title: A nanoparticulate drug-delivery system for glaucocalyxin A: formulation, characterization, increased in vitro, and vivo antitumor activity.
abstract: Glaucocalyxin A (GLA) is a phytochemical component with multiple pharmacological activities; however, glaucocalyxin A's wider use has been restricted by its poor solubility. In this study, GLA nanosuspensions were prepared with precipitation-combined ultrasonication and were characterized by dynamic light scattering (DLS), transmission electron microscope (TEM), and differential scanning calorimetry (DSC). The GLA nanosuspensions were spherical with a smooth surface and a small size of 143 nm, the drug payload achieved 8.95%, and the maximum GLA concentration reached 1 mg/mL. The lyophilized powders for the GLA nanosuspensions were amorphous and displayed a biphasic drug release pattern with an initial burst release and a consequent sustained release. In contrast to the free drug solution, GLA nanosuspensions showed higher in vitro antitumor activity against HepG2 cells (IC50value of 1.793 versus 2.884 μg/mL at 24 h, p < 0.01). Meanwhile, nanosuspensions displayed better anticancer efficacy than free GLA on H22 bearing mice (54.11% versus 36.02% tumor inhibition rate). These results indicate that GLA nanosuspensions have great potential for the treatment of hepatic cancer.
authors.affiliation: a Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing , PR China.
authors.forename: Meihua
authors.initials: M
authors.lastname: Han
authors.affiliation: b School of Pharmacy, Heilongjiang University of Chinese Medicine , Harbin , PR China , and.
authors.forename: Zhitao
authors.initials: Z
authors.lastname: Li
authors.affiliation: a Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing , PR China.
authors.forename: Yifei
authors.initials: Y
authors.lastname: Guo
authors.affiliation: c College of Pharmaceutical Sciences, Soochow University , Suzhou , PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhang
authors.affiliation: a Institute of Medicinal Plant Development, Chinese Academy of Medical Sciences & Peking Union Medical College , Beijing , PR China.
authors.forename: Xiangtao
authors.initials: X
authors.lastname: Wang
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D045786:Diterpenes, Kaurane / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D016503:Drug Delivery Systems; D051379:Mice; D053758:Nanoparticles / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy*; D012995:Solubility; D013535:Suspensions
chemical_list: D045786:Diterpenes, Kaurane; D013535:Suspensions; C055124:glaucocalyxin A
keywords: Characterization; Glaucocalyxin A nanosuspensions; in vitro antitumor efficacy; in vivo antitumor efficacy; preparation