Changes in Cisplatin Delivery Due to Surface-Coated Poly (Lactic Acid)–Poly(∊-Caprolactone)Microspheres

聚乳酸 聚己内酯 乙二醇 材料科学 药物输送 微粒 聚乙烯醇 可生物降解聚合物 己内酯 乳酸 PEG比率 核化学 化学工程 聚合物 化学 纳米技术 有机化学 复合材料 共聚物 细菌 经济 工程类 生物 遗传学 财务
作者
Thomas Chandy,Robert F. Wilson,Gundu H. R. Rao,Gladwin S. Das
出处
期刊:Journal of Biomaterials Applications [SAGE]
卷期号:16 (4): 275-291 被引量:40
标识
DOI:10.1106/088532802024246
摘要

Smooth muscle cell proliferation plays a major role in the genesisof restenosis after angioplasty or vascular injury. Local delivery of agents capable of modulating vascular responses, have the potential to prevent restenosis. However, the development of injectable microspheres for sustained drug delivery to the arterial wall is a major challenge. We demonstrated the possibility of entrapping an antiproliferative agent, cisplatin, in a series of surface coated biodegradable microspheres composed of poly(lactic acid)– poly(caprolactone) blends, with a mean diameter of 2–10 mm. The microspheres were surface coated with poly ethylene glycol (PEG), chitosan (Chit), or alginate (Alg). A solution of cisplatin and a 50: 50 blend of polylactic acid (PLA)– polycaprolactone (PCL) dissolved in acetone–dichloromethane mixture was poured into an aqueous solution of PEG (or polyvinyl alcohol or Chit or Alg) with stirring using a high speedhomogenizer, for the formation of microspheres. Cisplatin recovery inmicrospheres ranged from 25–45% depending on the emulsification system used for the preparations. Scanning electron microscopy revealed that the PLA–PCL microspheres were spherical in shape and had a smooth surface texture. The amount of drug release was much higher initially (20–30%), this was followed by a constant slow-release profile for a 30-day period of study. It has been found that drugrelease depends on the amount of entrapped drug, on the presence of extra cisplatin in the dispensing phase, and on the polymer coatings.This PEG or Alg-coated PLA/PCL microsphere formulation may have potential for the targeted delivery of antiproliferative agents to treat restenosis.
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