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The therapeutic efficacy of conjugated linoleic acid – Paclitaxel on glioma in the rat

Paper ID Volume ID Publish Year Pages File Format Full-Text
8193 580 2010 10 PDF Available
Title
The therapeutic efficacy of conjugated linoleic acid – Paclitaxel on glioma in the rat
Abstract

Considering the effects of conjugated linoleic acid (CLA) on anti-tumor and anti-angiogenic in brain tumor, synergistic anti-tumor activity with taxane as well as potential activity for transporting chemotherapeutic agents across the blood–brain barrier (BBB), the purpose of this study was to synthesize CLA–paclitaxel (CLA–PTX) conjugate which could reach to the brain tissue and target brain tumor. The CLA was covalently linked to PTX. The conjugate was stable in PBS and rat plasma in vitro and had no microtubule assembly activity in solution and slight effect of arresting cell cycle progression at the G2-M phase. The in vitro cytotoxicity of conjugate was lower than that of PTX (p < 0.05). The conjugate showed higher cellular uptake efficiency on C6 glioma cells. The entire pharmacokinetic index revealed the significant enhancement of the conjugate pharmacokinetics compared with that in PTX (p < 0.01). The conjugate, unlike PTX, could distribute in brain tissue and retained higher concentrations throughout 360 h. The anti-tumor efficacy in brain tumor-bearing rats after administering conjugate was significantly higher than that after giving Taxol (p < 0.01). In conclusion, this CLA–PTX conjugate showed great potential to become a new prodrug of PTX and the methodology can be applied to other anticancer drugs.

Keywords
Conjugated linoleic acid (CLA); Paclitaxel (PTX); Conjugate; Blood–brain barrier; Brain glioma-bearing rats; Anti-tumor efficacy
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The therapeutic efficacy of conjugated linoleic acid – Paclitaxel on glioma in the rat
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Publisher
Database: Elsevier - ScienceDirect
Journal: Biomaterials - Volume 31, Issue 22, August 2010, Pages 5855–5864
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us