采用开环聚合法制备了聚己内酯-聚乙二醇-聚己内酯(PCL-PEG-PCL)共聚物,再采用水包油包水(W1/O/W2)复乳法制备载姜黄素PCL-PEG-PCL微球,研究载药微球释药行为。通过红外光谱(FT-IR)、热重分析仪、扫描电镜(SEM)等技术对其组成及结构进行表征。FT-IR结果表明PEG接枝上PCL;SEM结果表明微球形貌圆整;粒度分析表明粒径范围在6.3～10.3μm;热分析结果表明在30～60℃内微球存在相变过程;体外释药结果表明微球对药物具有缓释功能,释药机制以扩散为主,微球外部骨架溶蚀为辅。
PCL-PEG-PCL polymers were prepared by ring-opening polymerization.Curcumin-loaded PCL-PEG-PCL microspheres were prepared by W1/O/W2 double emulsion method.The drug release behavior of drug-loaded microspheres were studied.The composition of the copolymers were characterized by FT-IR,TGA,SME analysis technology.FT-IR results showed that the copolymers contained the segments of PCL and PEG.SEM confirmed that the structure of the microsphere were round.Particle size analysis showed that the particle size ranges from 6.3～10.3μm.The results of thermal analysis showed that it's a phase transition process at 30～60℃.In vitro release results shown that PCL-PEG-PCL microspheres had sustained-release effect on Cur.The mechanism of drug release was mainly diffusion,supplemented by the dissolution of the external skeleton of the microspheres.
[1] 陈建海,马安德,来永毅,等.可吸收性生物材料PCL在体外与动物体内降解机制的研究[J].生物医学工程学杂志,1997,16(4):334-337.
[2] 蒋青锋,陈建海,陈志良,等.控缓释制剂载体材料聚己内酯的制备及表征[J].华西药学杂志,2004(4):260-263.
[3] 郑施施,李星熠,王增寿.PCL-PEG-PCL载姜黄素纳米粒子的制备以及体外药物释放的考察[J].中国现代应用药学,2012,29(6):513-516.
[4] 张艳,龚飞荣,程树军.树枝化聚己内酯替莫唑胺微球的制备和表征[J].塑料,2012,41(6):56,75-77.
[5] 孙敏捷,张乐洋,其能.长春碱PCL-PEG-PCL纳米粒的制备及质量评价[J].中国医科大学学报,2010,41(1):29-34.
[6] 务圣洁.基于PCL-PEG-PCL三嵌段共聚物在药物递送和抗原佐剂系统的研究[D].北京:北京协和医学院,2018.
[7] 王涵.可降解高分子载姜黄素纳米微球的制备、表征及其释药特性研究[D].武汉:华中科技大学,2009.
[8] Maiti K,Mukherjee K,Gantait A,et al.Curcumin-phospholipid complex:preparation,therapeutic evaluation and pharmacokinetic study in rats[J].International Journal of Pharmaceutics,2007,330(1-2):155-163.
[9] Shaikh J,Ankola D D,Beniwal V,et al.Nanoparticle encapsulation improves oral bioavailability of curcumin by at least 9-fold when compared to curcumin administered with piperine as absorption enhancer[J].European Journal of Pharmaceutical Sciences,2009,37(3-4):23-30.
[10] Jeremy J J,Hasan M.Curcumin for chemoprevention of colon cancer[J].Cancer Letters,2007,255(2):170-181.
[11] 李红良,贾太轩.PCL-PEG-PCL聚合物的合成及性质[J].辽宁化工,2016,45(9):1151-1154.
[12] 蔡杰慧,杨英全,蒋芸芬,等.聚乙二醇相对分子质量及用量对温敏型PCL-PEG-PCL水凝胶的制备及释药性研究[J].分子科学学报,2020,36(1):75-82.
[13] 辛贺.PCL-PEG-PCL三嵌段共聚物的合成与性能研究[D].吉林:长春工业大学,2011.
[14] 杭太俊.药物分析[M].北京:人民卫生出版社,2016,114.
[15] 石淑先,陈晓农,夏宇,等.姜黄素/聚(ɑ-氰基丙烯酸异丁酯)载药微球的制备及其药物释放[J].生物医学工程学杂志,2018,35(5):749-753.
[16] 王海鸥,李攀,张良珂,等.载姜黄素的可生物降解微球的制备及其体外释药研究[J].中国中药杂志,2009,34(23):3021-3024.
[17] 王毅峰.载环孢素A海藻酸钙/壳聚糖缓释微球的研制[D].西安:西北大学,2011.
