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J Biomater Sci Polym Ed ; 29(18): 2299-2311, 2018 12.
Article in English | MEDLINE | ID: mdl-30485754

ABSTRACT

A copolymeric micelle formulation of itraconazole (ITR-M) was prepared using linear-dendritic monoallyloxy poly (ethylene glycol)-b-poly (ε-caprolactone) (APEG-PCL) as drug carrier materials. DL and EE values of ITR-M were 5.70 ± 0.12% and 91.30 ± 1.90%, respectively. The micelle formulation enhanced the ITR solubility up to 30.42 µg/mL. In vitro release of ITR from the ITR-M was mainly drug diffusion process followed by the copolymer's degradation. ITR-M showed similar anti-Candida albicans activity to that of crude ITR although its release of ITR was slow and continuous. The in vivo pharmacokinetic study demonstrated that the ITR-M could improve tissue distribution of ITR. In conclusion, APEG-PCL could be a potential carrier in the development of antifungal drug delivery system.


Subject(s)
Antifungal Agents/chemistry , Drug Carriers/chemistry , Ethylene Glycols/chemistry , Itraconazole/chemistry , Micelles , Polyesters/chemistry , Animals , Antifungal Agents/pharmacokinetics , Candida albicans/drug effects , Drug Liberation , Itraconazole/pharmacokinetics , Kinetics , Male , Particle Size , Permeability , Rats, Wistar , Solubility , Tissue Distribution
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