Enhanced oral bioavailability of Bisdemethoxycurcumin-loaded self-microemulsifying drug delivery system: Formulation design, in vitro and in vivo evaluation

[Display omitted] In this study, we sought to overcome the poor solubility and bioavailability of bismethoxycurcumin (BDMC) by fabricating a BDMC-loaded self micro-emulsifying system (BDMC-SMEDDS). Solubility and compatibility tests, pseudo-ternary phase diagrams (PTPDs) as well as d-optimal concept...

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Veröffentlicht in:International journal of pharmaceutics 2020-11, Vol.590, p.119887-119887, Article 119887
Hauptverfasser: Liu, Jian, Wang, Qilong, Omari-Siaw, Emmanuel, Adu-Frimpong, Michael, Liu, Jing, Xu, Ximing, Yu, Jiangnan
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Sprache:eng
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Zusammenfassung:[Display omitted] In this study, we sought to overcome the poor solubility and bioavailability of bismethoxycurcumin (BDMC) by fabricating a BDMC-loaded self micro-emulsifying system (BDMC-SMEDDS). Solubility and compatibility tests, pseudo-ternary phase diagrams (PTPDs) as well as d-optimal concept was applied to design the formulation. The assessment of the prepared BDMC-SMEDDS in-vitro mainly included droplet size (DS) and entrapment efficiency (EE) determination, morphology, drug release and stability testing. Besides, the in vivo behavior was also evaluated after oral administration of BDMC-SMEDDS to rats. The optimal formulation was found to compose of Kolliphor EL (K-EL, emulsifier, 645.3 mg), PEG 400 (co-emulsifier, 147.2 mg), ethyl oleate (EO, oil, 207.5 mg) and BDMC (50 mg). The BDMC-SMEDDS with satisfactory stability had a mean size of 21.25 ± 3.23 nm and EE of 98.31 ± 0.32%. Roughly 70% of BDMC was released from BDMC-SMEDDS within 84 h compared with
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2020.119887