Naltrexone microspheres: in vitro release and effect on morphine analgesia in mice.
Acta Pharmacol Sin
; 22(6): 530-3, 2001 Jun.
Article
em En
| MEDLINE
| ID: mdl-11747760
ABSTRACT
AIM:
To study in vitro release and in vivo effect of four different types of sustained-release naltrexone microspheres on morphine analgesia.METHODS:
Release of naltrexone from four types of biodegradable microspheres was investigated by HPLC. Their antagonist effects on morphine analgesia were observed using mouse hot-plate procedure.RESULTS:
Poly latide-co-glycolide (PLGA) composition had a remarkable effect on naltrexone release from microspheres and its antagonism towards morphine analgesia. Two formulations of PLGA 5050 formulation released more than 80 % of total naltrexone and lost their antagonism by 8 d. The PLGA 7525 formulation with 20 % and 30 % drug loadings did not release 95 % of total drug and lose antagonism until 40 d and 30 d, respectively. Increasing the drug loading enhanced naltrexone release from microspheres and seemed to shorten the analgesic antagonistic effect of naltrexone.CONCLUSION:
Antagonism by naltrexone microspheres towards morphine analgesia correlates well with the drug release in vitro.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Morfina
/
Naltrexona
/
Antagonistas de Entorpecentes
Limite:
Animals
Idioma:
En
Ano de publicação:
2001
Tipo de documento:
Article