PREPARATION AND CHARACTERIZATION OF 5-FLUOROURACIL-LOADED MICROPARTICLES AS BIODEGRADABLE ANTICANCER DRUG CARRIERS
PREPARATION AND CHARACTERIZATION OF 5-FLUOROURACIL-LOADED MICROPARTICLES AS BIODEGRADABLE ANTICANCER DRUG CARRIERS
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DOI：
10.1111/j.2042-7158.1995.tb05760.x
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发表时间：
1995-02-01
影响因子：
3.3
通讯作者：
BENOIT, JP
中科院分区：
文献类型：
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作者：
BOISDRONCELLE, M;MENEI, P;BENOIT, JP
为了提供一种以可控的方式释放5-氟尿嘧啶并通过立体定向注射到脑内的装置，通过乳液萃取工艺制备了可生物降解的聚（（+/-）-丙交酯-共-乙交酯）（PLAGA）微粒。因此，5-氟尿嘧啶晶体的尺寸、有机相/水相比例、理论载药量和微粒尺寸起主要作用。通过选择合适的PLAGA和聚乙烯醇浓度以及初始乳液的搅拌速率，将微球尺寸调节至20-40 μ m.It表明，微粒结构直接取决于控制涂层材料沉淀速率的实验条件：表征了两种类型的微粒，I和II。颗粒的形态影响5-氟尿嘧啶的释放模式，其他工艺参数，如5-氟尿嘧啶晶体大小和PLAGA浓度也影响释放模式。
To provide a device releasing 5-fluorouracil in a controlled manner and injectable into the brain by stereotaxy, biodegradable poly ((+/-)-lactide-co-glycolide) (PLAGA) microparticles were prepared by an emulsion-extraction process.Although the solubility profile of the drug was not suitable for its encapsulation by the aforementioned method, careful choice of process variables allowed significant drug loading, reaching 30%. Thus, the size of the 5-fluorouracil crystals, the organic phase/aqueous phase ratio, the theoretical drug loading and the microparticle size played a predominant role. The microsphere size was adjusted to 20-40 mu m by selecting the appropriate PLAGA and polyvinylalcohol concentrations, and the stirring rate of the initial emulsion.It was shown that the microparticle structure depended directly on the experimental conditions governing the precipitation rate of the coating material: two types of microparticles, I and II, were characterized. The morphology of the particles influenced the 5-fluorouracil-release patterns, as did other process parameters, such as the 5-fluorouracil crystal size and the PLAGA concentration.It was possible to sustain the 5-fluorouracil release over 18 days.