Targeted delivery and enhanced gene-silencing activity of folic acid-siRNA conjugates in cancer cells.

2020 ◽  
Author(s):  
Lidya Salim
Keyword(s):  
Folic Acid ◽  
Gene Silencing ◽  
Cancer Cells ◽  
Targeted Delivery

scholarly journals Targeted delivery and enhanced gene-silencing activity of centrally modified folic acid–siRNA conjugates

2019 ◽  
Vol 48 (1) ◽  
pp. 75-85 ◽  
Author(s):  
Lidya Salim ◽  
Golam Islam ◽  
Jean-Paul Desaulniers
Keyword(s):  
Folic Acid ◽  
Gene Silencing ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Target Cells ◽  
Gene Target ◽  
Folate Receptors ◽  
Normal Tissues ◽  
Sense Strand ◽  
Low Cytotoxicity

Abstract One of the major hurdles in RNAi research has been the development of safe and effective delivery systems for siRNAs. Although various chemical modifications have been proposed to improve their pharmacokinetic behaviour, their delivery to target cells and tissues presents many challenges. In this work, we implemented a receptor-targeting strategy to selectively deliver siRNAs to cancer cells using folic acid as a ligand. Folic acid is capable of binding to cell-surface folate receptors with high affinity. These receptors have become important molecular targets for cancer research as they are overexpressed in numerous cancers despite being expressed at low levels in normal tissues. Employing a post-column copper-catalyzed alkyne–azide cycloaddition (CuAAC), we report the synthesis of siRNAs bearing folic acid modifications at different positions within the sense strand. In the absence of a transfection carrier, these siRNAs were selectively taken up by cancer cells expressing folate receptors. We show that centrally modified folic acid–siRNAs display enhanced gene-silencing activity against an exogenous gene target (∼80% knockdown after 0.75 μM treatment) and low cytotoxicity. In addition, these siRNAs achieved potent dose-dependent knockdown of endogenous Bcl-2, an important anti-apoptotic gene.

scholarly journals Effective Targeting of Colon Cancer Cells with Piperine Natural Anticancer Prodrug Using Functionalized Clusters of Hydroxyapatite Nanoparticles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 70 ◽  
Author(s):  
Khaled AbouAitah ◽  
Agata Stefanek ◽  
Iman M. Higazy ◽  
Magdalena Janczewska ◽  
Anna Swiderska-Sroda ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Folic Acid ◽  
Cancer Cells ◽  
Delivery System ◽  
Targeted Delivery ◽  
Gum Arabic ◽  
Colon Cancer Cells ◽  
Hydroxyapatite Nanoparticles ◽  
Anticancer Effects ◽  
Targeted Delivery System

Targeted drug delivery offers great opportunities for treating cancer. Here, we developed a novel anticancer targeted delivery system for piperine (Pip), an alkaloid prodrug derived from black pepper that exhibits anticancer effects. The tailored delivery system comprises aggregated hydroxyapatite nanoparticles (HAPs) functionalized with phosphonate groups (HAP-Ps). Pip was loaded into HAPs and HAP-Ps at pH 7.2 and 9.3 to obtain nanoformulations. The nanoformulations were characterized using several techniques and the release kinetics and anticancer effects investigated in vitro. The Pip loading capacity was >20%. Prolonged release was observed with kinetics dependent on pH, surface modification, and coating. The nanoformulations fully inhibited monolayer HCT116 colon cancer cells compared to Caco2 colon cancer and MCF7 breast cancer cells after 72 h, whereas free Pip had a weaker effect. The nanoformulations inhibited ~60% in HCT116 spheroids compared to free Pip. The Pip-loaded nanoparticles were also coated with gum Arabic and functionalized with folic acid as a targeting ligand. These functionalized nanoformulations had the lowest cytotoxicity towards normal WI-38 fibroblast cells. These preliminary findings suggest that the targeted delivery system comprising HAP aggregates loaded with Pip, coated with gum Arabic, and functionalized with folic acid are a potentially efficient agent against colon cancer.

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

2020 ◽  
Vol 231 ◽  
pp. 115682 ◽  
Author(s):  
Chinnaiyan Senthil Kumar ◽  
Ramar Thangam ◽  
Soloman Agnes Mary ◽  
Perumal Ramesh Kannan ◽  
Gopinath Arun ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Folic Acid ◽  
Ferulic Acid ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
Apoptosis Induction ◽  
Colon Cancer Cells ◽  
Acid Conjugate

Synthesis and Characterization of Folic Acid Conjugated Gemcitabine Tethered Silver Nanoparticles (FA-GEM-AgNPs) for Targeted Delivery

2020 ◽  
Vol 26 (26) ◽  
pp. 3141-3146 ◽  
Author(s):  
Arjunan Karuppaiah ◽  
Ravikumar Rajan ◽  
Sivaram Hariharan ◽  
Dinesh K. Balasubramaniam ◽  
Marslin Gregory ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Silver Nanoparticles ◽  
Folic Acid ◽  
Cancer Cells ◽  
Targeted Delivery ◽  
Cytotoxic Effect ◽  
Apoptotic Cell ◽  
Folate Receptor ◽  
Cancer Cell Line ◽  
One Pot

Background: Silver nanoparticles (AgNPs) have attracted considerable interest in the medical industry due to their physicochemical properties, small size, and surface plasmon behavior. Their smaller particle size and instability in blood circulation leads to toxicity due to its aggregation as Ag+ ions and accumulation at the deepseated organ. In the present study, we aimed at reducing the toxicity of AgNPs by conjugation with an anticancer drug GEM and to improve their internalization through folate receptors-mediated endocytosis by capping the nanoparticles with folic acid (FA). Methods: One-pot facile synthesis of FA capped silver nanoparticles (FA-AgNPs) has been achieved by using FA as a reducing agent. FA-AgNPs were mixed with Gemcitabine (GEM) to obtain tethered FA-GEM-AgNPs. Nanoparticles were characterized by Dynamic Light Scattering (DLS), UV-Visible spectroscopy, Transmission Electron Microscopy (TEM), Energy Dispersive X-ray Analysis (EDAX), Selected Area Electron Diffraction (SAED), and Atomic Absorption Spectroscopy (AAS). The 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay was carried out to determine the cytotoxic effect of the prepared nanoformulations. The apoptotic cell death induced by FA-GEM-AgNPs in breast cancer cells were monitored with Acridine orange (AO)/Ethidium Bromide (EtBr) staining. Conclusion: Compared to GEM and AgNPs, FA-GEM-AgNPs showed enhanced cytotoxic effect and internalization in MDA-MB-453 breast cancer cell line. FA-GEM-AgNPs could be an ideal candidate for targeting cancer cells via folate receptor-mediated endocytosis.

scholarly journals Folate receptor targeted delivery of paclitaxel to breast cancer cells via folic acid conjugated graphene oxide grafted methyl acrylate nanocarrier

2019 ◽  
Vol 110 ◽  
pp. 906-917 ◽  
Author(s):  
Kandasamy Vinothini ◽  
Naresh Kumar Rajendran ◽  
Andy Ramu ◽  
Nandhakumar Elumalai ◽  
Mariappan Rajan
Keyword(s):  
Breast Cancer ◽  
Graphene Oxide ◽  
Folic Acid ◽  
Cancer Cells ◽  
Methyl Acrylate ◽  
Targeted Delivery ◽  
Breast Cancer Cells ◽  
Folate Receptor

Targeted delivery of doxorubicin into cancer cells using a folic acid–dendrimer conjugate

2011 ◽  
Vol 2 (8) ◽  
pp. 1754 ◽  
Author(s):  
Yin Wang ◽  
Xueyan Cao ◽  
Rui Guo ◽  
Mingwu Shen ◽  
Mengen Zhang ◽  
...  
Keyword(s):  
Folic Acid ◽  
Cancer Cells ◽  
Targeted Delivery

Role of generation on folic acid-modified poly(amidoamine) dendrimers for targeted delivery of baicalin to cancer cells

2017 ◽  
Vol 75 ◽  
pp. 182-190 ◽  
Author(s):  
Tingting Lv ◽  
Tingting Yu ◽  
Yunpeng Fang ◽  
Suyan Zhang ◽  
Minghong Jiang ◽  
...  
Keyword(s):  
Folic Acid ◽  
Cancer Cells ◽  
Targeted Delivery

Folic acid-polyamine-β-cyclodextrin for targeted delivery of scutellarin to cancer cells

2015 ◽  
Vol 26 (5) ◽  
pp. 487-494 ◽  
Author(s):  
Rongqiang Liao ◽  
Yulin Zhao ◽  
Xiali Liao ◽  
Manshuo Liu ◽  
Chuanzhu Gao ◽  
...  
Keyword(s):  
Folic Acid ◽  
Cancer Cells ◽  
Targeted Delivery
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