title: Enhancing the oral bioavailability of biochanin A by encapsulation in mixed micelles containing Pluronic F127 and Plasdone S630.
abstract: Biochanin A (BCA), a natural dietary isoflavone, has been reported to show anticancer activities. However, its low biological availability and poor aqueous solubility limit its usefulness as a chemotherapeutic agent. We developed BCA-loaded micelles with Pluronic F127 and Plasdone S630 (BCA-FS). The optimized, spherical-shaped BCA-FS was obtained at a ratio of 1:1 (F127:S630). The particle size was 25.17±1.2 nm, and the zeta potential was -10.9±0.24 mV. BCA solubility in water increased to 5.0 mg/mL after encapsulation, and the drug-loading efficiency was 5.88%±0.76%. In vitro release experiments showed a delayed release of BCA from the mixed micelles. Furthermore, the BCA absorption permeability across a Caco-2 cell monolayer from the apical side to the basolateral side increased by 54% in BCA-FS. A pharmacokinetics evaluation showed a 2.16-fold increase in the relative oral bioavailability of BCA-FS compared with raw BCA, indicating that the mixed micelles may promote absorption in the gastrointestinal tract. A gastrointestinal safety assay was used to assess the reliability and safety of BCA-FS. On the basis of these findings, we conclude that this simple nanomicelle system could be leveraged to deliver BCA and other hydrophobic drugs.
authors.affiliation: Department of Pharmacy, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School.
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Wu
authors.affiliation: Department of Pharmacy, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School.
authors.forename: Weihong
authors.initials: W
authors.lastname: Ge
authors.affiliation: Department of Pharmacy, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School.
authors.forename: Tengfei
authors.initials: T
authors.lastname: Shao
authors.affiliation: Department of Pharmacy, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School.
authors.forename: Weijun
authors.initials: W
authors.lastname: Wu
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People's Republic of China.
authors.forename: Jian
authors.initials: J
authors.lastname: Hou
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People's Republic of China.
authors.forename: Li
authors.initials: L
authors.lastname: Cui
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People's Republic of China.
authors.forename: Jing
authors.initials: J
authors.lastname: Wang
authors.affiliation: Key Laboratory of New Drug Delivery System of Chinese Materia Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, People's Republic of China.
authors.forename: Zhenghai
authors.initials: Z
authors.lastname: Zhang
mesh_terms: D000085:Acetates / Q000737:chemistry*; D000284:Administration, Oral; D000818:Animals; D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000493:pharmacokinetics; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D018938:Caco-2 Cells / Q000187:drug effects; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods*; D019833:Genistein / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry*; D011205:Povidone / Q000031:analogs & derivatives* / Q000737:chemistry; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012995:Solubility
chemical_list: D000085:Acetates; D016588:Anticarcinogenic Agents; D000970:Antineoplastic Agents; D004337:Drug Carriers; D008823:Micelles; C525248:copolyvidonum Plasdone S-630; D020442:Poloxamer; D019833:Genistein; D011205:Povidone; C004541:biochanin A
keywords: Plasdone S630; Pluronic F127; biochanin A; mixed micelles; oral bioavailability