Formulation development and pharmacokinetic evaluation of celecoxib loaded hydroxyl propyl methyl cellulose (HPMC) microparticles in in-vivo model.

Abstract

This investigation aimed to formulate Celecoxib-loaded microparticles for targeted delivery to the colon, employing Hydroxypropylmethylcellulose (HPMC). Celecoxib's effectiveness in managing colorectal cancer (CRC)-related pain and inflammation is compromised by its low solubility and gastrointestinal side effects. A total of seventeen formulations were synthesized through emulsion solvent evaporation (ESE) oil-in-oil technique. The physicochemical properties of the formulations were analyzed through Fourier Transform Infrared Spectroscopy, X-ray Diffraction, Scanning Electron Microscopy and Differential Scanning Calorimetry; however, rabbits served as the biological specimens in the in vivo pharmacokinetic evaluation in Rabbits plasma. Celecoxib pure drug, F1 and F2 were given to the rabbits one time dose to assess the pharmacokinetics evaluation. The average particle size for F 1 was 497.93μm and 497.93 μm for F 2. In vitro showed cumulative release rates of 88.77% for F1 and 88.85% F2 after 24 hours. FTIR analysis confirmed the compatibility of the formulation ingredients, XRD revealed a transition of Celecoxib from its crystalline to amorphous form, DSC indicated the formulations' thermal stability and SEM images showed dense, spherical microparticles. Given these factors, using HPMC micro particles to carry Celecoxib could enhance the drug delivery and released in the body and may result effective treatment with fewer side effects.