以两亲性聚合物聚乙二醇-聚(乳酸-乙醇酸)共聚物(mPEG-PLGA)为材料，采用复乳法结合溶剂挥发法制备mPEG-PLGA刺突微球，用其吸附蛋白多肽类药物.考察了膜材组份比、LA/GA摩尔比、内水相与油相体积比、油相与外水相体积比、固化条件等因素对微球的形貌结构及包埋率的影响. 结果表明，优化的制备条件为：膜材组份比1/19，LA/GA摩尔比50/50，W1/O体积比0.2/1，O/W2体积比1/10，固化搅拌速率500 rpm. 该条件下，微球刺突结构特征明显，包埋率较高，达到70%以上，且比表面积是普通光滑微球的14倍.
Furcella methoxy poly(ethylene glycol-L-lactic-co-glycolic acid) (mPEG-PLGA) microspheres were successfully prepared by double emulsion method with solvent evaporate method. The effects of polymer components,LA/GA molar ratio,volume ratio of internal water phase to oil phase,volume ratio of oil phase to external water phase and solidification rate on morphology and encapsulation of microspheres were investigated. The results showed that the microspheres with furcella morphology were prepared by the condition of 1/19 polymer components,50/50 LA/GA molar ratio,0.2/1 volume ratio of internal water phase to oil phase,1/10 volume ratio of oil phase to external water phase and 500 rpm solidification rate. In addition, its encapsulation efficiency is as high as 70%, specifica surface area of furcella microspheres is as fourteen times as the smooth microspheres.
[1] 田瑞，马光辉，苏志国. 快速膜乳化法制备粒径均一的 PLGA 微球和微囊 [J]. 过程工程学报, 2009, 9(4): 754-762.
Tian R, Ma G H,Su Z G. Preparation of Uniform Size PLGA Microparticles and Microcapsules by Premix Membrane Emulsification [J]. The Chinese Journal of Process Engineering, 2009, 9(4): 754-762.
[2] 钦富华，蔡雁，赵黛坚. 多孔利福平PLGA微球的制备工艺研究 [J]. 安徽医药, 2015, 19(7): 1241-1244.
Qin F H, Cai Y ,Zhao D J. Preparation of porous rifampicin-loaded PLGA microspheres [J]. Anhui Medical and Pharmaceutical Journal, 2015, 19(7): 1241-1244.
[3] Wang Y X, Jia Q, Wei Y, et al. Preparation?strategies?of?thermo-sensitive?P(NIPAM-co-AA)?microspheres?with?narrow?size?distribution,[J]. Powder?Technology, 2013,236(2):107-113.
[4] Niu X F, Feng Q L, Wang M B. In vitro Degradation and Release Behavior of Porous Poly(lactic acid) Scaffolds Containing Chitosan Microspheres as a Carrier for BMP-2-derived Synthetic Peptide [J]. Polym. Degrad. Stab., 2009, 94(2): 176-182..
[5] Dai C L, Wang Y J, Hou X. Preparation and Protein Adsorption of Porous Dextran Microspheres [J]. Carbohydr. Polym.., 2012, 87(3): 2338-2343.
[6] Patel B, Gupta V, Ahsan F. PEG?PLGA Based Large Porous Particles for Pulmonary Delivery of a Highly Soluble Drug, Low Molecular Weight Heparin [J]. J. Controlled Release, 2012, 162(2): 310-320.
[7] Zhang H, Ju X J, Xie R. A Microfluidic Approach Fabricate Monodisperse Hollow or Porous Poly(HEMA?MMA) Microspheres Using Single Emulsions as Templates [J]. J. Colloid Interface Sci., 2009, 336(1): 235-243.
[8] Du J J, Chen W, Zhang C. Hydrothermal Synthesis of Porous TiO2 Microspheres and Their Photocatalytic Degradation of Gaseous Benzene [J]. Chem. Eng. J., 2011, 170(1): 53-58.
[9] Sun L, Zhou S, Wang W J, et al. Preparation and Characterization of Porous Biodegradable Microspheres Used for Controlled Protein Delivery [J]. Colloids Surf. A: Physicochem. Eng. Aspect, 2009,345(13): 173-181.
[10] 陈庆华，张强. 药物微囊化新技术及应用[M]. 2008年1月第1版, 北京: 人民卫生出版社出版地, 2008. 16-18.
[11] Vortia E, Kay M, Wyllie R. The role of growth hormone and insulin-like growth factor-1 in Crohn's disease: implications for therapeutic use of human growth hormone in pediatric patients. Current Opinion in Pediatrics,2011, 23(5):545-551.
[12] 张景环，朱坚 . 蛋白质多肽类药物新型释药系统的研究 [J]. 临床药物治疗杂志 , 2010, 8(5):38-41.
[13] Luo Y C, Wang Q. Recent development of chitosan-based polyelectrolyte complexes with natural polysaccharides for drug delivery[J]. Int J Bio Macromol, 2014, 64 (3): 353-367.
[14] Soliman M S, Behzad T. PLGA micro and nanoparticles in delivery of peptides and proteins; problems and approaches[J]. Pharm Dev Tech, 2014, 2(3): 33-35.
[15] Butun S, Ince F G, Erdugan H, et al. One-step fabrication of biocompatible carboxymethyl cellulose polymeric particles for drug delivery systems[J]. Carbohydrate Polymers, 2011, 86(2): 636-643.
[16] Gombotz W R, Wee S F. Protein release from alginate matrices[J]. Adv Drug Deliv Rev, 2012, 64(12): 194-205.
[17] Wei W, Lv P P, Ma G H, et al. Codelivery of mTERT siRNA and paclitaxel by chitosan-based nanoparticles promoted synergistic tumor suppression[J]. Biomaterials, 2013, 34 (15): 3912-3923.
[18] Bhavesh B P, Subhashis C. Biodegradable polymer: An emerging excipient in pharmaceutical and medical device industry [J].J Excipient Food Chem, 2013, 4(4): 126-157.
[19] Tanja P I, Lidija P T, Anita G, et al. From optimization of synbiotic microparticles prepared by spray-drying to development of new functional carrotjuice[J].ChemIndChemEngQ,2014,20(4):549-564.
[20] Sansone F, Mencherini T, Picerno P, et al. Microencapsulation by spray drying of Lannea microcarpa extract: technological characteristics and antioxidant activity [J]. J Pharm pharmacol, 2014,2 (4):100-109.
