed:author
pubmed:copyrightInfo
Copyright (c) 2009 Elsevier B.V. All rights reserved.
pubmed:issnType
Electronic
pubmed:day
30
pubmed:volume
388
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
231-41
pubmed:meshHeading
pubmed-meshheading:20060457-Administration, Cutaneous, pubmed-meshheading:20060457-Animals, pubmed-meshheading:20060457-Biological Availability, pubmed-meshheading:20060457-Calcium Channel Blockers, pubmed-meshheading:20060457-Chemistry, Pharmaceutical, pubmed-meshheading:20060457-Data Interpretation, Statistical, pubmed-meshheading:20060457-Dihydropyridines, pubmed-meshheading:20060457-Emulsions, pubmed-meshheading:20060457-Gels, pubmed-meshheading:20060457-Myristates, pubmed-meshheading:20060457-Organic Chemicals, pubmed-meshheading:20060457-Phase Transition, pubmed-meshheading:20060457-Polysorbates, pubmed-meshheading:20060457-Rabbits, pubmed-meshheading:20060457-Rats, pubmed-meshheading:20060457-Rats, Wistar, pubmed-meshheading:20060457-Skin Absorption, pubmed-meshheading:20060457-Solubility, pubmed-meshheading:20060457-Surface-Active Agents
pubmed:year
2010
pubmed:articleTitle
Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: formulation optimization, ex vivo and in vivo characterization.
pubmed:affiliation
National Facilities in Engineering and Technology with Industrial Collaboration (NAFETIC) Centre, University College of Pharmaceutical Sciences, Kakatiya University, Warangal 506 009, Andhra Pradesh, India.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't, Validation Studies