Open AccessDevelopment and in vivo evaluation of self‐microemulsion as delivery system for α‐mangostin
Author(s) -
Xu WenKe,
Jiang Hui,
Yang Kui,
Wang YaQin,
Zhang Qian,
Zuo Jian
Publication year - 2017
Publication title -
the kaohsiung journal of medical sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.439
H-Index - 36
eISSN - 2410-8650
pISSN - 1607-551X
DOI - 10.1016/j.kjms.2016.12.003
Subject(s) - pharmacokinetics , bioavailability , medicine , microemulsion , drug delivery , pharmacology , in vivo , distribution (mathematics) , delivery system , chromatography , biomedical engineering , nanotechnology , materials science , chemical engineering , microbiology and biotechnology , pulmonary surfactant , mathematical analysis , chemistry , mathematics , engineering , biology
α‐Mangostin (MG) is a versatile bioactive compound isolated from mangosteen and possesses significant pharmacokinetic shortages. To augment the potential clinical efficacy, MG‐loaded self‐microemulsion (MG‐SME) was designed and prepared in this study, and its potential as a drug loading system was evaluated based on the pharmacokinetic performance and tissue distribution feature. The formula of MG‐SME was optimized by an orthogonal test under the guidance of ternary phase diagram, and the prepared MG‐SME was characterized by encapsulation efficiency, size distribution, and morphology. Optimized high performance liquid chromatography method was employed to determine concentrations of MG and characterize the pharmacokinetic and tissue distribution features of MG in rodents. It was found that diluted MG‐SME was characterized as spherical particles with a mean diameter of 24.6 nm and an encapsulation efficiency of 87.26%. The delivery system enhanced the area under the curve of MG by 4.75 times and increased the distribution in lymphatic organs. These findings suggested that SME as a nano‐sized delivery system efficiently promoted the digestive tract absorption of MG and modified its distribution in tissues. The targeting feature and high oral bioavailability of MG‐SME promised a good clinical efficacy, especially for immune diseases.