Potential Use of Cyclodextrins for the Improvement of Ocular Bioavailability of Meloxicam
Journal Title: IOSR Journal of Pharmacy and Biological Sciences (IOSR-JPBS) - Year 2017, Vol 12, Issue 5
Abstract
Meloxicam (MX) is a nonsteroidal anti-inflammatory drug. Also, it is a more distinct COX-2 inhibitor than diclofenac with less secondary effects. Yet, its usage for the treatment of ophthalmic inflammations has retarded due to its low aqueous solubility and dissolution rate. The aim of this study was to prepare the inclusion complexes of MX with cyclodextrins to enhance its aqueous solubility, dissolution rate, and ocular bioavailability. Formulation of those complexes into different ocular delivery systems and also in-vitro and invivo assessments has not been accomplished in the earlier attempts. In this study, MX was complexed with each of hydroxyl propyl-β-cyclodextrin (HP-β-CyD) and β-cyclodextrin (β-CyD) utilizing kneading, co-evaporation, and freeze drying techniques. Moreover, the prepared complexes were discriminated in the solid state by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). These complexes were incorporated into eye drops, eye gels, and ocuserts using hydroxypropyl methylcellulose (HPMC), sodium carboxy methylcellulose (Sod. CMC), carbopol 940 (CP940), and sodium alginate (Sod. ALG). These formulae were characterized on the subject of drug content, pH, viscosity, in-vitro release characteristics. Kinetic analysis of the release data was done. Real inclusion complexes were obtained with co-evaporation method that confirmed by DSC investigations. The MX release was enhanced by complexation especially with HP-β-CyD. Ocular bioavailability of meloxicam from the selected formulations was investigated. In-vivo study proved that, ocuserts containing MX-HP-CyD complexes showed pronounced ocular bioavailability than MX alone which indicated by higher AUC, Cmax and relative bioavailability values.
Authors and Affiliations
Abd-Elgawad H. Abd-Elgawad, Osama A. Soliman, Marwa S. El-Dahan,, Ghada A. A. El-Emam*
Keywords
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