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Potential Tuberculostatic Agent: Micelle‐forming Pyrazinamide Prodrug
Author(s) -
Silva Marcia,
Ricelli Nara L.,
El Seoud Omar,
Valentim Celso S.,
Ferreira Antônio G.,
Sato Daisy N.,
Leite Clarice Q. F.,
Ferreira Elizabeth I.
Publication year - 2006
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200500039
Subject(s) - micelle , chemistry , ethylene glycol , critical micelle concentration , peg ratio , copolymer , pyrazinamide , poloxamer , prodrug , solubility , nuclear chemistry , polymer chemistry , organic chemistry , aqueous solution , polymer , biochemistry , antibiotics , finance , rifampicin , economics
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.