Fabrication, Physicochemical Characterization and Evaluation of In vitro Anticancer Efficacy of a Novel pH Sensitive Polymeric Nanoparticles for Efficient Delivery of Hydrophobic Drug against Colon Cancer

Manikandan Mahalingam,Kannan Krishnamoorthy

doi:10.7324/japs.2015.501123

Abstract

Objective: The present investigation was aimed to overcome the limitations and to enhance the incorporation of the hydrophobic drug into polymeric nanoparticles and characterize the prepared nanoparticles and also to evaluate the in vitro anticancer efficacy of prepared nanoparticles. Method: Nanoprecipitation method was used to prepare plain and hydrophobic drug (Camptothecin) loaded polymeric nanoparticles. Prepared nanoformulations were evaluated for average particle size, particle size uniformity, surface area, zeta potential, surface morphology, drug content, encapsulation efficiency, drug loading, in vitro release, anticancer activity and stability studies at long term and accelerated storage conditions. Results: Plain and Camptothecin loaded polymeric nanoparticles were successfully prepared by nanoprecipitation method using stirring technique. Prepared Camptothecin encapsulated polymeric nanoparticles were (a) spherical in shape with size 20 mV; (b) showed > 95% release in colonic environment; (c) demonstrated enhanced anticancer activity than pure Camptothecin; and (d) extremely stable at both long term and accelerated storage conditions. Conclusion: In summary, the investigation concluded that the prepared Camptothecin encapsulated polymeric nanoformulations may be considered as an attractive and promising formulation which significantly overcome the limitations of Camptothecin and synergistically enhance its anticancer activity.

Highlights

Colon cancer is a multifactorial disease and has emerged as a major public hazard (Giftson et al, 2001)
Prepared plain and Camptothecin loaded polymeric nanoparticles were characterized for average particle size, particle size uniformity, surface area, as these parameters decides the performance such as solubility, dissolution, stability, circulation half-life, drug release, cellular uptake and bio-distribution (Manikandan and Kannan, 2015, Xie and Smith, 2010)
Prepared Camptothecin loaded polymeric nanoparticles were spherical in shape

Summary

Introduction

Colon cancer is a multifactorial disease and has emerged as a major public hazard (Giftson et al, 2001). It is the third most common malignancy and second most common cause of cancer with more than 1.4 million new cases and over half a million death worldwide each year (Terzic et al, 2010). Solubility of the active ingredient is a major pharmaceutical concern in developing a novel drug delivery system and is a key parameter when it comes to screening, drug designing, formulating and improving the modeling of oral bioavailability of the drug (Averineni et al, 2012, Prakash et al, 2008). Delivering the drug precisely and safely to its target site at the right period of time to have a controlled release and achieve the maximum therapeutic effect remains a yardstick in the design and development of novel drug delivery systems (Mishra et al, 2010)

Methods

Results

Conclusion