intranasal delivery of camptothecin-loaded tat-modified nanomicells for treatment of intracranial brain tumors鼻内交付camptothecin-loaded tat-modified nanomicells颅内脑肿瘤的治疗.pdfVIP
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intranasal delivery of camptothecin-loaded tat-modified nanomicells for treatment of intracranial brain tumors鼻内交付camptothecin-loaded tat-modified nanomicells颅内脑肿瘤的治疗
Pharmaceuticals 2012, 5, 1092-1102; doi:10.3390/ph5101092
OPEN ACCESS
pharmaceuticals
ISSN 1424-8247
/journal/pharmaceuticals
Article
Intranasal Delivery of Camptothecin-Loaded Tat-Modified
Nanomicells for Treatment of Intracranial Brain Tumors
Hiroyuki Taki †, Takanori Kanazawa †,*, Fuminari Akiyama, Yuuki Takashima and
Hiroaki Okada
School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji,
Tokyo 192-0392, Japan
† These authors contributed equally to this work.
* Author to whom correspondence should be addressed; E-Mail: kanazawa@toyaku.ac.jp;
Tel./Fax: +81-42-676-4493.
Received: 3 September 2012; in revised form: 27 September 2012 / Accepted: 9 October 2012 /
Published: 15 October 2012
Abstract: The blood-brain barrier is a substantial obstacle for delivering anticancer agents
to brain tumors, and new strategies for bypassing it are sorely needed for brain tumor
therapy. Intranasal delivery provides a practical, noninvasive method for delivering
therapeutic agents to the brain. Intranasal application of nano-sized micelles that have been
modified with Tat peptide facilitates brain delivery of fluorescent model materials. In this
study, we evaluated a nose-to-brain delivery system for brain tumor therapy. We nasally
administered the anti-tumor drug camptothecin (CPT) in solution and in methoxy
poly(ethylene glycol) (MPEG)/poly(-caprolactone) (PCL) amphiphilic block copolymers
(MPEG-PCL) and cell penetrating peptide, Tat analog-modified
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