Improved bioavailability of oxcarbazepine, a BCS class II drug by centrifugal melt spinning: In-vitro and in-vivo implications

Poor bioavailability is a major obstacle in the development of an effective dosage form of the poorly soluble drugs. The present study aimed to improve the dissolution rate of a poorly soluble drug oxcarbazepine (OXC) exploiting the approach of surface area enhancement by fabricating drug loaded microfibers via centrifugal melt spinning (CMS) technique. For the generation of OXC loaded fibers, a well-known cotton candy process was used and the prepared fibers were characterized using SEM, DSC, XPRD and FTIR. Drug loaded fibers were also pressed into tablets which were also subjected to various in-vitro and in-vivo characterizations. The results have shown the formations of stable, amorphous, micro sized fibers, with average diameter of 6.0 +/- 2 mu m, loading efficiency > 80% and overall yield > 85%. In-vitro dissolution of OXC from fibers was > 90% within two minutes, which is - 5 times faster than that of pure drug. Pharmacokinetic data showed an improvement of - 25% and 35% in Cmax and AUC, respectively with two hours earlier Tmax. In-vivo studies in human oral cavity showed quick disintegration (45 +/- 5 s) with > 90% OXC dissolved. The study concludes that the OXC incorporated in microfibers showed rapid in-vitro and in-vivo (oral) dissolution which resulted in rapid systemic absorption and improved bioavailability parameters. Furthermore, the addition of PVP boosted the extrusion process and stability of fibers and the sucrose base of these fibers has masked the taste of OXC making such formulation palatable, especially for pediatric patients.

Automated summary

The study aimed to enhance the dissolution rate of poorly soluble drug OXC by fabricating drug loaded microfibers via CMS technique. The results showed stable, amorphous fibers with high loading efficiency and rapid in-vitro and in-vivo dissolution, improving bioavailability parameters. The addition of PVP and sucrose base improved the extrusion process, stability of fibers, and masked the taste of OXC.