Melt sonocrystallized piroxicam for oral delivery: particle characterization, solid state analysis, and pharmacokinetics

Abstract

Objectives: The present study investigates the effect of particle engineering technique on powder properties and pharmacokinetics of piroxicam (PXM).

Methods: PXM was subjected to melt sonocrystallization to obtain product designated as MSCPXM and characterized for various pharmacotechnical parameters, performance characteristics and pharmacokinetic evaluation.

Results: Micromeritic and rheological properties were found to be superior to the original form (OFPXM). On melt sonocrystallization, solubility and intrinsic dissolution rate were enhanced by 76.45% and 33.33%, respectively. Solid state evaluation by DSC and XRPD ruled out possibilities of polymorph formation but confirmed decreased crystallinity index. SEM analysis revealed uniformly shaped smaller drug particles of MSCPXM as compared to PXM. The thermodynamic stability of MSCPXM was monitored by XRPD and the sample was stable even after 3 months of storage at 40 ± 2°C and 75 ± 5% RH. The MSCPXM was formulated as immediate release tablets (F1 – F4) and evaluated with reference tablets of OFPXM (F0). F2 was identified as best formulation with suitable tablet characteristics and in-vitro drug release profile. Pharmacokinetic evaluation of F2 in rats supported the in-vitro data with 2.08-fold increase in bioavailability achieved at 4.8 ± 1.7 h with MSCPXM as compared to OFPXM.

Conclusions: Conclusively, melt sonocrystallization offered an efficient, solvent-free technique that can be exploited for particle designing of drugs with favorable pharmaceutical properties.

Keywords::

• melt sonocrystallization
• pharmacokinetics
• piroxicam
• solid state analysis

Declaration of interest

The authors state no conflict of interest and have received no payment in preparation of this manuscript.