| Preparation and characterisation of polyphosphazene-based controlled release systems for naproxen. | |
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MedLine Citation:
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PMID: 8634078 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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A new polyphosphazene polymer suitable for preparation of naproxen controlled release systems has been prepared by non complete substitution of the chlorine at the phosphorus atoms of polydichlorophosphazene with phenylalanine ethyl ester and imidazole. Polymeric disks obtained by solvent evaporation were found to maintain their integrity for months either "in vivo" and "in vitro" after incubation in buffer, although the intrinsic viscosity undergoes a rapid decrease. The release rate of naproxen from the films was found to depend on thickness of the matrixes and amount of entrapped drug. "In vitro" release spikes, corresponding to initial in plasma burst after subcutaneous implantation of the films in rats, have been observed with high concentrations of drug in the matrixes. On the other end decreasing the drug concentrations in the polymer matrixes, the naproxen release approximates a zero order kinetic and a controlled release is obtained for weeks. Scanning electron microscopy showed that the disks giving spikes in drug release are characterised by the presence of naproxen crystals on the matrix surface. "In vivo" studies are demonstrating that the initial naproxen concentration spike is useful in the treatment of acute models of inflammation, while a more constant and lasting release is successful in chronic inflammation models. The degradation profile of this new polyphosphazene as well as preliminary pharmacological data are also reported. |
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Authors:
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P Caliceti; S Lora; F Marsilio; F M Veronese |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Farmaco (Società chimica italiana : 1989) Volume: 50 ISSN: 0014-827X ISO Abbreviation: Farmaco Publication Date: 1995 Dec |
Date Detail:
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Created Date: 1996-07-11 Completed Date: 1996-07-11 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 8912641 Medline TA: Farmaco Country: ITALY |
Other Details:
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Languages: eng Pagination: 867-74 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutical Sciences, Centro di Studio di Chimica del Farmaco e dei Prodotti Biologicamente Attivi del CNR University of Padova, Italy. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Inflammatory Agents, Non-Steroidal / administration & dosage* Drug Delivery Systems* Male Naproxen / administration & dosage*, pharmacokinetics Polymers Rats Rats, Sprague-Dawley |
| Chemical | |
Reg. No./Substance:
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0/Anti-Inflammatory Agents, Non-Steroidal; 0/Polymers; 22204-53-1/Naproxen |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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