Document Detail


Potential tuberculostatic agent: micelle-forming pyrazinamide prodrug.
MedLine Citation:
PMID:  16688684     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Pyrazinamide was condensed with the poly(ethylene glycol)-poly(aspartic acid) copolymer (PEG-PASP), a micelle-forming derivative was obtained that was characterized in terms of its critical micelle concentration (CMC) and micelle diameter. The CMC was found by observing the solubility of Sudan III in Poly(ethylene glycol)-poly(pyrazinamidomethyl aspartate) copolymer (PEG-PASP-PZA) solutions. The mean diameter of PEG-PASP-PZA micelles, obtained by analyzing the dynamic light-scattering data, was 78.2 nm. The PEG-PASP-PZA derivative, when assayed for anti-Mycobacterium activity, exhibited stronger activity than the simple drug.
Authors:
Marcia Silva; Nara L Ricelli; Omar El Seoud; Celso S Valentim; Antônio G Ferreira; Daisy N Sato; Clarice Q F Leite; Elizabeth I Ferreira
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Archiv der Pharmazie     Volume:  339     ISSN:  0365-6233     ISO Abbreviation:  Arch. Pharm. (Weinheim)     Publication Date:  2006 Jun 
Date Detail:
Created Date:  2006-05-29     Completed Date:  2006-08-03     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  0330167     Medline TA:  Arch Pharm (Weinheim)     Country:  Germany    
Other Details:
Languages:  eng     Pagination:  283-90     Citation Subset:  IM    
Affiliation:
Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo, Brazil. silvam@fcfar.unesp.br
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MeSH Terms
Descriptor/Qualifier:
Antitubercular Agents / chemical synthesis*,  pharmacology
Chemistry, Pharmaceutical
Micelles*
Microbial Sensitivity Tests
Mycobacterium tuberculosis / drug effects,  growth & development
Particle Size
Polyethylene Glycols / chemistry*
Prodrugs / chemistry*,  pharmacology
Pyrazinamide / analogs & derivatives,  chemical synthesis*,  pharmacology
Chemical
Reg. No./Substance:
0/Antitubercular Agents; 0/Micelles; 0/Polyethylene Glycols; 0/Prodrugs; 0/polyethylene glycol-block-polyaspartic acid; 98-96-4/Pyrazinamide

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


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