可注射的双热可逆水凝,用于持续的肌内药物输送
Fakhar Ud Din1, Jung Suk Kim2, Ho Cheol Lee2
1College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea; Department of Pharmacy, Quaid-I-Azam University, Islamabad 45320, Pakistan.
一种新型的多塞塔塞尔装饰的固体脂质纳米粒子双热可逆系统 (DCT-DRTS) 提供了改进的肌肉内药物递送. 这种系统减少了突发释放,提供了持续的药物释放,并提高了抗瘤疗效,提高了生存率.
科学领域:
- 纳米技术纳米技术
- 药品制造 药品制造 药品制造
- 在瘤学瘤学.
背景情况:
- 多塞塔克塞尔是一种强效的化疗剂,在输送和潜在毒性方面存在限制.
- 固体脂质纳米颗粒 (SLN) 为药物输送提供了一个有前途的平台,但需要针对特定的输送路径进行优化配方.
- 双热可逆系统可以增强药物释放特征并改善治疗结果.
研究的目的:
- 开发和描述一种用于肌内注射的新型多塞塔克塞尔装饰固体脂质纳米粒子 (DCT-SLN) 载荷双热可逆系统 (DCT-DRTS).
- 评估DCT-DRTS的体外和体外性能,重点关注减少爆发效应,持续释放和改善抗瘤功效.
- 为了比较DCT-DRTS与传统的多塞素配方 (水凝和悬浮剂) 的疗效.
主要方法:
- 制备DCT-SLNs,并将其纳入双热可逆系统与poloxamer.
- 关于DCT-SLN的特征,包括粒子大小 (157 nm) 和捕获效率 (93%).
- 体释放药物研究和体瘤细胞异种移植模型中的抗瘤疗效评估,包括基因病理学和免疫基因化学分析.
主要成果:
- 在DCT-SLN中,点约为32°C,在双热可逆系统中,在生理温度下促进凝.
- 在DCT-DRTS中,药物释放持续并显著降低了初始血度,克服了DCT-水凝观察到的突发释放效应.
- 在接受DCT-DRTS治疗的小鼠中观察到增强的抗瘤疗效,改善的生存率,增加的亡和减少的增殖标志物.
结论:
- DCT-DRTS是一种适合肌肉内注射多塞素的配方,提供持续释放和改善生物可用性.
- 双热可逆系统有效地克服了多塞的突发释放,从而降低了毒性.
- DCT-DRTS显示出增强抗瘤效果和改善癌症治疗患者结果的显著潜力.
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