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Improvement of Oral Bioavailability and Anti-Tumor Effect of Zingerone Self-Microemulsion Drug Delivery System
Authors:Xia Cao  Qin Zhu  Qi-Long Wang  Michael Adu-Frimpong  Chun-Mei Wei  Wen Weng  Rui Bao  Ya-Ping Wang  Jiang-Nan Yu  Xi Ming Xu
Institution:1. Department of Pharmaceutics, School of Pharmacy, Centre for Nano Drug/Gene Delivery and Tissue Engineering, Jiangsu University, Zhenjiang, People’s Republic of China;2. Department of Biochemistry and Biotechnology, Kwame Nkrumah University of Science and Technology, Kumasi, Ghana
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.
Keywords:Zingerone  Self-emulsifying  Pharmacokinetic  Oral drug delivery  Bioavailability apoptosis  SMEDDS"}  {"#name":"keyword"  "$":{"id":"kwrd0040"}  "$$":[{"#name":"text"  "_":"The Self-microemulsion Drug Delivery System  PTPDs"}  {"#name":"keyword"  "$":{"id":"kwrd0050"}  "$$":[{"#name":"text"  "_":"Pseudo-ternary phase diagrams  TEM"}  {"#name":"keyword"  "$":{"id":"kwrd0060"}  "$$":[{"#name":"text"  "_":"Transmission electron microscopy  PEG-400"}  {"#name":"keyword"  "$":{"id":"kwrd0070"}  "$$":[{"#name":"text"  "_":"Polyethylene glycol  HCl"}  {"#name":"keyword"  "$":{"id":"kwrd0080"}  "$$":[{"#name":"text"  "_":"Hydrochloric acid  DDW"}  {"#name":"keyword"  "$":{"id":"kwrd0090"}  "$$":[{"#name":"text"  "_":"Double-distilled water  PBS"}  {"#name":"keyword"  "$":{"id":"kwrd0100"}  "$$":[{"#name":"text"  "_":"Phosphate buffered solution  FBS"}  {"#name":"keyword"  "$":{"id":"kwrd0110"}  "$$":[{"#name":"text"  "_":"Fetal bovine serum  HPLC"}  {"#name":"keyword"  "$":{"id":"kwrd0120"}  "$$":[{"#name":"text"  "_":"High-performance liquid chromatography  RSD"}  {"#name":"keyword"  "$":{"id":"kwrd0130"}  "$$":[{"#name":"text"  "_":"The relative standard deviation  EE"}  {"#name":"keyword"  "$":{"id":"kwrd0140"}  "$$":[{"#name":"text"  "_":"Encapsulation efficiency  ATCC"}  {"#name":"keyword"  "$":{"id":"kwrd0150"}  "$$":[{"#name":"text"  "_":"American Type Culture Collection  MTT"}  {"#name":"keyword"  "$":{"id":"kwrd0160"}  "$$":[{"#name":"text"  "_":"The 3-(4  5-dimethyl-2-thiazolyl)-2  5-diphenyl-2-H-tetrazole bromide  Thiazolyl blue tetrazole bromide  DMSO"}  {"#name":"keyword"  "$":{"id":"kwrd0170"}  "$$":[{"#name":"text"  "_":"Dimethyl sulfoxide  PDI"}  {"#name":"keyword"  "$":{"id":"kwrd0180"}  "$$":[{"#name":"text"  "_":"Polydispersity index  ZP"}  {"#name":"keyword"  "$":{"id":"kwrd0190"}  "$$":[{"#name":"text"  "_":"Zeta potential  MRT"}  {"#name":"keyword"  "$":{"id":"kwrd0200"}  "$$":[{"#name":"text"  "_":"Mean Residence Time
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