Buoyant in situ Gels of Meloxicam-b-Cyclodextrin-Triethanolamine Ternary Complex for Oral Delivery; From a Box-Behnken Experimental Design to in vivo Activity Detail

Mohammed Jafar1,*, Mohammed Salahuddin2, Tarek S. Kayed3, Niyaz Ahmad1, Huda A. Al-Eid1 and Abdullah H. Al-Qarros1

1Department of Pharmaceutics, College of Clinical Pharmacy, University of Dammam, P.O. Box 1982, Dammam-31441, Saudi Arabia

2Institute for Research and Medical Consultation studies, University of Dammam, P.O. Box 1982, Dammam-31441, Saudi Arabia

3Department of Basic Sciences and Humanities, College of Engineering, University of Dammam, P.O. Box 1982, Dammam-31441, Saudi Arabia

*Corresponding author: Tel: +966 502467326; E-mail: mjomar@uod.edu.sa

Abstract

The aim of the present study was to ameliorate the aqueous solubility and dissolution rate of meloxicam by preparing its ternary complex with b-cyclodextrin and triethanolamine and to develop its gastric buoyant in situ gels to improve in vivo anti-inflammatory activity of meloxicam. Meloxicam-b-cyclodextrin-triethanolamine ternary complexes were characterized by FTIR, XRD and SEM techniques. A total of fifteen meloxicam-b-cyclodextrin-triethanolamine ternary complex incorporated buoyant in situ gels were prepared and optimized using a Box-Behnken design. Independent variables (concentrations of gellan gum, calcium carbonate and meloxicam respectively) were optimized in order to achieve the desired responses. The response surface plots and the possible interactions between the independent variables were analyzed using the Design Expert software 10.0.3. (Stat-Ease, Inc, USA). The results showed that the optimized buoyant in situ gels with short floating lag time (0.7 min), low viscosity (210 cps) and high in vitro drug release at 6th hour (92 %) was obtained using an optimized combination of calcium carbonate (0.75 % w/v), gellan gum (0.25 %w/v) and MLX-b-CD-TEA ternary complex (equivalent to 11 mg of meloxicam), respectively. The optimized formulation exhibited significantly high anti-inflammatory activity compared to in situ gel containing pure meloxicam. It was stable for over 3 months. Hence it may be used for the effective oral delivery of meloxicam.

Keywords

Meloxicam, Inclusion complex, Solubility, in situ gel, in vivo activity.

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