Comparative evaluation of ibuprofen and ibuprofen sodium nano micelles loaded dissolving microneedles in healthy human volunteers.

This study is aimed to fabricate dissolving microneedles of ibuprofen and Ibuprofen sodium to have comparative bioavailability of both based on their pharmacokinetic profiles in healthy humans. Microneedles (MN) are a novel third generation transdermal drug delivery technology that overcomes skin barrier and enables enhanced drug delivery. Ibuprofen has a poor water solubility while Ibuprofen sodium, the salt of ibuprofen offers better solubility in aqueous media and hence quicker absorption into blood stream. The solubility of poor aqueous-soluble ibuprofen was enhanced by Soluplus (SP). The microneedles were fabricated using micromoulding technique. Morphology, drug content, mechanical strength studies, In-vitro drug release and in-vivo release in healthy humans were carried out. In-vivo pharmacokinetic analysis in healthy human volunteers revealed a Cmax of 21.5 µg/ml ±3.28 with the Tmax of 24h and the MRT of 19.5hrs for ibuprofen, showing a prolonged stay in the body and sustained release into the blood stream. Ibuprofen sodium MNs showed quicker release into the systemic circulation with a Tmax of 2h and quick clearance as compared to ibuprofen MNs. The in-vivo findings provided evidence for the use of ibuprofen sodium MNs for acute pain while Ibuprofen MNs for sustained release analgesic effect.