| Effect of 4-sulphonato-calix[n]arenes and cyclodextrins on the solubilization of niclosamide, a poorly water soluble anthelmintic. | |
| | |
MedLine Citation:
|
PMID: 16146345 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
The present study investigated the effect of water-soluble 4-sulphonato-calix[n]arenes, cyclodextrins, and combinations of these macromolecules on the aqueous solubility of a poorly water-soluble drug, niclosamide. Complexation between the macromolecules and niclosamide was confirmed by thermal analysis and phase solubility studies in a pH 7.0 Mcllvaine buffer kept at 30 degrees C. Results show that the increase in solubility ranked as follows: 4-sulphonato-calix[6]arene + hydroxypropyl-beta-cyclodextrin (HP-beta-CD) > 4-sulphonato-calix[6]arene + beta-cyclodextrin > 4-sulphonato-calix[6]arene + gamma-cyclodextrin = HP-beta-CD > 4-sulphonato-calix[6]arene > 4-sulphonato-calix[8]arene = 4-sulphonato-calix[4]arene > beta-cyclodextrin . Type B phase solubility profiles were observed, indicating a decrease in solubility at concentrations > 0.004 to 0.005 mol/L of the 4-sulphonato-calix[n]arenes or combinations of 4-sulphonato-calix[6]arene and the cyclodextrins. However, below this concentration, the greatest increase in the aqueous solubility niclosamide was observed when 4-sulphonato-calix[6]arene and HP-beta-CD were combined. This increase in solubility was additive. |
| | |
Authors:
|
Wenzhan Yang; Melgardt M de Villiers |
Related Documents
:
|
10528095 - Solubility profiles of some isoxazolyl-naphthoquinone derivatives. 12419905 - Synthesis of water-soluble polymeric prodrugs possessing 4-methylcatechol derivatives b... 3805445 - In vitro fermentation of sugars, grains, and by-product feeds in relation to initiation... 22615635 - Preparation and evaluation of poly (caprolactone fumarate) nanoparticles containing dox... 23170945 - Tailoring the chain packing in ultrathin polyelectrolyte films formed by sequential ads... 19620135 - Identification and characterization of the water gap in the physically dormant seeds of... |
Publication Detail:
|
Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2005-09-02 |
Journal Detail:
|
Title: The AAPS journal Volume: 7 ISSN: 1550-7416 ISO Abbreviation: AAPS J Publication Date: 2005 |
Date Detail:
|
Created Date: 2005-09-08 Completed Date: 2006-02-23 Revised Date: 2010-09-20 |
Medline Journal Info:
|
Nlm Unique ID: 101223209 Medline TA: AAPS J Country: United States |
Other Details:
|
Languages: eng Pagination: E241-8 Citation Subset: IM |
Affiliation:
|
Department of Basic Pharmaceutical Sciences, School of Pharmacy, University of Louisiana, Monroe, LA 71209, USA. |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Anthelmintics
/
chemistry* Arylsulfonates / chemistry Calixarenes / pharmacology* Calorimetry, Differential Scanning Cyclodextrins / pharmacology* Excipients Hydrophobicity Molecular Structure Molecular Weight Niclosamide / chemistry* Osmolar Concentration Solubility Solutions Water |
| Chemical | |
Reg. No./Substance:
|
0/Anthelmintics; 0/Arylsulfonates; 0/Cyclodextrins; 0/Excipients; 0/Solutions; 130036-26-9/Calixarenes; 50-65-7/Niclosamide; 7732-18-5/Water |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: Controlled release of dexamethasone from PLGA microspheres embedded within polyacid-containing PVA h...
Next Document: A random sampling approach for robust estimation of tissue-to-plasma ratio from extremely sparse dat...