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Abstract

Improving the Oral Absorption of Celecoxib via Solid Self-Microemulsion Drug Delivery System: Preparation and In Vitro/In Vivo Evaluation

Author(s): Xin Zhang, Xiaowen Wu, Yingshu Feng, Caleb Kesse Firempong, Quanzhu Yang, Tianxiang Chen, Dongli Li and Hongfei Liu*
School of Biotechnology and Health Sciences, Wuyi University, Jiangmen 529000, 1College of Pharmacy, Jiangsu University, Zhenjiang 212013, 2Jiangmen Hongxiao Biomedical Co., Ltd, Jiangmen 529000, 3Zhenjiang Key Laboratory of Functional Chemistry, Institute of Medicine and Chemical Engineering, Zhenjiang College, Zhenjiang, 212028, 4Jiangsu Sunan Pharmaceutical Industrial Co., LTD, Zhenjiang, 212400, China

Correspondence Address:
Hongfei Liu, Jiangmen Hongxiao Biomedical Co., Ltd, Jiangmen 529000, China, E-mail: liuhongfei2000@163.com


Celecoxib is a specific cyclooxygenase-2 inhibitor with poor solubility and low bioavailability. A solid self-microemulsifying drug delivery system of celecoxib was therefore developed to improve in vitro drug solubility and in vivo absorption. Solubility testing, compatibility testing and pseudo-ternary phase diagrams were employed in the design. Morphological observation, droplet size and in vitro release were used to characterize the formulation. The optimized celecoxib-liquid self-microemulsifying drug delivery system was determined as 10 % of celecoxib, 25 % of medium chain triglycerides, 56.25 % of emulsifier and 18.75 % of Transcutol HP. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide assay was used to investigate the cytoxicity of active pharmaceutical ingredients, blank self-microemulsion and celecoxib liquid self-microemulsifying drug delivery system on Caco-2 cells. Celecoxib solid self-microemulsifying drug delivery system was prepared with Neusilin-US2 as a solid adsorbent and characterized using scanning electron microscopy, X-ray, Fourier-transform infrared spectroscopy, differential scanning calorimetry and in vitro release. Celecoxib liquid self-microemulsifying drug delivery system had a clear and transparent light-yellow appearance with average particle size of about 22.68 nm, zeta potential of -31.92 mv, and polydisperse coefficient of 0.141. 3-[4,5-dimethylthiazol-2-yl]-2,5 diphenyl tetrazolium bromide results showed that the formulations virtually had no cytotoxic effect on the cells. The results also showed that celecoxib existed in an amorphous state in celecoxib-solid self-microemulsifying drug delivery system, and the celecoxib-liquid self-microemulsifying drug delivery system and celecoxib-solid-self-microemulsifying drug delivery system had a dissolution degree of more than 90 % in different media with good stability. The pharmacokinetic studies showed that the area under curve of the liquid self-microemulsifying drug delivery system and self-microemulsifying drug delivery system increased by 6.59 and 6.37 folds, respectively, compared with celecoxib suspension. The findings showed that the developed solid self-microemulsion formulations improved the bioavailability of the drug with no cytotoxicity, hence the formulation can serve as a promising carrier for the oral delivery of celecoxib.

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