从鼻腔到大脑靶向输送治疗剂的气溶胶配方研究进展。

Shristy Verma, Pramod Kumar Sharma, Rishabha Malviya
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引用次数: 0

摘要

阻碍药物进入大脑的复杂解剖和生理屏障仍然是药物有效分布到脑组织的一个显著障碍。这些障碍阻碍了活性治疗药物进入大脑。本手稿旨在描述通过鼻腔途径向大脑靶向给药的各个方面。药物从鼻腔吸收到大脑的主要传输机制是细胞旁/细胞外机制,该机制可实现药物的快速传输。跨细胞/细胞内途径包括通过类脂通道传输药物,该通道可调节阴离子、有机阳离子和肽的进出。光谱和 PET(正电子发射断层扫描)是评估药物分布的两种常用方法。MRI(磁共振成像)是另一种用于评估从鼻腔到大脑的气溶胶给药效果的成像方法。它可以识别肺气肿、药物引起的伤害、粘液分泌、水肿和血管重塑。由于嗅上皮位于鼻腔内,药物很难到达所需靶点。像 "OptiNose "这样的双向气溶胶系统和工具可以帮助减少鼻外颗粒沉积,提高主要鼻腔通路的颗粒沉积效率。然而,从 N-T-B 直接给药可以减少给药剂量,更容易在活动部位达到有效浓度,而且有可能实现商业化。
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Advances in Aerosol Formulation for Targeted Delivery of Therapeutic Agents from Nose to Brain.

The intricate anatomical and physiological barriers that prohibit pharmaceuticals from entering the brain continue to provide a noteworthy hurdle to the efficient distribution of medications to brain tissues. These barriers prevent the movement of active therapeutic agents into the brain. The present manuscript aims to describe the various aspects of brain-targeted drug delivery through the nasal route. The primary transport mechanism for drug absorption from the nose to the brain is the paracellular/extracellular mechanism, which allows for rapid drug transfer. The transcellular/intracellular pathway involves the transfer across a lipoidal channel, which regulates the entry or exit of anions, organic cations, and peptides. Spectroscopy and PET (positron emission tomography) are two common methods used for assessing drug distribution. MRI (Magnetic resonance imaging) is another imaging method used to assess the efficacy of aerosol drug delivery from nose to brain. It can identify emphysema, drug-induced harm, mucus discharge, oedema, and vascular remodeling. The olfactory epithelium's position in the nasal cavity makes it difficult for drugs to reach the desired target. Bi-directional aerosol systems and tools like the "OptiNose" can help decrease extranasal particle deposition and increase particle deposition efficiency in the primary nasal pathway. Direct medicine administration from N-T-B, however, can reduce the dose administered and make it easier to attain an effective concentration at the site of activity, and it has the potential to be commercialized.

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