Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib
The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-06-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/6/1669 |
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| author | Yong-Han Kim Seong-Bo Kim Se-Hee Choi Thi-Thao-Linh Nguyen Sung-Hoon Ahn Kyung-Sun Moon Kwan-Hyung Cho Tae-Yong Sim Eun-Ji Heo Sung Tae Kim Hyun-Suk Jung Jun-Pil Jee Han-Gon Choi Dong-Jin Jang |
| author_facet | Yong-Han Kim Seong-Bo Kim Se-Hee Choi Thi-Thao-Linh Nguyen Sung-Hoon Ahn Kyung-Sun Moon Kwan-Hyung Cho Tae-Yong Sim Eun-Ji Heo Sung Tae Kim Hyun-Suk Jung Jun-Pil Jee Han-Gon Choi Dong-Jin Jang |
| author_sort | Yong-Han Kim |
| collection | DOAJ |
| description | The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. The various physicochemical properties of microemulsion incorporating olaparib were confirmed by investigating the morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and absorption of olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul<sup>®</sup> MCM 10%, Labrasol<sup>®</sup> 80% and PEG 400 10%. The fabricated microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that they were maintained well without any problems of physical or chemical stability. The dissolution profiles of olaparib were significantly improved compared to the value of powder. Associated with the high dissolutions of olaparib, the pharmacokinetic parameters were also greatly improved. Taken together with the results mentioned above, the microemulsion could be an effective tool as a formulation for olaparib and other similar drugs. |
| first_indexed | 2024-03-11T02:03:33Z |
| format | Article |
| id | doaj.art-b5e63d5459814f3ea40e0ef1283817e8 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T02:03:33Z |
| publishDate | 2023-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-b5e63d5459814f3ea40e0ef1283817e82023-11-18T12:04:48ZengMDPI AGPharmaceutics1999-49232023-06-01156166910.3390/pharmaceutics15061669Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble OlaparibYong-Han Kim0Seong-Bo Kim1Se-Hee Choi2Thi-Thao-Linh Nguyen3Sung-Hoon Ahn4Kyung-Sun Moon5Kwan-Hyung Cho6Tae-Yong Sim7Eun-Ji Heo8Sung Tae Kim9Hyun-Suk Jung10Jun-Pil Jee11Han-Gon Choi12Dong-Jin Jang13College of Pharmacy, Hanyang University, Ansan 15588, Republic of KoreaBio-Living Engineering Major, Global Leaders College, Yonsei University, Seoul 03722, Republic of KoreaDepartment of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of KoreaCollege of Pharmacy, Gachon University, Incheon 21936, Republic of KoreaDepartment of Pharmacy, College of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of KoreaDepartment of Pharmacy, College of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of KoreaCollege of Pharmacy, Inje University, Gimhae 50834, Republic of KoreaDepartment of Artificial Intelligence, Sejong University, Seoul 05006, Republic of KoreaDepartment of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of KoreaDepartment of Nanoscience and Engineering, Inje University, Gimhae 50834, Republic of KoreaDepartment of Biochemistry, Kangwon National University, Chuncheon 24341, Republic of KoreaCollege of Pharmacy, Chosun University, Gwangju 61452, Republic of KoreaCollege of Pharmacy, Hanyang University, Ansan 15588, Republic of KoreaDepartment of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of KoreaThe purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. Through the solubility test of olaparib in various oils, surfactants and co-surfactants, pharmaceutical excipients were selected. Self-emulsifying regions were identified by mixing the selected materials at various ratios, and a pseudoternary phase diagram was constructed by synthesizing these results. The various physicochemical properties of microemulsion incorporating olaparib were confirmed by investigating the morphology, particle size, zeta potential, drug content and stability. In addition, the improved dissolution and absorption of olaparib were also confirmed through a dissolution test and a pharmacokinetic study. An optimal microemulsion was generated in the formulation of Capmul<sup>®</sup> MCM 10%, Labrasol<sup>®</sup> 80% and PEG 400 10%. The fabricated microemulsions were well-dispersed in aqueous solutions, and it was also confirmed that they were maintained well without any problems of physical or chemical stability. The dissolution profiles of olaparib were significantly improved compared to the value of powder. Associated with the high dissolutions of olaparib, the pharmacokinetic parameters were also greatly improved. Taken together with the results mentioned above, the microemulsion could be an effective tool as a formulation for olaparib and other similar drugs.https://www.mdpi.com/1999-4923/15/6/1669olaparibself-microemulsifying drug delivery systemmicroemulsionsolubilitydissolutionoral absorption |
| spellingShingle | Yong-Han Kim Seong-Bo Kim Se-Hee Choi Thi-Thao-Linh Nguyen Sung-Hoon Ahn Kyung-Sun Moon Kwan-Hyung Cho Tae-Yong Sim Eun-Ji Heo Sung Tae Kim Hyun-Suk Jung Jun-Pil Jee Han-Gon Choi Dong-Jin Jang Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib Pharmaceutics olaparib self-microemulsifying drug delivery system microemulsion solubility dissolution oral absorption |
| title | Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib |
| title_full | Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib |
| title_fullStr | Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib |
| title_full_unstemmed | Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib |
| title_short | Development and Evaluation of Self-Microemulsifying Drug Delivery System for Improving Oral Absorption of Poorly Water-Soluble Olaparib |
| title_sort | development and evaluation of self microemulsifying drug delivery system for improving oral absorption of poorly water soluble olaparib |
| topic | olaparib self-microemulsifying drug delivery system microemulsion solubility dissolution oral absorption |
| url | https://www.mdpi.com/1999-4923/15/6/1669 |
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