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研究了曲安缩松(Triamcinolone acetonide)的聚乳酸(PLA)毫微粒的制备方法和性质、不同浓度的聚合物对粒度分布、主药含量和释放的影响以及身体内的分有。以不同浓度的PLA(200、400和600 mg)制备样品,分别与曲安缩松20 mg 和[~3H]曲安缩松100μl 混合,加氯仿2 ml 溶解,与0.5%(W/W)明胶溶液10 ml用超声波乳化40 min,冰浴保持15℃以下,然后升温至40℃使氯仿缓慢蒸发,再用超声波处理45 min,离心(19,500×g)30 min,微粒用水洗三次后,混悬于水中,冷冻干燥2天待用。三种毫微粒的药物含量(%)分别为7.9±5.4、4.5±2.4和2.9±1.9W/W,包裹率(%)分别为64.5±10、71±6.4和75.4±1.5,平均粒径分别为500±397、476±410和710±406 nm。包裹率与聚合物的用量无关。选择药物与聚合物的适当比例,可以调节药物含量。聚合物的浓度高时,粒度分布范围广。由于PLA浓度增加,使内相的粘度增加,难于乳化,形成较大液滴。
The preparation methods and properties of polylactic acid (PLA) nanoparticles containing triamcinolone acetonide were studied. The effects of different concentrations of polymer on the particle size distribution, the content and release of the main drug, and in the body were studied. Samples were prepared with varying concentrations of PLA (200, 400 and 600 mg), mixed with triamcinolone acetonide 20 mg and [~ 3H] triamcinolone acetonide 100 μl, and then dissolved in 2 ml of chloroform and incubated with 0.5% (w / w) 10 ml of gelatin solution was emulsified with ultrasound for 40 min and kept below 15 ° C in an ice bath. The solution was then slowly warmed to 40 ° C. The solution was then gently sonicated for 45 min and centrifuged (19,500 × g) for 30 min. Suspended in water, freeze-dried for two days to be used. The drug content (%) of the three nanoparticles were 7.9 ± 5.4, 4.5 ± 2.4 and 2.9 ± 1.9 W / W respectively, and the encapsulation efficiency (%) was 64.5 ± 10, 71 ± 6.4 and 75.4 ± 1.5, 500 ± 397, 476 ± 410 and 710 ± 406 nm. The package rate is independent of the amount of polymer used. The appropriate ratio of drug to polymer can be chosen to adjust the drug content. When the polymer concentration is high, the particle size distribution is wide. As the PLA concentration increases, the viscosity of the internal phase increases, making it difficult to emulsify and form larger droplets.