开发和优化Soluplus®/Pluronic基聚合物微粒用于二甲胺的输送:表征,冷化,稳定性和细胞研究
Nihal Tugce Ozaksun1, Tugce Tayyar2, Aysun Ozdemir2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, 06330 Etiler, Ankara, Turkey.
概括
聚合物微粒有效地提供双胺 (BIC),显著增加其溶解度和增强抗癌活性. 这些稳定,生物相容的纳米载体显示出改善前列腺癌治疗的希望.
科学领域:
- 纳米技术 纳米技术
- 材料科学 材料科学 材料科学
- 制药科学 制药科学
背景情况:
- 聚合物微粒是先进的纳米载体,可提高药物的溶解性和有效性.
- 水溶性较差的药物在药物输送中提出了配方挑战.
- 比卡胺 (BIC) 是治疗前列腺癌的关键药物,具有有限的溶解性.
研究的目的:
- 开发和优化含有双胺的聚合物微粒.
- 评估这些纳米载体的物理化学特性,稳定性和体外性能.
- 评估前列腺癌细胞中双胺载小粒的细胞吸收和细胞毒性作用.
主要方法:
- 使用Soluplus®和Pluronic比率的中央复合设计 (CCD) 的配方优化.
- 通过TEM进行粒子大小,多分散度指数 (PDI),泽塔电位和形态的表征.
- 评估封装效率,体外药物释放,可溶性增强和体稳定性.
- 使用PC-3前列腺癌细胞进行体外细胞吸收和细胞毒性 (MTT测定) 研究.
主要成果:
- 优化的小粒显示颗粒大小<100 nm,PDI低 (≤0.066),封装效率高 (高达90.6%).
- 配方在72小时内持续释放药物,并显著增加BIC溶解率 (161-335倍).
- 微粒表现出优异的体和物理稳定性,有效的细胞吸收,以及对PC-3细胞的增强细胞毒性,与空白微粒的良好生物相容性.
结论:
- 开发的聚合物微粒是稳定的,生物相容的,有效的纳米载体对比卡胺.
- 这些系统显著提高了比卡胺的溶解性,并提高了其抗癌疗效.
- 优化的纳米载体系统具有改善前列腺癌治疗的潜力,需要进一步研究.
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