Design, graph theoretical analysis and bioinformatic studies of proanthocyanidins encapsulated ethyl cellulose nanoparticles for effective anticancer activity

Abstract

Phytoconstituent's has significant antioxidant and anticancer activity against various types of cancer cells. But these water soluble phytoconstituent's has poor absorption due to their huge molecular size as well as it cannot be reach at the targeted disease site, thus targeted drug delivery system is one of the effective approaches to enhancing the bioavailability and decreasing drug toxicity. To achieve this target, the Proanthocyanidins (Pro) and ethyl cellulose (EC) was used to formulate nanoparticles (NPs) for effective drug delivery system. The Pro encapsulated ECNPs were formulated by simple anti-solvent particle induction method and its physico-chemical characteristics were examined by FTIR, XRD, Zeta size analyzer, SEM, and TEM. The graph theoretical network analysis was implemented to identify the drug target and subsequently molecular docking studies were screened. The identified target using graph theoretical analysis and molecular docking study reported strong interaction of Pro encapsulated ECNPs in binding pockets of MAPK. The formulated ECNPs has been very effective in arresting the proliferation of colon cancer (HT-29) cells with an IC 50 value of 33.4 μg ml −1 after 24 h treatment. Further, HT-29 cells exposure with Pro encapsulated ECNPs resulted in typical apoptotic through necrotic cellular morphology, loss of mitochondrial transmembrane potential, and high ROS generation were also observed. The observed results highlight that EC as a potential carrier material for enhancing the bioavailability of anti-cancer drugs.

Capsaicin-loaded solid lipid nanoparticles: design, biodistribution, in silico modeling and in vitro cytotoxicity evaluation

“…The in vitro cytotoxicity of capsaicin loaded SLNs was evaluated in human hepatocellular carcinoma cells (HepG2) using the 3-(4,5-dimethylthiazol-2-yl-)-2,5-diphenyltetrazolium bromide (MTT) assay according to the previously reported method [54] with slight modifications. HepG2 cells were seeded onto 96 multi-well plate at approximately 5×10 3 cells/well and incubated for 24 h in 5% CO 2 atmosphere and 95% humidity to obtain 100% confluence.…”

Design,in silicomodelling and functionality theory of folate-receptor-targeted myricetin-loaded bovine serum albumin nanoparticle formulation for cancer treatment

“…To evaluate apoptosis using fluorescence microscopy, AO/ EB staining was used [4]. In brief, MCF-7 cells (1× 10 5 cells/well) were seeded onto a cover slip insert in a 24-well culture plate and incubated for 24 h prior to the assay.…”

“…The mitochondrial membrane potential change (ΔΨ m ) was monitored using a method described previously [4]. In brief, MCF-7 cells were cultured at 37 °C for 4 h with IC 50 concentration of FA-Myr-BSA NPs, and washed with ice-cold PBS.…”

“…The leading global causes of death are cardiovascular disorders, cancers, and diabetes [2]. Breast, stomach, lung, colorectal/colon, and liver cancers are the most common causes of cancer-related deaths [3,4]. In women, breast cancer is the most often and frequently diagnosed malignancy and a major cause of death, with ∼11+million new cases and ∼6+million deaths in 2018 [5].…”

Surface receptor‐mediated targeted drug delivery systems for enhanced cancer treatment: A state‐of‐the‐art review

“…Regrettably, most of the chemotherapeutics (both under development and in clinical use) are non‐selectively distributed to entire organs/tissues of the body and interact with cancerous as well as normal healthy cells (Baskararaj et al, 2020; Nazir et al, 2014). The nonselective distribution of drug leads to unfavorable toxic effects and disturbance of normal levels of reactive oxygen species (ROS)/reactive nitrogen species (RON), Ca 2+ , and so forth, and it could trigger oxidative damage in normal cellular mitochondria and finally initiate cell death (Chauhan, 2002; Kunjiappan, Theivendren, et al, 2019). Again, repeated nonselective chemotherapeutics leads to drug resistance (failure of therapeutics) against cancer cells (Silva et al, 2012).…”