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Papers of the Week


2022 Mar 28


Drug Dev Ind Pharm

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

Authors

Hussain A, Hussain F, Arshad M S, Abbas N, Nasir S, Mudassir J, Mahmood F, Ali E
Drug Dev Ind Pharm. 2022 Mar 28:1-19.
PMID: 35343341.

Abstract

The conventional dosage forms (tablets, capsules), of ibuprofen has less potential in suppression of pain and inflammation due to their slow dissolution rates and lower bioavailability. 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 15 ± 5 µm. The drug loading efficiency (DLE) was 85 ± 5%. The tablets dissolved rapidly (<40s). 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, andDSC have shown 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 has improved dissolution rates and bioavailability of ibuprofen. Incorporation of polymer in the formulations improves the production yield and drug loading efficiency of microfibers.