PLGA基载药复合微球的制备及其释放性能

doi:10.3969/j.issn.1000-2006.2016.02.016

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南京林业大学学报（自然科学版） ›› 2016, Vol. 40 ›› Issue (02): 95-99.doi: 10.3969/j.issn.1000-2006.2016.02.016

PLGA基载药复合微球的制备及其释放性能

王芳,袁健,刘秀秀,方兵,杨思倩,高勤卫

南京林业大学化学工程学院,江苏南京 210037

出版日期:2016-04-18 发布日期:2016-04-18
基金资助:
收稿日期:2015-05-28 修回日期:2015-10-21
基金项目:国家自然科学基金项目(31200451); 大学生实践创新训练计划项目(2013); 江苏高校优势学科建设工程资助项目(PAPD)
第一作者:王芳(wangfang@njfu.edu.cn),副教授,博士。
引文格式:王芳,袁健,刘秀秀,等. PLGA基载药复合微球的制备及其释放性能[J]. 南京林业大学学报(自然科学版),2016,40(2):95-99.

Preparation and drug release properties of PLGA complex microparticles

WANG Fang, YUAN Jian, LIU Xiuxiu, FANG Bing, YANG Siqian, GAO Qinwei

College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China

Online:2016-04-18 Published:2016-04-18

摘要/Abstract

摘要： 以聚乳酸-羟基乙酸(PLGA)为载体材料,牛血清蛋白(BSA)为蛋白模型药物,采用复相乳化溶剂法制备PLGA载药微球,探索载药微球制备过程中囊芯比、初乳水油比、分散剂浓度、超声乳化时间对微球粒径大小、载药率、包封率的影响。结果表明,最优载药微球的制备条件为:囊芯比1:1,初乳水油比3:5,分散剂质量分数0.5%,超声乳化时间2 min。在此条件下,所得PLGA微球的粒径为268.7 nm,载药率30.88%,包封率46.95%; 电镜照片表明微球表面连续光滑,粒径分布较均匀。采用静电吸附法用阳离子聚电解质壳聚糖对最佳条件下的PLGA载药微球进行表面修饰,扫描电镜表明复合后微球粒径变大,能谱分析表明复合后微球中有N元素存在,即复合微球中存在壳聚糖,电荷测试表明微球表面带正电; 体外释放实验表明PLGA-CS复合载药微球的缓释时间延长,释药初期的突释性明显改善。

Abstract: Poly(lactic-co-glycolic acid)(PLGA)microparticles were prepared by an emulsion-solvent evaporation technique using bovine serum albumin(BSA)as model drug. When the ratio of shell to core was 1:1, ratio of water to oil 3:5, dispersant concentration 0.5%, and the ultrasonic emulsification time 2 min, PLGA microparticles were 268.7 nm in diameter, characterized by the laser light scattering technique, and the drug content and drug encapsulation efficiency in this case were 30.88% and 46.95%, respectively. Scanning electron microscopy(SEM)and transmission electron microscope(TEM)showed the products were spherical in shape and uniform in dimension. When the PLGA microparticles surface was modified with chitosan(CS)by adsorption technique, the microparticle became larger in diameter. The presence of N element and the positive zeta potential of modified microparticles revealed the presence of CS on the surface of the PLGA microparticles. In vitro drug release test showed that the burst release of modified microparticles eased and the release time was prolonged compared with unmodified PLGA microparticles.

中图分类号:

TQ463

王芳,袁健,刘秀秀,等. PLGA基载药复合微球的制备及其释放性能[J]. 南京林业大学学报（自然科学版）, 2016, 40(02): 95-99.

WANG Fang, YUAN Jian, LIU Xiuxiu, FANG Bing, YANG Siqian, GAO Qinwei. Preparation and drug release properties of PLGA complex microparticles[J].Journal of Nanjing Forestry University (Natural Science Edition), 2016, 40(02): 95-99.DOI: 10.3969/j.issn.1000-2006.2016.02.016.

参考文献

[1] 刘红, 马玉樊,高剑利,等. 高分子聚合物包裹胰岛素微球的制备及其体外质量评价[J]. 药物分析杂志, 2014, 34(7): 1321-1326. Liu H, Ma Y F, Gao J L, et al. Preparation of polymer coated insulin microspheres and the in vitro quality evaluation [J]. Chinese Journal of Pharmaceutical Analysis, 2014, 34(7): 1321-1326.
[2] 陈红丽, 王永学, 郭伟云,等. 提高PLGA微球载蛋白多肽类药物稳定性添加剂的研究进展[J]. 国际生物医学工程杂志, 2012, 35(3): 185-188. Chen H L, Wang Y X, Guo W Y, et al. Research progress of additives for improving therapeutic peptides and proteins stability in PLGA microspheres [J]. International Jorunal of Biomedical Engineering, 2012, 35(3): 185-188.
[3] 金启星, 成晓岚, 罗宇燕,等. 工艺因素对复乳法制备的载牛血清白蛋白PLGA微球形态与释放行为的影响[J]. 广东药学院学报, 2014, 30(5): 539-543. Jin Q X, Cheng X L, Luo Y Y, et al. Effect of process parameters on morphology and release of protein loaded PLGA microspheres made by W/O/W method [J]. Journal of Guangdong Pharmaceutical University, 2014, 30(5): 539-543.
[4] 封硕. 生物可降解高分子材料研究综述[J]. 中山大学研究生学刊(自然科学与医学版), 2012, 33(1):29-33. Feng S. Research and development of biodegradable polymer materials [J]. Journal of the Graduates Sun YAT-SEN University(Natural Sciences Medicine),2012, 33(1): 29-33.
[5] Chen Y C, Hsieh W Y. Effects of surface modification of PLGA-PEG-PLGA nanoparticles on loperamide delivery efficiency across the blood-brain barrier [J]. Journal of Biomaterials Applications, 2013, 27(7): 909-922.
[6] Nafee N, Taetz S, Schneider M, et al. Chitosan-coated PLGA nanoparticles for DNA/RNA delivery: effect of the formulation parameters on complexation and transfection of antisense oligonucleotides[J]. Nanotechnology, Biology and Medicine, 2007, 3(3): 173-183.
[7] 杨帆, 汪朝阳, 潘育方,等. 聚乳酸-乙醇酸的合成及在药物缓释微球中的应用[J]. 高分子材料科学与工程, 2005, 21(3): 77-80. Yang F, Wang C Y, Pan Y F, et al. Studies on the direct synthesis of poly(lactic acid-glycolic acid)and its application in drug delivery microspheres [J]. Polymer Materials Science and Engineering, 2005, 21(3): 77-80.
[8] 陆春燕, 龙伟, 温露,等. 载牛血清白蛋白PLGA微球的包封率测定及体外表征[J]. 海峡药学, 2014,26(9): 141-143. Lu C Y, Long W, Wen L, et al. Determination of encapsulation efficiency of PLGA microspheres loaded with bovine serum albumin and their in vitro characterization [J]. Strait Pharmaceutical Journal, 2014, 26(9): 141-143.
[9] Anand P. Design of curcumin-loaded PLGA nanoparticles formulation with enhanced cellular uptake, and increased bioactivity in vitro and superior bioavailability in vivo [J]. Biochemical Pharmacology, 2010, 79(3): 330-338.
[10] Wang Y, Li P, Kong L, et al. Chitosan-modified PLGA nanoparticles with versatile surface for improved drug delivery[J]. Aaps Pharmscitech, 2013, 14(2): 585-592.
[11] 李卫红, 司鹏, 雷文. 药用合成高分子缓、控释材料研究进展[J]. 高分子通报, 2015(1): 56-59. Li W H, Si P, Lei W, et al. Development of synthetic polymer materials used as sustained and controlled drug-release systems [J]. Polymer Bulletin, 2015(1): 56-59.
[12] Astete C E, Sabliov C M. Synthesis and characterization of PLGA nanoparticles [J]. Journal of Biomaterials Science Polymer Edition, 2006, 17(3): 247-289.
[13] 甘盛龙, 路振平, 杨哲,等. 壳交联pH响应型PLGA载药微球的制备与研究[J]. 高分子学报, 2015(2):228-235. Gan S L, Lu Z P, Yang Z, et al. Preparation and characterization of shell cross-linked PLGA nanoparticles with pH-responsiveness for drug delivery[J]. Acta Polymerica Sinica, 2015(2): 228-235.
[14] Yallapu M M, Gupta B K, Jaggi M, et al. Fabrication of curcumin encapsulated PLGA nanoparticles for improved therapeutic effects in metastatic cancer cells [J]. Journal of Colloid & Interface Science, 2010, 351(1): 19-29.
[15] 高勤卫,何刚,李明子,等. 氯化亚锡/萘二磺酸对D,L-乳酸聚合物微结构的影响 [J]. 南京林业大学学报(自然科学版),2009,33(3):111-115.Doi:10.3969/j.issn-1000-2006.2009.03.026. Gao Q W, He G, Li M Z, et al. The effects of SnCl₂ /naphthalene disulphonic acid on the microstructure of polymers prepared from D,L-lactic acid [J]. Journal of Nanjing Forestry University(Natural Sciences Edition), 2009,33(3):111-115.
[16] Mirakabad F, Akbarzadeh A, Zarghami N, et al. PLGA-based nanoparticles as cancer drug delivery systems [J]. Asian Pacific Journal of Cancer Prevention Apjcp, 2014, 15(2): 517-535.

PLGA基载药复合微球的制备及其释放性能

Preparation and drug release properties of PLGA complex microparticles

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