Journal
PHARMACEUTICAL RESEARCH
Volume 26, Issue 6, Pages 1324-1331Publisher
SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-009-9841-2
Keywords
amphotericin B; bioavailability; biodegradable; nephrotoxicity; oral delivery
Funding
- Department of Science and Technology (DST), Government of India
- NIPER
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Amphotericin B (AMB), an effective antifungal and antileishmanial agent associated with low oral bioavailability (0.3%) and severe nephrotoxicity, was entrapped into poly(lactide-co-glycolide) (PLGA) nanoparticles to improve the oral bioavailability and to minimize the adverse effects associated with it. The AMB-nanoparticles (AMB-NP) were prepared by nanoprecipitation method employing Vitamin E-TPGS as a stabilizer. In vitro release was carried out using membrane dialysis method. The in vitro hemolytic activity of AMB-NP was evaluated by incubation with red blood cells (RBCs). The acute nephrotoxicity profile and oral bioavailability of AMB-NP were evaluated in rats. The prepared AMB-NP formulation contained monodispersed particles in the size range of 165.6 +/- 2.9 nm with 34.5 +/- 2.1% entrapment at 10% w/w initial drug loading. AMB-NP formulation showed biphasic drug release, an initial rapid release followed by a sustained release. The AMB-NP formulation exerted lower hemolysis and nephrotoxicity as compared to FungizoneA (R). The relative oral bioavailability of the AMB-NP was found to be similar to 800% as compared to FungizoneA (R). Together, these results offer a possibility of treating systemic fungal infection and leishmaniasis with oral AMB-NP, which could revolutionize the infectious disease treatment modalities.
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