Improvement of Oral Bioavailability and Anti-tumor Effect of Zingerone Self-microemulsion Drug Delivery System.


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Improvement of Oral Bioavailability and Anti-tumor Effect of Zingerone Self-microemulsion Drug Delivery System.

J Pharm Sci. 2021 Feb 18;:

Authors: Cao X, Zhu Q, Wang QL, Adu-Frimpong M, Wei CM, Weng W, Bao R, Wang YP, Yu JN, Xu XM

Abstract
This study sought to prepare a self-microemulsion drug delivery system containing zingerone (Z-SMEDDS) to improve the low oral bioavailability of zingerone and anti-tumor effect. Z-SMEDDS was characterized by particle size, zeta potential and encapsulation efficiency, while its pharmacokinetics and anti-tumor effects were also evaluated. Z-SMEDDS had stable physicochemical properties, including average particle size of 17.29 ± 0.07 nm, the zeta potential of -22.81 ± 0.29 mV, and the encapsulation efficiency of 97.96% ± 0.02%. In vitro release studies have shown the release of zingerone released by Z-SMEDDS was significantly higher than free zingerone in different release media. The relative oral bioavailability of Z-SMEDDS was 7.63 times compared with free drug. Meanwhile, the half inhibitory concentration (IC50)of Z-SMEDDS and free zingerone was 8.45 μg/mL and 13.30 μg/mL, respectively on HepG2. This study may provide a preliminary basis for further clinical research and application of Z-SMEDDS.

PMID: 33610568 [PubMed – as supplied by publisher]

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