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Potential tuberculostatic agent: micelle-forming pyrazinamide prodrug.

作者信息

Silva Marcia, Ricelli Nara L, El Seoud Omar, Valentim Celso S, Ferreira Antônio G, Sato Daisy N, Leite Clarice Q F, Ferreira Elizabeth I

机构信息

Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, São Paulo, Brazil.

出版信息

Arch Pharm (Weinheim). 2006 Jun;339(6):283-90. doi: 10.1002/ardp.200500039.

DOI:10.1002/ardp.200500039
PMID:16688684
Abstract

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.

摘要

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