4.5 Article

Improved oral bioavailability of myricitrin by liquid self-microemulsifying drug delivery systems

Journal

JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
Volume 52, Issue -, Pages 597-606

Publisher

ELSEVIER
DOI: 10.1016/j.jddst.2019.05.003

Keywords

Myricitrin; SMEDDS; Pharmacokinetics; Oral bioavailability

Funding

  1. National Natural Science Foundation of China [81473172, 81503025, 81720108030, 81773695]
  2. Program for Scientific Research Innovation Team in Colleges and Universities of Jiangsu Province [SJK-2015-4]

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This study aimed to prepare a self-microemulsifying drug delivery system loaded with myricitrin (M-SMEDDS) to improve the low oral bioavailability of myricitrin. Prepared M-SMEDDS consisted of an oil phase (ethyl oleate), a surfactant (Cremophor EL35) and a co-surfactant (dimethyl carbinol). M-SMEDDS was characterized using the particle size, zeta potential and encapsulation efficiency, while the pharmacokinetics studies were also investigated. The prepared M-SMEDDS exhibited stable physicochemical properties with a small average droplet size (21.68 +/- 0.15 nm), negative zeta potential ( - 23.17 +/- 1.03 mV) and high encapsulation efficiency (92.73%). The in vitro release study showed that myricitrin was significantly released from M-SMEDDS compared with the free myricitrin. The relative oral bioavailability of M-SMEDDS was 2.47-fold higher than that of the free drug. These results indicated that the preparation, in vitro and in vivo studies of M-SMEDDS could obviously improve the solubility and oral bioavailability of myricitrin. This study therefore provides preliminary evidence for further clinical research and application of M-SMEDDS.

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