PLGA(75:25)(poly(lactic-co-glycolic acid))是一种低毒、生物相容、可生物降解的可控给药载体，可在生物体内实现缓释。
PLGA(poly (lactic-co-glycolic acid)) is made by random polymerization of two monomers: lactic acid and glycolic acid. It is a degradable functional polymer organic compound with good biocompatibility, non-toxic, and good cystforming and film forming properties. It is widely used in pharmaceutical, medical engineering materials and modern industrial fields[1,2].
PLGA@Icaritin nanoparticles (NPs) dramatically suppressed cell growth, induced Lactic dehydrogenase (LDH) leakage, arrested more GC cells at G2 phase, and inhibited the invasion and metastasis of GC cells, compared to free icaritin. In addition, PLGA@Icaritin could help generate dozens of reactive oxygen species (ROS) within GC cells, following by significant mitochondrial membrane potentials (MMPs) loss and excessive production of oxidative-mitochondrial DNA (Ox-mitoDNA)[3].
PLGA. 聚乳酸-羟基乙酸共聚物 (poly (lactic-co-glycolic acid),PLGA)由两种单体——乳酸和羟基乙酸随机聚合而成,是一种可降解的功能高分子有机化合物,具有良好的生物相容性、无毒、良好的成囊和成膜的性能,被广泛应用于制药、医用工程材料和现代化工业领域[1,2]
PLGA@Icaritin NPs与游离Icaritin相比,可以显著抑制细胞生长,诱导乳酸脱氢酶(LDH)渗漏,在G2期阻滞更多的GC细胞,抑制GC细胞的侵袭和转移。此外,PLGA@Icaritin可以帮助在GC细胞内产生数十种活性氧(ROS),造成显著的线粒体膜电位(MMPs)损失和氧化线粒体DNA (Ox-mitoDNA)的过度产生[3]。
参考文献:
[1]. Gentile P, Chiono V, et,al. An overview of poly(lactic-co-glycolic) acid (PLGA)-based biomaterials for bone tissue engineering. Int J Mol Sci. 2014 Feb 28;15(3):3640-59. doi: 10.3390/ijms15033640. PMID: 24590126; PMCID: PMC3975359.
[2]. Sadat Tabatabaei Mirakabad F, Nejati-Koshki K, et,al.PLGA-based nanoparticles as cancer drug delivery systems. Asian Pac J Cancer Prev. 2014;15(2):517-35. doi: 10.7314/apjcp.2014.15.2.517. PMID: 24568455.
[3]. Xiao Y, Yao W, et,al.Icaritin-loaded PLGA nanoparticles activate immunogenic cell death and facilitate tumor recruitment in mice with gastric cancer. Drug Deliv. 2022 Dec;29(1):1712-1725. doi: 10.1080/10717544.2022.2079769. PMID: 35635307; PMCID: PMC9176696.
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Protocol 1 (Synthesis of PLGA@ Icaritin )[1]： |
| 1.PLGA-PEG copolymers (PEG2000) were prepared by melt polymerization under vacuum using stannous octoate [stannous 2-ethylhexanoate] as a catalyst.? PLGA and PEG2000 (0.77 g) (45%/w) were heated to 140℃ in a bottleneck flask under a nitrogen atmosphere for complete melting. (The molar ratio of DL-lactide to glycolide was 3:1 in PLGA) 2.Stannous octoate [0.05% (w/w)] was added, and the temperature of the reaction mixture was increased to 180℃. This temperature was maintained for 4 h. Polymerization was performed under vacuum. 3.The copolymer was recovered by dissolution in methylene chloride, followed by precipitation in ice-cold diethyl ether. After 24 h, PLGA-PEG was purified by washing with ethanol and drying under vacuum. 4.Icaritin (0.5 mg) was dissolved in 500 μL dimethyl sulfoxide and mixed with 5 mg of PLGA-PEG in the drug solution. 5.The drug-polymer mixture was added dropwise to 10 mL of deionized water while stirring and stirred for 24 h at room temperature in a beaker. 6.PLGA@Icaritin was obtained, dialyzed to remove the organic solvent, and freeze-dried.
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参考文献: [1]. Xiao Y, Yao W, et,al. Icaritin-loaded PLGA nanoparticles activate immunogenic cell death and facilitate tumor recruitment in mice with gastric cancer. Drug Deliv. 2022 Dec;29(1):1712-1725. doi: 10.1080/10717544.2022.2079769. PMID: 35635307; PMCID: PMC9176696.? |
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