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市場調查報告書 - 250521


Advances in Delivery to the Central Nervous System

出版商 Business Insights
出版日期 內容資訊 英文 64 Pages
中樞神經系統的給藥的演變 Advances in Delivery to the Central Nervous System
出版日期: 2012年08月31日 內容資訊: 英文 64 Pages





  • 中樞神經系統的給藥的改善手法的開發:主要因素


  • 介導BBB(血腦障壁)的給藥
  • 直接注射和移植
    • 總論
  • 化學修飾
    • 脂質化
    • 陽離子化
    • 前體藥物
    • CNS "鎖定do" 前體藥物
    • 載體介導前體藥物
    • 受體介導前體藥物
    • 總論
  • 滲透催化劑(permeability enhancer)
    • 排放輸送抑製劑
    • 總論
  • 奈米給藥技術
    • 微脂體
    • 相關案例研究:G-Technology (to-BBB Technologies BV)
    • bolaamphiphiles
    • 相關案例研究:V-Smart technology (Lauren Sciences)
    • 奈米粒子
  • 受體介導給藥技術
    • 相關案例研究:EPiC technology (Angiochem)
    • 其他受體介導給藥技術
  • 奈米&受體介導給藥技術的總論
  • 鼻腔內施打
    • 鼻腔內施打的機制
    • 生物醫藥的鼻腔內施打
    • 鼻腔內的處方
    • 鼻腔用設備
    • 相關案例研究:POD設備(Impel NeuroPharma)
    • 總論







CNS drugs are associated with longer development times and higher attrition rates than drugs for other therapy areas. Advances in delivery technologies are essential if the pursuit of novel treatments is to remain commercially viable.



The blood-brain barrier (BBB) and the blood cerebrospinal fluid barrier (BCSFB) exist to protect the brain, stringently regulating substances into and out of the brain. This report examines the ways in which these natural barriers may be overcome or circumvented to ensure that drugs can reach their intended target in the brain.


  • Identify the five main strategies for maximizing the delivery of drugs to the brain.
  • Understand the scientific basis of the most promising and recent technology advances.
  • Identify the companies that are at the cutting edge of each type of delivery technology.
  • Gain insight from quotes and opinions from leaders in the field of CNS drug delivery.
  • Assess which types of delivery technology are best suited to which types of drug and therapy area.


Increasingly, drug delivery specialists are harnessing endogenous BBB mechanisms such as receptormediated delivery pathways with nano-enabled platform technologies to improve the uptake and targeted delivery of substances into the brain.

Improvements in intranasal delivery devices and advances in formulation technologies have enabled researchers to deliver a wide range of substances in therapeutic doses into the olfactory regions. Medical device companies Kurve Technology, Impel NeuroPharma, and OptiNose have all developed devices that are compatible with intranasal delivery.

Chemical modification (e.g. lipidation and cationization) can be used to improve passive delivery across the blood-brain barrier but is rarely used in isolation. Permeability enhancers can be used to transiently disrupt the BBB to allow the passage of drugs into the CNS, but they have yet to be fully validated in the clinic.


  • Which delivery technologies can be considered for a drug that needs to achieve high CNS penetration?
  • What types of chemical modification have been applied and how successful have these been?
  • What role can nanotechnology play in drug delivery?
  • How well validated are the delivery technologies and which have data from human trials?
  • Are there in indications in which the problems of blood-brain barrier penetration can be justifiably circumvented by direct injection or implantation?

Table of Contents

About the author

  • Disclaimer


  • Strategies for drug delivery to the brain


  • Key factors in the development of improved methods of drug delivery to the central nevous system

Strategies for drug delivery to the brain

  • Delivery of drugs across the BBB
  • Direct injection and implantation
    • Conclusions on direct injection and implantation
  • Chemical modifications
    • Lipidation
    • Cationization
    • Prodrugs
    • CNS "locked" prodrugs
    • Carrier-mediated prodrugs
    • Receptor-mediated prodrugs
    • Conclusions on chemical modifications
  • Permeability enhancers
    • Efflux transporter inhibitors
    • Conclusions on permeability enhancers
  • Nano-enabled delivery technologies
    • Liposomes
    • Case study: G-Technology (to-BBB Technologies BV)
    • Bolaamphiphiles
    • Case study: V-Smart technology (Lauren Sciences)
    • Nanoparticles
  • Receptor-mediated delivery technologies
    • Case study: EPiC technology (Angiochem)
    • Other receptor-mediated delivery technologies
  • Conclusions on nano-enabled and receptor-mediated delivery technologies
  • Intranasal delivery
    • Mechanism of intranasal delivery
    • Intranasal delivery of biopharmaceuticals
    • Intranasal formulations
    • Intranasal devices
    • Case study: POD device (Impel NeuroPharma)
    • Intranasal conclusions
  • Overall conclusions


  • Scope
  • Methodology
    • Research methodology
    • Acknowledgements
  • Abbreviations
  • Bibliography/references


  • Table: Products approved for intrathecal delivery
  • Table: Inhibitors of blood-brain barrier efflux transporters
  • Table: Receptor-mediated targeting ligands


  • Figure: Enhancing lipophilicity may increase CNS delivery
  • Figure: Schematic of the prodrug approach for CNS delivery
  • Figure: Chemical structures of both exogenous and endogenous LAT substrates
  • Figure: Schematic of G-Technology
  • Figure: Schematic of nose-to-brain pathways for drugs
  • Figure: Intranasal delivery devices
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