title: Development and in vivo evaluation of self-microemulsion as delivery system for α-mangostin.
abstract: 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.
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China.
authors.forename: Wen-Ke
authors.initials: WK
authors.lastname: Xu
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Jiang
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China.
authors.forename: Kui
authors.initials: K
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China.
authors.forename: Ya-Qin
authors.initials: YQ
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, Yijishan Hospital, Wannan Medical College, Wuhu, China; Anhui Provincial Engineering Technology Research Center of Polysaccharides Drug, Wuhu, China. Electronic address: zuojian8178@163.com.
authors.forename: Jian
authors.initials: J
authors.lastname: Zuo
mesh_terms: D000284:Administration, Oral; D000818:Animals; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D004655:Emulsions; D005163:Factor Analysis, Statistical; D005260:Female; D029762:Garcinia mangostana / Q000737:chemistry*; D065569:Gastrointestinal Absorption / Q000502:physiology*; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D009928:Organ Specificity; D010316:Particle Size; D010936:Plant Extracts / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014018:Tissue Distribution; D044004:Xanthones / Q000302:isolation & purification / Q000493:pharmacokinetics*
chemical_list: D004655:Emulsions; D010936:Plant Extracts; D044004:Xanthones; C021053:mangostin
keywords: Pharmacokinetics; Self-microemulsion; Tissue distribution; α-Mangostin