Enhanced dissolution and bioavailability of revaprazan using self-nanoemulsifying drug delivery system
- Authors
- Goo, Yoon Tae; Sa, Cheol-Ki; Kim, Min Song; Sin, Gi Hyeong; Kim, Chang Hyun; Kim, Hyeon Kyun; Kang, Myung Joo; Lee, Sangkil; Choi, Young Wook
- Issue Date
- Apr-2022
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Self-nanoemulsifying drug delivery system; revaprazan; oral bioavailability; lymphatic transport; cycloheximide
- Citation
- PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY, v.27, no.4, pp 414 - 424
- Pages
- 11
- Journal Title
- PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY
- Volume
- 27
- Number
- 4
- Start Page
- 414
- End Page
- 424
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/58060
- DOI
- 10.1080/10837450.2022.2070644
- ISSN
- 1083-7450
1097-9867
- Abstract
- A self-nanoemulsifying drug delivery system (SNEDDS) was developed to enhance the dissolution and oral bioavailability (BA) of revaprazan (RVP). Various SNEDDSs containing 200 mg of RVP were formulated using Capmul MCM, Tween 80, and Brij L4, and they were characterized according to their size, polydispersity index, and dissolution behavior. Dissolution rates of all SNEDDS formulations significantly (p < 0.05) improved with the formation of nanoemulsion with monodispersity. Formulation D resulted in RVP dissolution exceeding 70% at 2 h. Compared to raw RVP, SNEDDS exhibited a 4.8- to 7.4-fold improved effective permeability coefficient (P-eff) throughout the intestine in the in situ single pass intestinal permeability study and a 5.1-fold increased oral BA in the in vivo oral absorption assessment in rats. To evaluate the degree of lymphatic uptake, cycloheximide (CYC), a chylomicron flowing blocker, was pretreated prior to the experiment. This pretreatment barely affected the absorption of raw RVP; however, it greatly influenced the absorption of SNEDDS, resulting in an approximately 40% reduction in both the P-eff value and oral BA representing lymphatic transport. Thus, we suggest that the SNEDDS formulation is a good candidate for improving oral absorption of RVP through enhanced lymphatic uptake.
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