Preparation and In Vitro Evaluation of Apigenin Loaded Lipid Nanocapsules

被引:35
作者
Ding, Buyun [1 ]
Chen, Hao [2 ]
Wang, Chao [1 ]
Zhai, Yingjie [1 ]
Zhai, Guangxi [1 ]
机构
[1] Shandong Univ, Coll Pharm, Dept Pharmaceut, Jinan 250012, Peoples R China
[2] Shandong Univ, Qilu Hosp, Dept Pharm, Jinan 250012, Peoples R China
关键词
Apigenin; Lipid Nanocapsules; Simplex Lattice Experiment; Phase Inversion; MTT; NANOPARTICLES; DELIVERY; FORMULATION; FLAVONOIDS; MECHANISM; CELLS; MICROEMULSION; ENCAPSULATION; NANOCARRIERS; ABSORPTION;
D O I
10.1166/jnn.2013.7763
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In the present study, apigenin loaded lipid nanocapsules (AP-LNC) was prepared with phase inversion method and the formulation was optimized by simplex lattice design experiment with drug loading and encapsulation efficiency as the indexes. The drug loading and encapsulation efficiency of the optimal AP-LNC formulation were 1.26 +/- 0.05% and 95.86 +/- 0.38%, respectively. The drug concentration in the AP-LNC solution was 5.88 mg/mL. The shape of the AP-LNC was spherical with good dispersion. The average particle size and zeta potential of the AP-LNC were 46.1 nm and -28.18 mV, respectively. The in vitro release experiments showed that the release behavior of AP from LNC fitted the two phase dynamics process. The anti-proliferative activity of the AP-LNC was investigated using the MTT assay, and the results showed AP-LNC could significantly enhance the inhibition rate to HepG2 cell and MCF-7 cell. It could be concluded that LNC was a potential carrier for improving solubility and biological activity of AP.
引用
收藏
页码:6546 / 6552
页数:7
相关论文
共 46 条
[1]   In vitro drug release mechanism from lipid nanocapsules (LNC) [J].
Abdel-Mottaleb, Mona M. A. ;
Neumann, Dirk ;
Lamprecht, Alf .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2010, 390 (02) :208-213
[2]   Formulation and characterization of polyphenol-loaded lipid nanocapsules [J].
Barras, A. ;
Mezzetti, A. ;
Richard, A. ;
Lazzaroni, S. ;
Roux, S. ;
Melnyk, P. ;
Betbeder, D. ;
Monfilliette-Dupont, N. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 379 (02) :270-277
[3]   Anti-proliferative effect of apigenin and its apoptotic induction in human Hep G2 cells [J].
Chiang, Lien-Chai ;
Ng, Lean Teik ;
Lin, I. -Cheng ;
Kuo, Po-Lin ;
Lin, Chun-Ching .
CANCER LETTERS, 2006, 237 (02) :207-214
[4]   Mechanism of apoptosis induced by apigenin in HepG2 human hepatoma cells: Involvement of reactive oxygen species generated by NADPH oxidase [J].
Choi, Soo Im ;
Jeong, Choon Sik ;
Cho, So Yeon ;
Lee, Yong Soo .
ARCHIVES OF PHARMACAL RESEARCH, 2007, 30 (10) :1328-1335
[5]   Bioactivity-guided Isolation of Antiproliferative Compounds from Centaurea arenaria [J].
Csapi, Bence ;
Hajdu, Zsuzsanna ;
Zupko, Istvan ;
Berenyi, Agnes ;
Forgo, Peter ;
Szabo, Pal ;
Hohmann, Judit .
PHYTOTHERAPY RESEARCH, 2010, 24 (11) :1664-1669
[6]   In Vitro Antifungal Activity and Toxicity of Itraconazole in DMSA-PLGA Nanoparticles [J].
Cunha-Azevedo, Elaine P. ;
Silva, Jaqueline R. ;
Martins, Olimpia P. ;
Siqueira-Moura, Marigilson P. ;
Bocca, Anamelia L. ;
Felipe, Maria Sueli S. ;
Tedesco, Antonio C. ;
Azevedo, Ricardo B. .
JOURNAL OF NANOSCIENCE AND NANOTECHNOLOGY, 2011, 11 (03) :2308-2314
[7]   Comparison of Pharmacokinetic Profiles of PM02734 Loaded Lipid Nanoparticles and Cyclodextrins: In Vitro and In Vivo Characterization [J].
Estella-Hermoso de Mendoza, A. ;
Calvo, P. ;
Bishop, A. ;
Aviles, P. ;
Blanco-Prieto, M. J. .
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY, 2012, 8 (04) :703-708
[8]   Apigenin inhibits VEGF and HIF-1 expression via PI3K/AKT/p70S6K1 and HDM2/p53 pathways [J].
Fang, J ;
Xia, C ;
Cao, ZX ;
Zheng, JZ ;
Reed, E ;
Jiang, BH .
FASEB JOURNAL, 2005, 19 (03) :342-353
[9]  
Ferrari F, 1996, Pharm Dev Technol, V1, P159, DOI 10.3109/10837459609029890
[10]   High Entrapment Efficiency of Chitosan/Polylactic Acid/Tripolyphotspate Nanosized Microcapsules for Rapamycin by an Emulsion-Evaporation Approach [J].
Fu, Jing ;
Wang, Daxin ;
Wang, Ting ;
Yang, Wenjing ;
Deng, Yan ;
Wang, Hua ;
Jin, Shiguang ;
He, Nongyue .
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY, 2010, 6 (06) :725-728