Tailoring Formulations for Intranasal Nose-to-Brain Delivery: A Review on Architecture, Physico-Chemical Characteristics and Mucociliary Clearance of the Nasal Olfactory Mucosa.
Tailoring Formulations for Intranasal Nose-to-Brain Delivery: A Review on Architecture, Physico-Chemical Characteristics and Mucociliary Clearance of the Nasal Olfactory Mucosa.
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DOI：
10.3390/pharmaceutics10030116
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发表时间：
2018-08-03
期刊：
影响因子：
5.4
通讯作者：
Schindowski K
中科院分区：
文献类型：
--
作者：
Gänger S;Schindowski K
血脑屏障和血脑脊液屏障是中枢神经系统（CNS）药物递送的主要障碍，因为它们阻止大多数分子进入大脑。像脑实质内或鞘内等替代给药途径是侵入性方法，仍有感染风险。相比之下，鼻 - 脑递送是一种微创给药途径，由于药物从鼻腔直接输送到大脑，从而绕过血脑屏障。特别是位于鼻腔顶部的颅底紧邻中枢神经系统。该区域覆盖着嗅黏膜。为了设计和定制适合鼻 - 脑药物递送的制剂，黏膜的结构、构造和物理化学特性是重要标准。因此，在此我们综述了关于鼻腔，特别是嗅黏膜特性的最新知识，这些知识是合理设计鼻内制剂和剂型所必需的。此外，这些信息也适用于全身性或局部鼻内药物递送以及鼻内疫苗接种的研发。
The blood-brain barrier and the blood-cerebrospinal fluid barrier are major obstacles in central nervous system (CNS) drug delivery, since they block most molecules from entering the brain. Alternative drug delivery routes like intraparenchymal or intrathecal are invasive methods with a remaining risk of infections. In contrast, nose-to-brain delivery is a minimally invasive drug administration pathway, which bypasses the blood-brain barrier as the drug is directed from the nasal cavity to the brain. In particular, the skull base located at the roof of the nasal cavity is in close vicinity to the CNS. This area is covered with olfactory mucosa. To design and tailor suitable formulations for nose-to-brain drug delivery, the architecture, structure and physico-chemical characteristics of the mucosa are important criteria. Hence, here we review the state-of-the-art knowledge about the characteristics of the nasal and, in particular, the olfactory mucosa needed for a rational design of intranasal formulations and dosage forms. Also, the information is suitable for the development of systemic or local intranasal drug delivery as well as for intranasal vaccinations.
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