Document Detail

Melatonin-loaded lecithin/chitosan nanoparticles: physicochemical characterisation and permeability through Caco-2 cell monolayers.
MedLine Citation:
PMID:  19596430     Owner:  NLM     Status:  MEDLINE    
In this study, the potential of lecithin/chitosan nanoparticles (NPs) as a mucoadhesive colloidal nanosystem for transmucosal delivery of melatonin was investigated. The size, zeta potential and melatonin loading of the lecithin/chitosan NPs were investigated as a function of lecithin type (Lipoid S45, S75 and S100) and chitosan content in the preparation. The NPs were characterised by mean diameter and zeta potential ranging between 121.6 and 347.5 nm, and 7.5 and 32.7 mV, respectively, and increasing with lecithin-negative charge and chitosan content in the preparation. Melatonin loadings were up to 7.1%. All NPs were characterised by prolonged release profiles with an initial burst (approximately 25%), followed by a slow release phase. Approximately 60-70% of melatonin was released in 4h. The permeability of melatonin was investigated using Caco-2 cells as an in vitro model of the epithelial barrier. Melatonin permeability from an NP suspension prepared with Lipoid S45 lecithin and a lecithin-to-chitosan weight ratio (L/C) of 20:1 (sample C2) was significantly improved compared to the permeability of melatonin from the solution (P<0.001) and from all other NPs investigated (P<0.05). The results obtained by the cell viability studies (MTT and LDH leakage assays) showed that C2 NP suspension did not induce plasma membrane damage or decrease cell viability and could be safely applied to Caco-2 cells in the concentration range tested (<400 microg/ml).
Anita Hafner; Jasmina Lovri??; Dario Voinovich; Jelena Filipovi??-Grci??
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2009-07-09
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  381     ISSN:  1873-3476     ISO Abbreviation:  Int J Pharm     Publication Date:  2009 Nov 
Date Detail:
Created Date:  2009-09-28     Completed Date:  2010-02-04     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  205-13     Citation Subset:  IM    
Department of Pharmaceutics, Faculty of Pharmacy & Biochemistry, University of Zagreb, A. Kovacica 1, 10000 Zagreb, Croatia.
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MeSH Terms
Biocompatible Materials / chemistry*,  metabolism
Caco-2 Cells
Cell Survival / drug effects
Chitosan / chemistry*,  metabolism
Colloids / chemistry,  metabolism
Dose-Response Relationship, Drug
Drug Carriers / chemistry*,  metabolism
Drug Stability
Electric Impedance
Electrochemical Techniques
Intestinal Mucosa / metabolism
Lecithins / chemistry*,  metabolism
Melatonin / chemistry*,  metabolism
Mucins / metabolism
Nanoparticles / chemistry*,  ultrastructure
Particle Size
Suspensions / chemistry,  metabolism
Reg. No./Substance:
0/Biocompatible Materials; 0/Colloids; 0/Drug Carriers; 0/Lecithins; 0/Mucins; 0/Suspensions; 73-31-4/Melatonin; 9012-76-4/Chitosan

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