Poly (ethylene)-glycol conjugated solid lipid nanoparticles of noscapine improve biological half-life, brain delivery and efficacy in glioblastoma cells.

Abstract

Noscapine crosses blood-brain-barrier and inhibits proliferation of glioblastoma cells. However, short plasma half-life and rapid elimination necessitate the administration of multiple injections for successive chemotherapy. Noscapine bearing solid lipid nanoparticles, Nos-SLN and poly (ethylene)-glycol conjugated solid lipid nanoparticles of noscapine, Nos-PEG-SLN of 61.3 ± 9.3-nm and 80.5 ± 8.9-nm containing 80.4 ± 3.2% and 83.6 ± 1.2% of Nos, were constructed. First order kinetic and Higuchi equation were followed to release the Nos at intracellular pH~4.5. Further, a decrease in IC₅₀ (Nos; 40.5 μM>Nos-SLN; 27.2 μM>20.8 μM) and enhanced subG1 population were observed in U87cells. Plasma half-life was enhanced up to ~11-fold and ~5-fold by Nos-PEG-SLN and Nos-SLN which significantly (P<0.05) deposits 400.7 μg/g and 313.1 μg/g of Nos in comparison to 233.2 μg/g by drug solution. This is first report demonstrating a workable approach to regulate the administration of multiple injections of Nos, warranting further in vivo tumor regression study for superior management of brain cancer.

FROM THE CLINICAL EDITOR:

This report describes a possible approach to regulate the administration of multiple injections of Noscapine using solid lipid nanoparticles. The data warrant further in vivo tumor regression studies for optimal management of glioblastoma, a generally very poorly treatable brain cancer.

• Authors: Jitender Madan, Ravi Shankar Pandey, Vikas Jain, Om Prakash Katare, Ramesh Chandra, Anju Katyal
• Journal: Nanomedicine : nanotechnology, biology, and medicine (Nanomedicine) Vol. 9 Issue 4 Pg. 492-503 (May 2013) ISSN: 1549-9642 [Electronic] United States
• PMID: 23117045 (Publication Type: Journal Article)
• Copyright: Copyright © 2013 Elsevier Inc. All rights reserved.

Chemical References

• Lipids
• Polyethylene Glycols
• Noscapine

Topics

• Brain (metabolism)
• Brain Neoplasms (pathology)
• Cell Line, Tumor
• Glioblastoma (pathology)
• Half-Life
• Humans
• Hydrogen-Ion Concentration
• Lipids
• Nanoparticles
• Noscapine (administration & dosage, chemistry, pharmacokinetics)
• Polyethylene Glycols (chemistry)
• Powder Diffraction