Strategies for drug delivery through the blood-brain barrier通过血脑屏障的药物递送策略.pptVIP

下载本文档

9
0
约5.65千字
约 37页
2017-09-04 发布于江西
举报
版权申诉

Strategies for drug delivery through the blood-brain barrier通过血脑屏障的药物递送策略.ppt

1、本文档共37页，可阅读全部内容。
2、原创力文档（book118）网站文档一经付费（服务费），不意味着购买了该文档的版权，仅供个人/单位学习、研究之用，不得用于商业用途，未经授权，严禁复制、发行、汇编、翻译或者网络传播等，侵权必究。
3、本站所有内容均由合作方或网友上传，本站不对文档的完整性、权威性及其观点立场正确性做任何保证或承诺！文档内容仅供研究参考，付费前请自行鉴别。如您付费，意味着您自己接受本站规则且自行承担风险，本站不退款、不进行额外附加服务；查看《如何避免下载的几个坑》。如果您已付费下载过本站文档，您可以点击这里二次下载。
4、如文档侵犯商业秘密、侵犯著作权、侵犯人身权等，请点击“版权申诉”（推荐），也可以打举报电话：400-050-0827(电话支持时间：9:00-18:30)。
5、该文档为VIP文档，如果想要下载，成为VIP会员后，下载免费。
6、成为VIP后，下载本文档将扣除1次下载权益。下载后，不支持退款、换文档。如有疑问请联系我们。
7、成为VIP后，您将拥有八大权益，权益包括：VIP文档下载权益、阅读免打扰、文档格式转换、高级专利检索、专属身份标志、高级客服、多端互通、版权登记。
8、VIP文档为合作方或网友上传，每下载1次，网站将根据用户上传文档的质量评分、类型等，对文档贡献者给予高额补贴、流量扶持。如果你也想贡献VIP文档。上传文档

Strategies for drug delivery through the blood-brain barrier通过血脑屏障的药物递送策略

Introduction to CNS pharmacology Anne McKinney Microanatomy Neurons Non-neuronal -Microglia -Microglial related macrophages -Cells of the cerebral vasculation -Meninges c) Blood brain barrier Blood brain barrier (BBB) Cortical microvasculature The BBB has several functions Protects the brain from “foreign substances” in the blood that my injure the brain Protects the brain from hormones and neurotransmitters in the rest of the body Maintains a constant environment for the brain General properties Large molecules do not pass through the BBB easily Low lipid (fat) soluble molecules do not penetrate into the brain. However lipid soluble molecules e.g. barbiturate drugs rapidly cross through the brain Molecules that have a high electrical charge are slowed Transport of substances into the brain are dependent on: Conc between compartments Size of molecule (MW) Flexibility and conformation of molecules Amino acid composition Lipophilicity Cellular enzymatic stability Cellular sequestration Affinity for efflux mechanisms Hydrogen bonding potentials (charge) Affinity for carrier mechanisms Effects of existing pathological conditions Penetration of drugs across BBB Factors determining the ability of a drug to cross the blood-brain barrier 1. Lipid solubility 2. Ionization 3. Plasma protein binding Molecular mass Transporter Diffusion of substances in the brain Paracellular (between cells) (not occur to great extent at the BBB due to tight junctions) - Transcellular (across cells) The higher the lipohilicity of a substance the greater the diffusion in the brain Transport at the BBB 4 basic mechanisms: Simple diffusion (low to high conc) Facilitated diffusion: a carrier mediated endocytosis( solute molecules bind to specific membrane protein carrier low to high conc Simple diffusion through an aqueous channel formed within membrane Active transport through a protein carrier: specific binding site that undergoes a change in affinity. Active transport requi