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摘要
以聚乳酸-羟基乙酸共聚物(PLGA)、聚乙二醇(PEG)、异佛尔酮二异氰酸酯(IPDI)和2,2-二羟甲基丙酸(DMPA)为原料,采用预聚—扩链—中和—分散法制备PLGA改性聚氨酯水溶液,然后采用钙离子(Ca2+)的交联作用凝聚成PLGA改性聚氨酯微球。优化了合成条件,并对PLGA改性聚氨酯微球进行了傅里叶变换红外光谱(FT-IR)和扫描电子显微镜(SEM)表征,研究了PLGA含量和pH对微球降解性能的影响,以盐酸四环素(TH)为模型药物研究微球体外释药情况。结果表明,在降解反应初期微球的降解速率较大,而后趋于平稳,微球在碱性环境降解性能优于酸性环境,载药微球的载药量为0.83%,包封率为59.17%,载药PLGA改性聚氨酯微球的累积释药率可达74%。
Abstract
Polyurethane modified with PLGA aqueous solution was synthesized using poly lactic-co-glycolic acid(PLGA),polyethylene glycol(PEG),isophorone diisocyanate(IPDI) and dihydroxymethyl propionic acid (DMPA) as raw materials by prepolymerization-chain extension-neutralization-dispersion method.The polyurethane microspheres were coacervation by the crosslinking of Ca2+ ions.The synthesis conditions were optimized,and fourier transform infrared spectroscopy(FT-IR) and scanning electron microscope(SEM) were applied for further characterization.The effect of PLGA content and pH on the degradation performance of microspheres were studied.The drug release of microspheres using tetracycline hydrochloride (TH) as a model drug was studied.The results showed that the degradation rate of microspheres was higher at the initial stage of degradation reaction and then stabilized,and the degradation performance of microspheres in alkaline environment was better than acid environment.And the drug-loading rate of microspheres was 0.83%,the encapsulating rate of microspheres was 59.17%,and the accumulating drug release rate was 74%.
关键词
聚氨酯
/
聚乳酸-羟基乙酸共聚物
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盐酸四环素
/
改性
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降解
/
药物释放
Key words
polyurethane
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poly lactic-co-glycolic acid
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tetracycline hydrochloride
/
modification
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degradation
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drug release
PLGA改性聚氨酯微球的制备及性能研究[J].
化工新型材料, 2019, 47(6): 232-235 DOI:
[1] Fatima Zia,Khalid Mahmood Zia,Mohammad Zuber,et al.Glucomannan based polyurethanes:a critical short review of recent advances and future perspectives[J].International Journal of Biological Macromolecules,2016,87:229-236.
[2] Poussard L,Burel F,Couvercelle J P,et al.Hemocompatibilty of new ionic polyurethanes:influence of carboxylic group insertion modes[J].Biomaterials,2004,25:3473-3483.
[3] Yi Hou,Nan Jiang,Li Zhang,et al.Oppositely charged polyurethane microspheres with tunable zata potentials as an injectable dual-loaded system for bone repair[J].ACS Appl Mater Interfaces,2017,9,25808-25817.
[4] 张军瑞,高煜,蒋国军.功能聚氨酯的研究进展[J].化学通报,2017,80(11):1027-1035.
[5] Han Felicity Y,Thurecht Kristofer J,Whittaker Andrew K,et al.Bioerodable PLGA-based microparticles for producing sustained-release drug formulations and strategies for improving drug loading[J].Frontiers in Pharmacology,2016,7:185-195.
[6] Ramazani Farshad,Chen Weiluan,Van Nostrum Cornelis F,et al.Strategies for encapsulation of small hydrophilic and amphiphilic drugs in PLGA microspheres:state-of-the-art and challenges[J].International Journal of Pharmaceutics,2016,499:358-367.
[7] Fatemeh Sadat Tabatabaei Mirakabad,Kazem Nejati-Koshki,Abolfazl Akbarzadeh,et al.PLGA-based nanoparticles as cancer drug delivery systems[J].Asian Pac J Cancer Prev,2014,15(2):517-535.
[8] Anderson James M,Shive Matthew S.Biodegradation and biocompatibility of PLA and PLGA microspheres[J].Advanced Drug Delivery Reviews,2012,64:72-82.
[9] Makadia Hirenkumar K,Siegel Steven J.Poly lactic-co-glycolic acid(PLGA) as biodegradable controlled drug delivery carrier[J].Polymers,2011,3:1377-1397.
基金资助
国家自然科学基金资助项目(21401151)
