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Open AccessArticle

Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers

1
College of Pharmacy, Chung-Ang University, Seoul 06974, Korea
2
Graduate School of Pharmaceutical Management, Chung-Ang University, Seoul 06974, Korea
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Pharmaceutics 2019, 11(1), 1; https://doi.org/10.3390/pharmaceutics11010001
Received: 23 November 2018 / Revised: 18 December 2018 / Accepted: 19 December 2018 / Published: 20 December 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
This study aimed to design phosphatidylcholine (PC)-based solid dispersion (SD) systems for enhancing the apparent aqueous solubility and dissolution of celecoxib (CLC), a selective cyclooxygenase-2 inhibitor with a highly hydrophobic property. Although PC-based dispersion formulations considerably increased solubilities of CLC, the lipidic texture of PC was not appropriate as a solid dosage form for oral administration of CLC. To mask the lipidic texture of PC-based matrices, Neusilin® US2, an adsorbent material with a porous structure and large surface area widely used in the pharmaceutical industry, was employed and thereby fully powderized PC-based dispersion formulations could be fabricated. However, PC matrices containing CLC strongly adsorbed to the pores of Neusilin® US2 was not able to be rapidly released. To address this problem, different hydrophilic materials were examined to promote the release of the CLC-dispersed PC matrices from Neusilin® US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin® US2 particles, showing significantly enhanced apparent aqueous solubility and dissolution behavior of CLC. Through differential scanning calorimetry, X-ray diffraction, and Fourier transform infrared spectroscopy (FT-IR) analysis, a considerably reduced crystallinity of CLC dispersed in the PC-based dispersion formulations was demonstrated. The PC-based SD formulations developed in this study would be useful for improving the oral bioavailability of poorly soluble drugs such as CLC. View Full-Text
Keywords: celecoxib; phosphatidylcholine; solid dispersion; solubility; dissolution rate celecoxib; phosphatidylcholine; solid dispersion; solubility; dissolution rate
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Jo, K.; Cho, J.M.; Lee, H.; Kim, E.K.; Kim, H.C.; Kim, H.; Lee, J. Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers. Pharmaceutics 2019, 11, 1.

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