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Design of an anti-inflammatory composite nanosystem and evaluation of its potential for ocular drug delivery.
MedLine Citation:
PMID:  23828405     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
This study compared two specific embodiments of an ocular nanosystem (NS): one portraying a purely polymeric system, referred to as the chitosan-poly(ε-caprolactone) nanosystem, and the other based on a composite lipoidal-polymeric NS architecture utilizing phospholipids-the lipoidal-chitosan-poly(ε-caprolactone) nanosystem. Investigations undertaken were implicit to warrant inclusion in an implantable system for the intelligent treatment of inflammatory disorders (specifically ocular afflictions). Results obtained highlighted the enhanced efficacy of both NS to an indomethacin suspension in terms of tissue permeation, cell uptake, and anti-inflammatory activity. Furthermore, the size (134.3 vs. 140.7 nm); surface charge (+49.4 vs. +55.7 mV); drug incorporation efficiency (75.00% vs. 67.20%); flux across the retinal pigment epithelium-choroid-sclera (0.002951 vs. 0.001255 mg cm (-2) h(-1) ); anti-inflammatory efficacy, demonstrated by a decrease in 4-chloro-7-nitrobenzo-2-oxa-1,3-diazole complex formation (0.0031 vs. 0.0023 mmol L(-1) ) and decrease in NFκB formation (decrease in relative optical density of 0.2027 vs. 0.2420); and enhanced inflammatory cell uptake, visualized via high-speed fluorescence and confocal microscopy, all highlighted the enhanced potential of the lipoidal system compared with the purely polymeric NS for potentially targeting inflammatory disorders of the posterior segment of the eye. Mechanics energy relationships revealed the favorable hydrophilic-lipophilic balance of the composite NS compared with the purely polymeric NS. © 2013 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci.
Authors:
Lisa C Du Toit; Thirumala Govender; Trevor Carmichael; Pradeep Kumar; Yahya E Choonara; Viness Pillay
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-7-4
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  -     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2013 Jul 
Date Detail:
Created Date:  2013-7-5     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2013 Wiley Periodicals, Inc.
Affiliation:
Department of Pharmacy and Pharmacology, University of the Witwatersrand, Parktown, Johannesburg 2193, South Africa.
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