Targeted delivery and apoptosis induction of trans-resveratrol-ferulic acid loaded chitosan coated folic acid conjugate solid lipid nanoparticles in colon cancer cells

• Published in: Carbohydrate polymers Vol. 231; p. 115682
• Main Authors: Senthil Kumar, Chinnaiyan, Thangam, Ramar, Mary, Soloman Agnes, Kannan, Perumal Ramesh, Arun, Gopinath, Madhan, Balaraman
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.03.2020
• Subjects: apoptosis; cancer therapy; Cellular apoptosis; chitosan; Colon cancer; colorectal neoplasms; Cytotoxicity; drug delivery systems; drugs; Ferulic acid; flow cytometry; fluorescence; folic acid; Fourier transform infrared spectroscopy; human cell lines; nanoparticles; neoplasm cells; particle size; Solid lipid nanoparticles (SLNs); staining; stearic acid; Trans-resveratrol; Western blotting; X-ray diffraction; zeta potential; Trans-resveratrol; Solid lipid nanoparticles (SLNs); Cytotoxicity; Colon cancer; Cellular apoptosis; Ferulic acid
• ISSN: 0144-8617; 1879-1344; 1879-1344
• DOI: 10.1016/j.carbpol.2019.115682

[Display omitted] •Chitosan coated RSV-FER-FA-SLNs are synthesized for targeted dual drug delivery.•Characterized using FTIR, XRD, HRTEM, NMR and HPLC analysis.•C-RSV-FER-FA-SLNs showed cytotxicity towards cancer cells with targeting efficiency.•C-RSV-FER-FA-SLNs effectively delivered the loaded drugs and activated apoptosis.•C-RSV-FER-FA-SLNs regulated the expression of cyclin proteins and cell cycle arrest. The present study is aimed to study and to evaluate the colon cancer targeting efficacy of chitosan-coated-trans-resveratrol (RSV) and ferulic acid (FER) loaded SLNs (solid lipid nanoparticles) that conjugated with folic acid (FA) (C-RSV-FER-FA-SLNs) in suitable models (in vitro). The FA conjugation is performed using co-encapsulation method of stearic acid. Similarly, the prepared SLNs are exhibited better stability even under acidic conditions to exhibit their potentials to use as drug delivery system. Further, the optimized formulations (SLNs) are tested for physiochemical characterizations, which include FTIR, XRD, 1HNMR, particle size, zeta potential, and drug release. In vitro anti-cancer studies using HT-29 cells including, fluorescence staining, flow cytometry, and western blot analysis revealed that the C-RSV-FER-FA-SLNs effectively involved and increased cytotoxicity in cancer cells that leads to induction of apoptosis as compared to free RSV-FER. Thus, it is reported that, the good stability under acidic conditions of this C-RSV-FER-FA-SLNs may serve as a promising candidate for novel nanodrug formulations in cancer therapy.