Development of Noninvasive Drug Delivery Systems to the Brain for the Treatment of Brain/Central Nervous System Diseases

  • Kanazawa Takanori
    Laboratory of Pharmaceutical Technology, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences

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Other Title
  • 非侵襲的な脳内への薬物送達技術の開発と脳神経疾患治療への応用
  • Review for award 非侵襲的な脳内への薬物送達技術の開発と脳神経疾患治療への応用
  • Review for award ヒシンシュウテキ ナ ノウナイ エ ノ ヤクブツ ソウタツ ギジュツ ノ カイハツ ト ノウ シンケイ シッカン チリョウ エ ノ オウヨウ
  • Development of non-invasive drug delivery system to the brain for brain diseases therapy

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Abstract

 In general, the blood-brain barrier (BBB) poses a major challenge to drug development efforts targeting brain/central nervous system (CNS) diseases, since it limits the distribution of systemically administered therapeutics to the brain/ CNS. Therefore, the development of effective strategies for enhancing drug delivery to the brain has been a topic of great interest in both the clinical and pharmaceutical fields. Intranasal administration has been noted as a method for noninvasive delivery of a drug to the brain/CNS by bypassing the BBB via the “nose-to-brain” route. This nose-to-brain delivery system has the potential to be highly versatile, and a combination of this system with new drugs and siRNA shows promise in the treatment of CNS diseases. Cell-penetrating Tat peptide-modified block copolymer micelles have the potential for improving mucosal permeability and nose-to-brain transport efficiency. In addition, nano-sized drug carriers can improve nose-to-brain delivery through their ability to increase the stability of encapsulated drugs against biological degradation in the nasal cavity and brain/CNS. In this review, we introduce the assessment of and mechanisms for delivery to the brain after intranasal drug/siRNA administration with our cell-penetrating peptide-modified nano-sized polymer micelles. Our findings show that the use of polymer micelles with surface modification by cell-penetrating peptides for intranasal administration enables the noninvasive delivery of therapeutic agents to the brain/CNS by increasing the nose-to-brain transfer of the drug or siRNA administered from the nasal cavity.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 138 (4), 443-450, 2018-04-01

    The Pharmaceutical Society of Japan

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