Document Detail


Enhancing effect of chitosan on nasal absorption of salmon calcitonin in rats: comparison with hydroxypropyl- and dimethyl-beta-cyclodextrins.
MedLine Citation:
PMID:  12711157     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Two types of chitosan, i.e. the free amine (CS J) and the glutamate salt (CS G), were evaluated for their enhancing effect on in vivo nasal absorption of salmon calcitonin (sCT) in rats. The results were subsequently compared with beta-cyclodextrins, one of the most commonly studied enhancers. Solutions containing sCT and chitosan (0-1.25% w/v) in isotonic phosphate buffers (IPB; pH 3.0-6.0) were nasally administered at the dose of 10 IU/kg. The plasma calcium lowering effect in each sCT-treated rat was determined by calculating the total percent decrease in plasma calcium (%D). CS J showed an increase in %D as the solution pH was decreased in accordance with the increased ionization and hydration of the free amine chitosan at the more acidic pH. However, CS G showed an increase in %D with increasing pH, with maximum hypocalcemic effect observed at pH 6.0. At their optimal pH (4.0 for CS J and 6.0 for CS G), the absorption enhancing effect of both chitosans was concentration dependent from 0.25 to 1.0% and leveled off at 1.25%. Using specific RIA, the absolute bioavailability of sCT after comparison with i.v. administration was determined to be 2.45, 1.91, and 1.22% for 1% CS J, 5% dimethyl-beta-cyclodextrin (DM-beta-CD) and control group (intranasal (in) sCT alone), respectively. Although the absolute nasal bioavailability seemed to be low when compared to the i.v. administration, the inclusion of 1% CS J resulted in two-fold increase in the AUC(0-180) of plasma sCT relative to that of the control group. Addition of 5% DM-beta-CD also led to 1.56-fold increase in absorption over the control group. All the enhancers showed significant absorption enhancement (P<0.05) with the highest effect observed with CS J. In conclusion, cationic polymer chitosan may have promising potential as a safe and effective nasal absorption enhancer of sCT.
Authors:
Prapasri Sinswat; Parkpoom Tengamnuay
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  International journal of pharmaceutics     Volume:  257     ISSN:  0378-5173     ISO Abbreviation:  Int J Pharm     Publication Date:  2003 May 
Date Detail:
Created Date:  2003-04-24     Completed Date:  2003-05-29     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  7804127     Medline TA:  Int J Pharm     Country:  Netherlands    
Other Details:
Languages:  eng     Pagination:  15-22     Citation Subset:  IM    
Affiliation:
Department of Pharmacy, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand. sprapas1@mail.utexas.edu
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MeSH Terms
Descriptor/Qualifier:
Absorption
Animals
Biological Availability
Calcitonin / pharmacokinetics*
Chitin / analogs & derivatives*,  pharmacology*
Chitosan
Cyclodextrins / pharmacology*
Dose-Response Relationship, Drug
Hydrogen-Ion Concentration
Nasal Mucosa / metabolism*
Rats
Rats, Sprague-Dawley
beta-Cyclodextrins*
Chemical
Reg. No./Substance:
0/Cyclodextrins; 0/beta-Cyclodextrins; 1398-61-4/Chitin; 47931-85-1/salmon calcitonin; 51166-71-3/heptakis(2,6-O-dimethyl)beta-cyclodextrin; 9007-12-9/Calcitonin; 9012-76-4/Chitosan; 94035-02-6/2-hydroxypropyl-beta-cyclodextrin

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


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