通过液固体技术提升利科紧物的溶解
Narendra Kundavarapu1, Kannadasan Mahalingam1, Kiran Kumar Yada2
1Motherhood University Faculty of Pharmaceutical Sciences, Department of Pharmaceutics, Uttarakhand, India.
Turkish journal of pharmaceutical sciences
|September 8, 2025
概括
聚乳酸-协同甘油酸 (PLGA) 纳米泡 (NBs) 开发用于改善前列腺癌的博特佐米布 (BTZ) 输送. 这些增强的BTZ载荷的NB显示出更好的稳定性,生物可用性和持续释放性,为口服纳米医学铺平了道路.
科学领域:
- 纳米医学是一种纳米医学.
- 药物输送系统 药物输送系统
- 前列腺癌治疗方法 前列腺癌治疗方法
背景情况:
- 博特佐米布 (BTZ) 是一种用于前列腺癌的雄激素受体信号抑制剂.
- 由于溶解性差,第一通代谢和低生物可用性,BTZ的治疗潜力受到限制.
- 需要新的药物输送系统来提高BTZ的疗效和患者的治疗结果.
研究的目的:
- 开发和优化聚乳酸-协同甘油酸 (PLGA) 纳米泡 (NBs) 持续释放博尔特佐米布 (BTZ).
- 为了提高BTZ的稳定性和生物可用性,使用PLGA纳米泡配方.
- 评估BTZ装载PLGA NBs在改善口服药物递送和治疗疗效方面的潜力.
主要方法:
- 使用Box-Behnken设计优化配方,使用不同的药物,PLGA和聚乙烯醇度.
- 纳米气泡的粒子大小,多分散性指数,泽塔潜力和捕获效率的表征.
- 使用FTIR,DSC和XRD评估药物聚合物相互作用;通过SEM进行形态学;体外药物释放;稳定性研究;并在老鼠中进行药物动力学评估.
主要成果:
- 优化的BTZ装载PLGA NBs显示了有利的特征:大小为186.9±13.9nm,PDI为0.146±0.042,zeta电位为-21.4±2.28mV,捕获效率为66.12±1.48%.
- 分析证实没有药物聚合物相互作用和均的球形形态.
- 在体外研究表明,在一个月内,药物释放和稳定性优越. 药理动力学研究显示,Cmax和AUC显著增加,表明持续释放和吸收有所改善.
结论:
- 装有BTZ的PLGA纳米泡有效地提高了药物动力学和生物可用性,促进了向的输送和改善治疗结果.
- 开发的纳米泡配方显示出对BTZ持续释放口服药物输送的显著前景.
- 这项研究为未来的口服纳米药物开发提供了宝贵的见解,特别是用于增强药物吸收和药理动力学.
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