| Autor: |
Kim YH; College of Pharmacy, Hanyang University, Ansan 15588, Republic of Korea., Kim SB; Bio-Living Engineering Major, Global Leaders College, Yonsei University, Seoul 03722, Republic of Korea., Choi SH; Department of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of Korea.; Department of Bio-Pharmaceutical Engineering, Kangwon National University, Chuncheon 24341, Republic of Korea., Nguyen TT; College of Pharmacy, Gachon University, Incheon 21936, Republic of Korea., Ahn SH; Department of Pharmacy, College of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of Korea., Moon KS; Department of Pharmacy, College of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of Korea., Cho KH; College of Pharmacy, Inje University, Gimhae 50834, Republic of Korea., Sim TY; Department of Artificial Intelligence, Sejong University, Seoul 05006, Republic of Korea., Heo EJ; Department of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of Korea.; Department of Bio-Pharmaceutical Engineering, Kangwon National University, Chuncheon 24341, Republic of Korea., Kim ST; Department of Nanoscience and Engineering, Inje University, Gimhae 50834, Republic of Korea.; Department of Pharmaceutical Engineering, Inje University, Gimhae 50834, Republic of Korea., Jung HS; Department of Biochemistry, Kangwon National University, Chuncheon 24341, Republic of Korea., Jee JP; College of Pharmacy, Chosun University, Gwangju 61452, Republic of Korea., Choi HG; College of Pharmacy, Hanyang University, Ansan 15588, Republic of Korea., Jang DJ; Department of Bio-Health Technology, College of Biomedical Science, Kangwon National University, Chuncheon 24341, Republic of Korea.; Department of Pharmacy, College of Pharmacy, Kangwon National University, Chuncheon 24341, Republic of Korea. |
| Abstrakt: |
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 ® MCM 10%, Labrasol ® 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. |
