Ibuprofen-loaded centrifugally spun microfibers for quick relief of inflammation in rats.

The conventional dosage forms (tablets, capsules) of ibuprofen have less potential in the suppression of pain and inflammation due to their slow dissolution rates and lower bioavailability. The aim of this study was to fabricate fibrous solid dispersion of ibuprofen for improved dissolution rate and quick therapeutic action. Drug-loaded microfibers were fabricated using centrifugal melt spinning (CMS) technique from the physical mixture of sucrose, ibuprofen and a hydrophilic polymer, PVP. These fibers were characterized by SEM, PXRD, DSC, and FTIR spectroscopy. The selected formulation was also pressed into tablets by direct compression method followed by its in vitro and in vivo characterization. The production yield of fibers was 75 ± 2% with an average diameter of 15 ± 5 µm. The drug loading efficiency (DLE) was 85 ± 5%. The tablets dissolved rapidly (<40 s). In vitro dissolution studies have shown >85% of ibuprofen dissolved from tablet within first 2 min which was ∼5 times quicker than drug alone. Dissolution efficiency has improved from 0.63 of ibuprofen to 0.95 of that in fibers with ∼7 times reduction in mean dissolution time. PXRD, and DSC have shown the amorphous state of ibuprofen in the formulation and FTIR spectra demonstrated no interaction of drug with excipients. In vivo anti-inflammatory studies using rabbits revealed a significant (p < 0.05) reduction in paw volume (mm) in the groups treated with fibrous formulation. This study concludes that microfibers produced by centrifugal melt spinning have improved dissolution rates and bioavailability of ibuprofen. Incorporation of polymer in the formulations improves the production yield and drug loading efficiency of microfibers.

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 µm, 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.