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

摘要

Graphical abstractDisplay OmittedHighlights?Curcumin loaded SLN using cholesterol (Chol CUR SLN) were prepared by High shear homogenization.?Box-Behnken Design was applied to study the effect of variables on formulation parameters.?DSC, XRD, FTIR and drug release studies were performed to characterize the formulated SLN.?Chol CUR SLN exhibited superior cell uptake and higher cytotoxicity in MDA-MB-231 cell line compared to free drug.?Greater percentage of apoptosis was induced by Chol CUR SLN as studied by Annexin V/PI binding assay.AbstractThe 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 efficacyin vitrousing 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 vitrocell 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.]]>