Formulation optimization, characterization, and evaluation of in vitro cytotoxic potential of curcumin loaded solid lipid nanoparticles for improved anticancer activity

Chem Phys Lipids. 2017 Nov:208:10-18. doi: 10.1016/j.chemphyslip.2017.08.009. Epub 2017 Aug 23.

Abstract

The aim of the present research was to develop a novel, biocompatible, amenable to industrial scale up and affordable solid lipid nanoparticles (SLN) preparation of curcumin and evaluate the therapeutic efficacy in vitro using cancer cells. We have incorporated cholesterol as the lipid to prepare SLN along with the Poloxamer-188 as stabilizer. High shear homogenization was used to prepare the SLN and formulation was optimized using Quality by Design The optimized Chol CUR SLN exhibited a narrow size distribution with a particle size of 166.4±3.5nm. Percentage encapsulation (%EE) was found to be 76.9±1.9%. The SLN were further characterized by DSC, FTIR, XRD and drug release. In vitro cell studies in MDA-MB-231 (Human Breast cancer) cell line revealed that the Chol CUR SLN showed superior cytotoxicity and uptake in comparison to the free curcumin. Furthermore, Chol CUR SLN induced a significantly higher apoptosis compared to free CUR treatment. These results indicated that the curcumin encapsulated in Chol SLN was able to significantly improve the cytotoxic potential and induction of apoptosis in MDA-MB-231 cells. The promising result from our study could lead a further exploration of this nanoparticle formulation to be utilized clinically for cancer treatment.

Keywords: Anti-cancer; Box-Behnken design; Cell uptake; Cholesterol; Curcumin; Solid lipid nanoparticles.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / metabolism
  • Antineoplastic Agents / pharmacology*
  • Apoptosis / drug effects
  • Biological Transport
  • Cell Line, Tumor
  • Curcumin / chemistry*
  • Curcumin / metabolism
  • Curcumin / pharmacology*
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Humans
  • Lipids / chemistry*
  • Nanoparticles*
  • Particle Size

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Lipids
  • Curcumin