Enhanced oral bioavailability of nevirapine within micellar nanocarriers compared with Viramune®

MORETTON M.A.; COHEN L.; LEPERA L.; BERNABEU E.; TAIRA C.; HOCHT C.; CHIAPPETTA D.A.

COLLOIDS AND SURFACES B-BIOINTERFACES

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2014 vol. 122 p. 56 - 65

0927-7765

In this work, Nevirapine (NVP) was encapsulated within three derivatives of poly(ethylene oxide)?poly(propylene oxide)?poly(ethylene oxide) (PEO?PPO?PEO) block copolymers (Tetronic®904,1107 and Pluronic®F127) with and without the addition of three pharmaceutical cosolvents (glycerin, propylene glycol and polyethylene glycol 400) over a wider range of concentrations (0?40% v/v). Also, we evaluated the effect of addition of the cosolvents on the micellar size as determined by dynamic light scattering (DLS) measurements and transmission electron microscopy (TEM). The solubilization capacity of the systems was investigated by UV-spectrophotometry (282 nm) and the systems stability was evaluated for 1 month at 25◦C. Finally, oral bioavailability of the NVP-loaded micellar systems (2 mg/mL) was assessed in male Wistar rats (8 mg/kg) and compared with a pediatric commercially available formulation (Viramune®). The present study demonstrates that PEO?PPO?PEO polymeric micelles were able to enhance apparent aqueous solubility of NVP with the addition of cosolvents. Moreover, micellar nanocarriers significantly (p < 0.05) improved the oral bioavailability of the drug versus Viramune®. Overall results support the suitability of the strategy toward the development of an optimized NVP aqueous formulation to prevent HIV/AIDS mother-to-child transmission.