Preparation, In Vivo and In Vitro Release of Polyethylene Glycol Monomethyl Ether-Polymandelic Acid Microspheres Loaded Panax Notoginseng Saponins

被引:8
|
作者
He, Yi [1 ]
Li, Hongli [1 ]
Zheng, Xiangyu [1 ]
Yuan, Mingwei [1 ]
Yang, Renyu [1 ]
Yuan, Minglong [1 ]
Yang, Cui [1 ]
机构
[1] Yunnan Minzu Univ, Natl & Local Joint Engn Res Ctr Green Preparat Te, Kunming 650500, Yunnan, Peoples R China
基金
中国国家自然科学基金;
关键词
Panax notoginseng saponins; microspheres; sustained-release; biocompatibility; anti-inflammatory; anti-cancer; RESPONSIVE POLYMERIC MICELLES; MPEG-PLA NANOPARTICLES; MULTIDRUG-RESISTANCE; COPOLYMER MICELLES; DRUG-DELIVERY; PHARMACOKINETICS; ATHEROSCLEROSIS; ANTITUMOR; EFFICACY; BRAIN;
D O I
10.3390/molecules24102024
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In order to enrich the types of Panax notoginseng saponins (PNS) sustained-release preparations and provide a new research idea for the research and development of traditional Chinese medicine sustained-release formulations, a series of Panax notoginseng saponins microspheres was prepared by a double emulsion method using a series of degradable amphiphilic macromolecule materials polyethylene glycol monomethyl ether-polymandelic acid (mPEG-PMA) as carrier. The structure and molecular weight of the series of mPEG-PMA were determined by nuclear magnetic resonance spectroscopy ((1) HNMR) and gel chromatography (GPC). The results of the appearance, particle size, drug loading and encapsulation efficiency of the drug-loaded microspheres show that the mPEG10000-PMA (1:9) material is more suitable as a carrier for loading the total saponins of Panax notoginseng. The particle size was 2.51 +/- 0.21 m, the drug loading and encapsulation efficiency were 8.54 +/- 0.16% and 47.25 +/- 1.64%, respectively. The drug-loaded microspheres were used for in vitro release and degradation experiments to investigate the degradation and sustained release behaviour of the drug-loaded microspheres. The biocompatibility of the microspheres was studied by haemolytic, anticoagulant and cytotoxicity experiments. The pharmacological activity of the microspheres was studied by anti-inflammatory and anti-tumour experiments. The results showed that the drug-loaded microspheres could be released stably for about 12 days and degraded within 60 days. At the same time, the microspheres had good biocompatibility, anti-inflammatory and anti-tumour activities.
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页数:16
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