| 彭巧 宋宁 马巍 代佳音 毕良佳△.影响PLGA微球包封率和粒径相关因素研究进展[J].,2015,15(29):5790-5793 |
| 影响PLGA微球包封率和粒径相关因素研究进展 |
| Advanced Studies on Influence Factors on Encapsulation Efficiency andParticle Size of PLGA Microspheres |
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| DOI： |
| 中文关键词: PLGA 微球 包封率 粒径 |
| 英文关键词: PLGA Microspheres Encapsulation efficiency Particle size |
| 基金项目:高等学校博士学科点专项科研基金联合资助课题（20132307110018） |
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| 中文摘要: |
| 聚乳酸乙醇酸共聚物（PLGA）是一种可生物降解的高分子聚合物，具有良好的生物相容性，其降解产物为乳酸和乙醇酸，是
机体正常代谢的中间产物，最终可分解为二氧化碳和水，并分别经肺和肾脏排出体外，对人体不产生危害，所以PLGA在微球制
剂的制备中常作为首选载体。近年来PLGA微球制剂在医药领域有着飞跃发展，尤其是在抗肿瘤、免疫疫苗、蛋白给药、基因治
疗、诊断试剂和细胞支架等方面显现出很大优势。而且已有许多PLGA微球获得美国FDA批准上市，临床应用也有令人满意的
效果，未见报道有严重的不良反应。但现阶段国内生产的PLGA 缓释微球的质量还有很多不足之处如微球粒径偏大、包封率和载
药量偏低、突释过大等，有待进一步提高和改进。本文将综述在制备包裹水溶性药物的PLGA 微球过程中相关因素如药物本身理
化性质、制备方法、PLGA 结构特点、有机溶剂等对微球粒径、包封率的影响，以期为提高以PLGA为药物载体的药效奠定良好的
理论基础。 |
| 英文摘要: |
| Poly lactic-co-glycolic acid (PLGA) is a biodegradable polymer with good biocompatibility. Because the products of
its hydrolysis process are Lactic acid (LA) and Glycolic acid (GA), the middle products of normal metabolism, which are finally catabolized
into carbon dioxide and water that are respectively eliminated via lungs and kidneys and make no bad effects on human bodies, it is
often as the preferred carrier to be used to prepare microspheres.In recent years, microsphere has developed rapidly in pharmaceutical field
and it has turned out to be a potential formulation with great advantages inanticancer, vaccine, protein administration and gene therapy,
diagnostic reagents and cytoskeleton. At present, some PLGA microspheres have been approved by the FDA in US and have acquired
satisfactory results in clinical application without serious side effects being reported. However the quality of domestic PLGA microspheres
still exists many problems such as the bigger particle size, the lower encapsulation efficiency and drug loading and the larger
burst rate which have great scope to improve. This article will review the influence factors such as the physicochemical properties of the
drug itself, the preparation method, structure features of PLGA and organic solvents on particle size, encapsulation efficiency during the
procedure of PLGA microspheres encapsuled with hydrophilic drugs in order to make a good theory basis of improving pesticide effects
of medicine loaded by PLGA. |
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