Abstract：OBJECTIVE To prepare brefeldin A solid lipid nanoparticles (BFA-SLNs) and evaluate its antitumor effect in vitro. METHODS BFA-SLNs was prepared by ultrasonic dispersion method, and the formulation was optimized by orthogonal test. The average particle size, polydispersity index (PDI), Zeta potential, loading efficiency (LE), entrapment efficiency (EE) and release effect in vitro were determined. CCK-8 method was used to evaluate its inhibitory effect on the proliferation of HepG2 cells in vitro. RESULTS According to the results of laser nano particle size analyzer, the average diameter, PDI and Zeta potential were (185.38±4.74) nm, (0.233±0.03), (-66.10±2.26) mV, respectively. The LE% was (7.64±0.28)%. The EE% was more than 80%. It has a good sustained-release effect in vitro release test. BFA-SLNs can effectively inhibit the proliferation of HepG2 cells. CONCULUSION BFA-SLNs has high EE and sustained-release effect, and its anti-tumor effect is stronger than that of free drug in vitro.
司梦雅, 刘万云, 霍平. 布雷菲德菌素A固体脂质纳米粒的制备及其体外抗肿瘤效果的评价[J]. 中国药学杂志, 2021, 56(24): 1997-2001.
SI Meng-ya, LIU Wan-yun, HUO Ping. Preparation of Brefeldin A Solid Lipid Nanoparticles and Evaluation of Its Antitumor Effect in Vitro. Chinese Pharmaceutical Journal, 2021, 56(24): 1997-2001.
ZHENG R S, SUN K X, ZHANG S H, et al. Report of cancer epidemiology in China, 2015. Chin J Oncol(中华肿瘤杂志), 2019,41(1):19-28
[2]
DING X Y, WANG Z, SHI J, et al. Chinese expert consensus on multidisciplinary treatment of liver cancer. J Clin Hepatol(临床肝胆病杂志), 2021, 37(2):278-285.
[3]
MILLER K D, NOGUEIRA L, MARIOTTO A B, et al. Cancer treatment and survivorship statistics, 2019. Cancer J Clin, 2020, 30(3):179-194.
[4]
RISHI P, SHIVANI R P, RAMESHROO K, et al. Solid lipid nanoparticles:a review on recent perspectives and patents. Expert Opin Ther Pat, 2020, 30(3):179-194.
[5]
RAJPOOT K. Solid lipid nanoparticles:a promising nanomaterial in drug delivery. Curr Pharm Des, 2019, 25(37):3943-3959.
[6]
DEUKJOON K, JONGKOOK L, PHIL J S, et al. Asymmetric total synthesis of (+)-Brefeldin a from (S)-lactate by triple chirality transfer process and nitrile oxide cycloaddition. J Org Chem, 2002, 67(3):764-771.
[7]
WANG Y J, XUE F, WU Y F, et al. Development of macrolide lactone antibiotic brefeldin A fermentation process with eupenicillium brefeldianum ZJB082702. J Biosci Bioeng, 2012, 114(3):262-267.
[8]
BRNING A, ISHIKAWA T, KNEUSEL R E, et al. Brefeldin A binds to glutathione S-transferase and is secreted as glutathione and cysteine conjugates by Chinese hamster ovary cells. J Biol Chem, 1992, 267(11):7726-7732.
[9]
LIU W Y, FANG M J, XU P X, et al. An orthogonal experiment in the brefeldin A fermentation of pencillium. Microbiology(微生物学通报), 2005,32(6):52-57.
[10]
LI H Z. Study on preparation technology and quality standard of teniposide solid lipid nanoparticles. Changchun:Changchun University of Chinese Medicine, 2019.
[11]
ROMPICHARLA S V K, HIMANSHU B, AASHMA S, et al. Formulation optimization, characterization, and evaluation of in vitro cytotoxic potential of curcumin loaded solid lipid nanoparticles for improved anticancer activity. Chem Phys Lip, 2017, 208(1):10-18.
[12]
ZHAO Y W, LI J, TIAN S Y, et al. Preparation and physicochemical investigation of montmorillonite-betaxolol hydrochloride solid lipid nanoparticles. Northwest Pharm J(西北药学杂志), 2019, 34 (1):76-80.
[13]
LIANG Z, ZHANG Z, LI J G, et al. Optimization of formulation of econazole solid lipid nanoparticles based on pseudo-ternary phase diagrams and central composite design-response surface methodology. Chin Pharm J(中国药学杂志), 2020, 55(16):1358-1362.
[14]
LI X, YING X, YAN H L, et al. Preparation of hispidulin liposomes and its antitumor effect in vitro. Chin Pharm J(中国药学杂志), 2017, 52(18):1624-1628.
[15]
WANG F Y, LI W H. Preparation and anti-tumor activity of curcumol-loaded solid lipid nanoparticles. Chin Tradit Pat Med(中成药), 2020, 42(5):1114-1119.
[16]
HUANG H R, LIU T, GUO J X, et al. Brefeldin A enhances docetaxel-induced growth inhibition and apoptosis in prostate cancer cells in monolayer and 3D cultures. Bioorg Med Chem Lett, 2017, 27(11):2286-2291.
2021, Vol. 56 
