Improving Efficacy, Oral Bioavailability, and Delivery of Paclitaxel Using Protein-Grafted Solid Lipid Nanoparticles.

Abstract

Oral delivery of anticancer drugs remains challenging despite the most convenient route of drug administration. Hydrophobicity and nonspecific toxicities of anticancer agents are major impediments in the development of oral formulation. In this study, we developed wheat germ agglutinin (WGA)-conjugated, solid lipid nanoparticles to improve the oral delivery of the hydrophobic anticancer drug, paclitaxel (PTX). This study was focused to improve the PTX loading in biocompatible lipid matrix with high bioconjugation efficiency. WGA-conjugated, PTX-loaded solid lipid nanoparticles (LPSN) exhibited enhanced anticancer activity against A549 lung cancer cells after internalization through lectin receptors than free PTX. Biodistribution studies in rats revealed that LPSN significantly improved the oral bioavailability and lung targetability of PTX, which could be due to cumulative bioadhesive property of the nanocarrier system and the targeting ligand WGA.

• Authors: Deep Pooja, Hitesh Kulhari, Madhusudana Kuncha, Shyam S Rachamalla, David J Adams, Vipul Bansal, Ramakrishna Sistla
• Journal: Molecular pharmaceutics (Mol Pharm) Vol. 13 Issue 11 Pg. 3903-3912 (11 07 2016) ISSN: 1543-8392 [Electronic] United States
• PMID: 27696858 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Paclitaxel

Topics

• A549 Cells
• Animals
• Apoptosis (drug effects)
• Cell Proliferation (drug effects)
• Humans
• Lung Neoplasms (metabolism)
• Nanoparticles (chemistry)
• Nanostructures (chemistry)
• Paclitaxel (chemistry, pharmacology)
• Rats