title: Bioavailability enhancement of paclitaxel via a novel oral drug delivery system: paclitaxel-loaded glycyrrhizic acid micelles.
abstract: Paclitaxel (PTX, taxol), a classical antitumor drug against a wide range of tumors, shows poor oral bioavailability. In order to improve the oral bioavailability of PTX, glycyrrhizic acid (GA) was used as the carrier in this study. This was the first report on the preparation, characterization and the pharmacokinetic study in rats of PTX-loaded GA micelles The PTX-loaded micelles, prepared with ultrasonic dispersion method, displayed small particle sizes and spherical shapes. Differential scanning calorimeter (DSC) thermograms indicated that PTX was entrapped in the GA micelles and existed as an amorphous state. The encapsulation efficiency was about 90%, and the drug loading rate could reach up to 7.90%. PTX-loaded GA micelles displayed a delayed drug release compared to Taxol in the in vitro release experiment. In pharmacokinetic study via oral administration, the area under the plasma concentration-time curve (AUC0→24 h) of PTX-loaded GA micelles was about six times higher than that of Taxol (p < 0.05). The significant oral absorption enhancement of PTX from PTX-loaded GA micelles could be largely due to the increased absorption in jejunum and colon intestine. All these results suggested that GA would be a promising carrier for the oral delivery of PTX.
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. fhyang2011@126.com.
authors.forename: Fu-Heng
authors.initials: FH
authors.lastname: Yang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. zq1699@126.com.
authors.forename: Qing
authors.initials: Q
authors.lastname: Zhang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. qianyinglny@163.com.
authors.forename: Qian-Ying
authors.initials: QY
authors.lastname: Liang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. wsq2011@126.com.
authors.forename: Sheng-Qi
authors.initials: SQ
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. zhaobx@smu.edu.cn.
authors.forename: Bo-Xin
authors.initials: BX
authors.lastname: Zhao
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. alicemagic@126.com.
authors.forename: Ya-Tian
authors.initials: YT
authors.lastname: Wang
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. cayun2@126.com.
authors.forename: Yun
authors.initials: Y
authors.lastname: Cai
authors.affiliation: Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. liguofeng_2010@126.com.
authors.forename: Guo-Feng
authors.initials: GF
authors.lastname: Li
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D004337:Drug Carriers; D016503:Drug Delivery Systems; D065546:Drug Liberation; D019695:Glycyrrhizic Acid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D007413:Intestinal Mucosa / Q000378:metabolism; D007583:Jejunum / Q000378:metabolism; D008297:Male; D008823:Micelles; D017239:Paclitaxel / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
chemical_list: D000893:Anti-Inflammatory Agents; D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D008823:Micelles; D019695:Glycyrrhizic Acid; D017239:Paclitaxel