Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe
Rehmana Rashid,1 Dong Wuk Kim,1 Abid Mehmood Yousaf,1 Omer Mustapha,1 Fakhar ud Din,1 Jong Hyuck Park,1 Chul Soon Yong,2 Yu-Kyoung Oh,3 Yu Seok Youn,4 Jong Oh Kim,2 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Kor...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Dove Medical Press
2015-09-01
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| Series: | International Journal of Nanomedicine |
| Online Access: | https://www.dovepress.com/comparative-study-on-solid-self-nanoemulsifying-drug-delivery-and-soli-peer-reviewed-article-IJN |
| _version_ | 1819129930512859136 |
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| author | Rashid R Kim DW Yousaf AM Mustapha O Din FU Park JH Yong CS Oh YK Youn YS Kim JO Choi HG |
| author_facet | Rashid R Kim DW Yousaf AM Mustapha O Din FU Park JH Yong CS Oh YK Youn YS Kim JO Choi HG |
| author_sort | Rashid R |
| collection | DOAJ |
| description | Rehmana Rashid,1 Dong Wuk Kim,1 Abid Mehmood Yousaf,1 Omer Mustapha,1 Fakhar ud Din,1 Jong Hyuck Park,1 Chul Soon Yong,2 Yu-Kyoung Oh,3 Yu Seok Youn,4 Jong Oh Kim,2 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Korea; 2College of Pharmacy, Yeungnam University, Gyeongsan, South Korea; 3College of Pharmacy, Seoul National University, Seoul, South Korea; 4School of Pharmacy, Sungkyunkwan University, Suwon, South KoreaBackground: The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability.Methods: For the liquid SNEDDS formulation, Capryol 90, Cremophor EL, and Tween 80 were selected as the oil, surfactant, and cosurfactant, respectively. The nanoemulsion-forming region was sketched using a pseudoternary phase diagram on the basis of reduced emulsion size. The optimized liquid SNEDDS was converted to solid SNEDDS by spray drying with silicon dioxide. Furthermore, SMSDs were prepared using the spray drying technique with various amounts of hydroxypropylcellulose and Tween 80, optimized on the basis of their drug solubility. The SESD formulation was prepared with the same composition of optimized SMSD. The aqueous solubility, dissolution, physicochemical properties, and pharmacokinetics of all of the formulations were investigated and compared with the drug powder.Results: The drug existed in the crystalline form in SMSD, but was changed into an amorphous form in SNEDDS and SESD, giving particle sizes of approximately 24, 6, and 11 µm, respectively. All of these formulations significantly improved the aqueous solubility and dissolution in the order of solid SNEDDS ≥ SESD > SMSD, and showed a total higher plasma concentration than did the drug powder. Moreover, SESD gave a higher area under the drug concentration time curve from zero to infinity than did SNEDDS and SMSD, even if they were not significantly different, suggesting more improved oral bioavailability.Conclusion: Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.Keywords: ezetimibe, solid self-nanoemulsifying drug delivery system, solid dispersion, solubility, bioavailability |
| first_indexed | 2024-12-22T08:51:32Z |
| format | Article |
| id | doaj.art-613c851925b949f0918d0d0148a2bee2 |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-22T08:51:32Z |
| publishDate | 2015-09-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-613c851925b949f0918d0d0148a2bee22022-12-21T18:31:57ZengDove Medical PressInternational Journal of Nanomedicine1178-20132015-09-012015default6147615923917Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibeRashid RKim DWYousaf AMMustapha ODin FUPark JHYong CSOh YKYoun YSKim JOChoi HGRehmana Rashid,1 Dong Wuk Kim,1 Abid Mehmood Yousaf,1 Omer Mustapha,1 Fakhar ud Din,1 Jong Hyuck Park,1 Chul Soon Yong,2 Yu-Kyoung Oh,3 Yu Seok Youn,4 Jong Oh Kim,2 Han-Gon Choi11College of Pharmacy and Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, South Korea; 2College of Pharmacy, Yeungnam University, Gyeongsan, South Korea; 3College of Pharmacy, Seoul National University, Seoul, South Korea; 4School of Pharmacy, Sungkyunkwan University, Suwon, South KoreaBackground: The objective of this study was to compare the physicochemical characteristics, solubility, dissolution, and oral bioavailability of an ezetimibe-loaded solid self-nanoemulsifying drug delivery system (SNEDDS), surface modified solid dispersion (SMSD), and solvent evaporated solid dispersion (SESD) to identify the best drug delivery system with the highest oral bioavailability.Methods: For the liquid SNEDDS formulation, Capryol 90, Cremophor EL, and Tween 80 were selected as the oil, surfactant, and cosurfactant, respectively. The nanoemulsion-forming region was sketched using a pseudoternary phase diagram on the basis of reduced emulsion size. The optimized liquid SNEDDS was converted to solid SNEDDS by spray drying with silicon dioxide. Furthermore, SMSDs were prepared using the spray drying technique with various amounts of hydroxypropylcellulose and Tween 80, optimized on the basis of their drug solubility. The SESD formulation was prepared with the same composition of optimized SMSD. The aqueous solubility, dissolution, physicochemical properties, and pharmacokinetics of all of the formulations were investigated and compared with the drug powder.Results: The drug existed in the crystalline form in SMSD, but was changed into an amorphous form in SNEDDS and SESD, giving particle sizes of approximately 24, 6, and 11 µm, respectively. All of these formulations significantly improved the aqueous solubility and dissolution in the order of solid SNEDDS ≥ SESD > SMSD, and showed a total higher plasma concentration than did the drug powder. Moreover, SESD gave a higher area under the drug concentration time curve from zero to infinity than did SNEDDS and SMSD, even if they were not significantly different, suggesting more improved oral bioavailability.Conclusion: Among the various formulations tested in this study, the SESD system would be strongly recommended as a drug delivery system for the oral administration of ezetimibe with poor water solubility.Keywords: ezetimibe, solid self-nanoemulsifying drug delivery system, solid dispersion, solubility, bioavailabilityhttps://www.dovepress.com/comparative-study-on-solid-self-nanoemulsifying-drug-delivery-and-soli-peer-reviewed-article-IJN |
| spellingShingle | Rashid R Kim DW Yousaf AM Mustapha O Din FU Park JH Yong CS Oh YK Youn YS Kim JO Choi HG Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe International Journal of Nanomedicine |
| title | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| title_full | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| title_fullStr | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| title_full_unstemmed | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| title_short | Comparative study on solid self-nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| title_sort | comparative study on solid self nanoemulsifying drug delivery and solid dispersion system for enhanced solubility and bioavailability of ezetimibe |
| url | https://www.dovepress.com/comparative-study-on-solid-self-nanoemulsifying-drug-delivery-and-soli-peer-reviewed-article-IJN |
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