Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers
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...
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| Format: | Article |
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MDPI AG
2018-12-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/1/1 |
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| author | Kanghee Jo Jae Min Cho Hyunjoo Lee Eun Kyung Kim Hong Chul Kim Hyeongmin Kim Jaehwi Lee |
| author_facet | Kanghee Jo Jae Min Cho Hyunjoo Lee Eun Kyung Kim Hong Chul Kim Hyeongmin Kim Jaehwi Lee |
| author_sort | Kanghee Jo |
| collection | DOAJ |
| description | 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<sup>®</sup> 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<sup>®</sup> 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<sup>®</sup> US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin<sup>®</sup> 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. |
| first_indexed | 2024-04-14T01:37:32Z |
| format | Article |
| id | doaj.art-43f62d6ab7bc4b3cb8536bd84760c222 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T01:37:32Z |
| publishDate | 2018-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-43f62d6ab7bc4b3cb8536bd84760c2222022-12-22T02:19:54ZengMDPI AGPharmaceutics1999-49232018-12-01111110.3390/pharmaceutics11010001pharmaceutics11010001Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent CarriersKanghee Jo0Jae Min Cho1Hyunjoo Lee2Eun Kyung Kim3Hong Chul Kim4Hyeongmin Kim5Jaehwi Lee6College of Pharmacy, Chung-Ang University, Seoul 06974, KoreaCollege of Pharmacy, Chung-Ang University, Seoul 06974, KoreaCollege of Pharmacy, Chung-Ang University, Seoul 06974, KoreaGraduate School of Pharmaceutical Management, Chung-Ang University, Seoul 06974, KoreaGraduate School of Pharmaceutical Management, Chung-Ang University, Seoul 06974, KoreaCollege of Pharmacy, Chung-Ang University, Seoul 06974, KoreaCollege of Pharmacy, Chung-Ang University, Seoul 06974, KoreaThis 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<sup>®</sup> 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<sup>®</sup> 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<sup>®</sup> US2. Among tested hydrophilic materials, croscarmellose sodium was the most suitable to facilitate fast drug dissolution from Neusilin<sup>®</sup> 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.https://www.mdpi.com/1999-4923/11/1/1celecoxibphosphatidylcholinesolid dispersionsolubilitydissolution rate |
| spellingShingle | Kanghee Jo Jae Min Cho Hyunjoo Lee Eun Kyung Kim Hong Chul Kim Hyeongmin Kim Jaehwi Lee Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers Pharmaceutics celecoxib phosphatidylcholine solid dispersion solubility dissolution rate |
| title | Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers |
| title_full | Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers |
| title_fullStr | Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers |
| title_full_unstemmed | Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers |
| title_short | Enhancement of Aqueous Solubility and Dissolution of Celecoxib through Phosphatidylcholine-Based Dispersion Systems Solidified with Adsorbent Carriers |
| title_sort | enhancement of aqueous solubility and dissolution of celecoxib through phosphatidylcholine based dispersion systems solidified with adsorbent carriers |
| topic | celecoxib phosphatidylcholine solid dispersion solubility dissolution rate |
| url | https://www.mdpi.com/1999-4923/11/1/1 |
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