title: Characterization, pharmacokinetics and tissue distribution of chlorogenic acid-loaded self-microemulsifying drug delivery system.
abstract: The purpose of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) to improve the oral bioavailability of Chlorogenic acid (CA), an important bioactive compound from Lonicerae Japonicae Flos with poor permeability. SMEDDS was prepared and characterized by self-emulsifying rate, morphological observation, droplet size determination, stability, in vitro release, in vivo bioavailability and tissue distribution experiments. Results shown that the SMEDDS of CA has a high self-emulsifying rate (>98%) in the dissolution media, and its microemulsion exhibits small droplet size (16.37nm) and good stability. In vitro release test showed a complete release of CA from SMEDDS in 480min. After oral administration in mice, significantly enhanced bioavailability of CA was achieved through SMEDDS (249.4% relative to the CA suspension). Interestingly, SMEDDS significantly changed the tissue distribution of CA and showed a better targeting property to the kidney (2.79 of the relative intake efficiency). It is suggested that SMEDDS improves the oral bioavailability of CA may mainly through increasing its absorption and slowing the metabolism of absorbed CA via changing its distribution from the liver to the kidney. In conclusion, it is indicated that SMEDDS is a promising carrier for the oral delivery of CA.
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China. Electronic address: zmu_cl@126.com.
authors.forename: Li
authors.initials: L
authors.lastname: Chen
authors.affiliation: School of Traditional Chinese Medical Sciences, Southern Medical University, Guangzhou 510515, PR China; Guangdong Provincial Key Laboratory of Chinese Medicine Pharmaceutics, Southern Medical University, Guangzhou 510515, PR China. Electronic address: lcshun1225@163.com.
authors.forename: Chang-Shun
authors.initials: CS
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China.
authors.forename: Qing-Zhen
authors.initials: QZ
authors.lastname: Chen
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China.
authors.forename: Sen
authors.initials: S
authors.lastname: Wang
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China.
authors.forename: Yong-Ai
authors.initials: YA
authors.lastname: Xiong
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China.
authors.forename: Jing
authors.initials: J
authors.lastname: Jing
authors.affiliation: School of Pharmacy, Zunyi Medical University, Zunyi 563003, PR China.
authors.forename: Jia-Jia
authors.initials: JJ
authors.lastname: Lv
mesh_terms: D000818:Animals; D001682:Biological Availability; D002726:Chlorogenic Acid / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004355:Drug Stability; D004655:Emulsions; D005260:Female; D007668:Kidney / Q000378:metabolism; D008099:Liver / Q000378:metabolism; D008168:Lung / Q000378:metabolism; D008297:Male; D051379:Mice; D009206:Myocardium / Q000378:metabolism; D013154:Spleen / Q000378:metabolism; D014018:Tissue Distribution
chemical_list: D004655:Emulsions; D002726:Chlorogenic Acid
keywords: Characterization evaluation; Chlorogenic acid; Oral bioavailability; Self-microemulsifying drug delivery system; Tissue distribution