Pharmaceuticals 2012, 5(10), 1092-1102; doi:10.3390/ph5101092
Article

Intranasal Delivery of Camptothecin-Loaded Tat-Modified Nanomicells for Treatment of Intracranial Brain Tumors

Received: 3 September 2012; in revised form: 27 September 2012 / Accepted: 9 October 2012 / Published: 15 October 2012
(This article belongs to the Special Issue Cell-penetrating Peptides)
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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(e-caprolactone) (PCL) amphiphilic block copolymers (MPEG-PCL) and cell penetrating peptide, Tat analog-modified MPEG-PCL (MPEG-PCL-Tat) MPEG-PCL-Tat to rats bearing intracranial glioma tumors and quantified the cytotoxicity against glioma cells, and the therapeutic effects. CPT-loaded MPEG-PCL-Tat micelles showed higher cytotoxicity than CPT-loaded MPEG-PCL. CPT-free MPEG-PCL-Tat didn’t show any cytotoxicity, even at high concentrations (2 mmol/mL). CPT-loaded MPEG-PCL-Tat micelles significantly prolonged the median survival of rats. These results indicate that intranasal delivery of anti-cancer drugs with cell penetrating peptide-modified nanomicelles might be an effective therapy for brain tumors.
Keywords: intranasal brain delivery; glioma; anti-cancer drug; cell penetrating peptides; nanomicelles
PDF Full-text Download PDF Full-Text [321 KB, uploaded 15 October 2012 17:07 CEST]

Export to BibTeX |
EndNote


MDPI and ACS Style

Taki, H.; Kanazawa, T.; Akiyama, F.; Takashima, Y.; Okada, H. Intranasal Delivery of Camptothecin-Loaded Tat-Modified Nanomicells for Treatment of Intracranial Brain Tumors. Pharmaceuticals 2012, 5, 1092-1102.

AMA Style

Taki H, Kanazawa T, Akiyama F, Takashima Y, Okada H. Intranasal Delivery of Camptothecin-Loaded Tat-Modified Nanomicells for Treatment of Intracranial Brain Tumors. Pharmaceuticals. 2012; 5(10):1092-1102.

Chicago/Turabian Style

Taki, Hiroyuki; Kanazawa, Takanori; Akiyama, Fuminari; Takashima, Yuuki; Okada, Hiroaki. 2012. "Intranasal Delivery of Camptothecin-Loaded Tat-Modified Nanomicells for Treatment of Intracranial Brain Tumors." Pharmaceuticals 5, no. 10: 1092-1102.

Pharmaceuticals EISSN 1424-8247 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert