Potential anticancer activity of protocatechuic acid loaded in montmorillonite/Fe 3 O 4 nanocomposites stabilized by seaweed Kappaphycus alvarezii

• Published in: International journal of pharmaceutics Vol. 572; p. 118743
• Main Authors: Yew, Yen Pin, Shameli, Kamyar, Mohamad, Shaza Eva Bt, Nagao, Yuki, Teow, Sin-Yeang, Lee, Kar Xin, Mohamed Isa, Eleen Dayana
• Format: Journal Article
• Language: English
• Published: Netherlands 15.12.2019
• Subjects: Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Bentonite - chemistry; Cell Line; Cell Line, Tumor; Drug Carriers - chemistry; Drug Delivery Systems - methods; Drug Liberation; Ferrous Compounds - chemistry; HCT116 Cells; Humans; Hydroxybenzoates - chemistry; Hydroxybenzoates - pharmacology; Nanocomposites - chemistry; Particle Size; Rhodophyta - chemistry; Seaweed - chemistry; Transmission electron microscopy; FeO nanocomposites; Anticancer assay; Sustained drug release; Drug delivery; Protocatechuic acid
• ISSN: 1873-3476
• DOI: 10.1016/j.ijpharm.2019.118743

Superparamagnetic magnetite nanocomposites (Fe O -NCs) were successfully synthesized, which comprised of montmorillonite (MMT) as matrix support, Kappaphycus alvarezii (SW) as bio-stabilizer and Fe O as filler in the composites to form MMT/SW/Fe O -NCs. Nanocomposite with 0.5 g Fe O (MMT/SW/0.5Fe O ) was selected for anticancer activity study because it revealed high crystallinity, particle size of 7.2 ± 1.7 nm with majority of spherical shape, and M  = 5.85 emu/g with negligible coercivity. Drug loading and release studies were carried out using protocatechuic acid (PCA) as the model for anticancer drug, which showed 19% and 87% of PCA release in pH 7.4 and 4.8, respectively. Monolayer anticancer assay showed that PCA-loaded MMT/SW/Fe O (MMT/SW/Fe O -PCA) had selectivity towards HCT116 (colorectal cancer cell line). Although MMT/SW/Fe O -PCA (0.64 mg/mL) showed higher IC than PCA (0.148 mg/mL) and MMT/SW/Fe O (0.306 mg/mL, MMT/SW/Fe O -PCA showed more effective killing towards tumour spheroid model generated from HCT116. The IC for MMT/SW/Fe O -PCA, MMT/SW/Fe O and PCA were 0.132, 0.23 and 0.55 mg/mL, respectively. This suggests the improved penetration efficiency and drug release of MMT/SW/Fe O -PCA towards HCT116 spheroids. Moreover, concentration that lower than 2 mg/mL MMT/SW/Fe O -PCA did not result any hemolysis in human blood, which suggests them to be ideal for intravenous injection. This study highlights the potential of MMT/SW/Fe O -NCs as drug delivery agent.