不同的血脑屏障运输和细胞摄取循环的活体和体外
Erik Melander1, Camilla Eriksson2, Sara Wellens3
1Department of Pharmacy, Uppsala University, 75123 Uppsala, Sweden.
Pharmaceutics
|May 27, 2023
概括
SFTI-1有效地穿越血脑屏障 (BBB) 进行潜在的药物输送,而Katafa B1进入神经细胞. 这些循环细胞透 (cCPPs) 对中枢神经系统药物开发具有独特的运输特性.
科学领域:
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
背景情况:
- 血脑屏障 (BBB) 限制了治疗剂向中枢神经系统 (CNS) 的输送.
- 循环细胞透 (cCPPs) 是药物输送支架的有希望的候选者,因为它们能够跨越生物障碍.
- SFTI-1 和 kalata B1 是两种具有中枢神经系统药物开发潜力的cCPP.
研究的目的:
- 调查SFTI-1和卡塔拉B1在BBB的运输情况.
- 评估它们在大脑中的分布.
- 评估它们作为中枢神经系统药物输送的支架的潜力.
主要方法:
- 利用老鼠模型研究跨越BBB的类运输.
- 在BBB中量化了未绑定的SFTI-1和卡塔拉B1的分割.
- 评估了这些的细胞吸收到神经细胞中的情况.
主要成果:
- SFTI-1显示出显著的BBB传输,其Kp,uu,brain为13%.
- 卡拉塔B1显示BBB透率有限 (0.5%平衡).
- 卡拉塔B1很容易进入神经细胞,而SFTI-1则没有.
结论:
- SFTI-1是一种潜在的支架,可以将药物输送到中枢神经系统内的细胞外点.
- 卡拉塔B1可能适用于细胞内中枢神经系统的药物输送.
- 对于选择适合中枢神经系统药物开发的基架来说,BBB传输和细胞吸收的差异至关重要.
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