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Preparation of Polylactic Acid/Glycolic Acid Copolymer Nanoparticles and Its Effect in the Treatment of Diabetes

PLGA公司 乙醇酸 纳米颗粒 材料科学 粒径 聚乳酸 核化学 甘油三酯 可生物降解聚合物 控制释放 共聚物 溶剂 聚合物 化学工程 胆固醇 乳酸 化学 纳米技术 有机化学 生物化学 生物 细菌 工程类 复合材料 遗传学
作者
Wentian Liu,Yumei He,Wei Li,Jin Zhang,Feng Wu
出处
期刊:Science of Advanced Materials [American Scientific Publishers]
卷期号:13 (6): 1037-1047 被引量:3
标识
DOI:10.1166/sam.2021.4028
摘要

Insulin (INS) is easily degraded when administered orally and loading it into polylactic acid/glycolic acid (PLGA) polymer nanoparticles can enhance the efficacy of the drug. The W/O/W double emulsion solvent volatilization method was adopted to prepare INS-loaded PLGA nanoparticles. The preparation formula of nanoparticles was determined according to the type, concentration, and PLGA concentration of the emulsifier. Then, the morphology, particle size, and drug encapsulation efficiency of nanoparticles were characterized. Phosphate buffered solution (PBS) with pH = 7.4 was utilized as the release medium, and the prepared nanoparticles were analyzed for in vitro release performance. In addition, the rat diabetes model was constructed, and subcutaneous injection of nanoparticle in vitro release solution was performed to observe its hypoglycemic effect, which was used for the treatment of diabetic patients. Patients were rolled into experimental group and control group. The changes of the patients’ HbA1c, blood lipids (total cholesterol (TC), triglyceride (TG), high-density lipoprotein cholesterol (HDL-C), and low-density lipoprotein cholesterol (LDL-C)), C peptide, and aminopeptidase N (APN) were observed before and after treatment. Through the test, the appearance of the prepared nanoparticles was round, the average particle size was 416.7 nm, and the INS encapsulation efficiency was (36.82±2.26)%. After 36 h, the cumulative release of INS reached (60.58 ±1.45)%, and then the release rate gradually slowed down. The drug release tended to be balanced after 72 h, and the best hypoglycemic effect was achieved after subcutaneous administration 3 h ( P < 0.01). The blood glucose level of the rat diabetes model was greatly decreased after 3 h injection of 36.8 IU/kg PLGA polymer nanoparticles ( P < 0.05), and the blood glucose dropped to the lowest at 8 h ( P < 0.01), which was only (38.8 ± 3.72)% of the initial blood glucose. HbA1C of diabetic patients increased remarkably after treatment ( P < 0.05), TG, TC, and LDL-C in blood lipids decreased, and HDL-C increased, without statistically considerable differences ( P > 0.05). The serum APN level increased greatly ( P < 0.01). In short, the prepared PLGA polymer nanoparticles can effectively reduce blood glucose, help diabetic patients to relieve the toxicity of high glucose in the body, and improve the secretion function of INS.

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