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Issue 22, 2017, Issue in Progress
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Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

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Abstract

Celecoxib (CLX) is a selective cyclooxygenase-2 (COX-2) inhibitor; however, the application of CLX is compromised due to its poor aqueous solubility and low oral bioavailability. This study aims to develop a nanotechnology to overcome these issues. Celecoxib nanosuspensions (CLX-NS) were formulated using D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) as stabilizer via high pressure homogenization (HPH) and then freeze-dried to solid powder. Transmission electron microscopy (TEM), differential scanning calorimetry (DSC), X-ray powder diffraction (XRD) and Fourier transform infrared spectroscopy (FT-IR) were employed to characterize the physicochemical and pharmaceutical properties of CLX-NS lyophilization. In vitro dissolution, an in situ single-pass intestinal perfusion study, and in vivo pharmacokinetic studies were performed for further investigation. Particles of the nanosuspensions were short-rod shaped (∼388 nm) and remained in the same crystalline state as CLX coarse powder. In the test of in vitro dissolution, CLX-NS displayed a higher dissolution amount (90.8% during 60 minutes) compared to groups of CLX coarse powder (47.9%) and physical mixture (52.9%). Moreover, in situ single-pass intestinal perfusion study indicated that CLX-NS could be well absorbed in the whole intestine with the main absorption site being the duodenum. Significant improvements in Cmax and AUC0–t of CLX-NS were obtained in pharmacokinetic analyses with a 245.8% increase in relative bioavailability compared to CLX coarse powder. This study showed that nanosuspension preparations could be a promising strategy in influencing CLX absorption in gastrointestinal tract, and improving dissolution and oral bioavailability of poorly water-soluble drugs.

Graphical abstract: Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

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Article information


Submitted
25 Dec 2016
Accepted
16 Feb 2017
First published
24 Feb 2017

This article is Open Access

RSC Adv., 2017,7, 13053-13064
Article type
Paper

Preparation and evaluation of celecoxib nanosuspensions for bioavailability enhancement

J. He, Y. Han, G. Xu, L. Yin, M. Ngandeu Neubi, J. Zhou and Y. Ding, RSC Adv., 2017, 7, 13053
DOI: 10.1039/C6RA28676C

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