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The Novel Approach in the Anticancer Agents: From Design to Formulation

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (28 February 2024) | Viewed by 1568

Special Issue Editor


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Guest Editor
1. Department of Paediatrics and Inherited Metabolic Disorders, First Faculty of Medicine, Charles University and General University Hospital in Prague, Ke Karlovu 455/2, 128 08 Prague 2, Czech Republic
2. BIOCEV, First Faculty of Medicine, Charles University, Průmyslová 595, 252 50 Vestec, Czech Republic
3. Department of Analytical Chemistry, Faculty of Chemical Engineering, University of Chemistry and Technology, Technická 5, 166 28 Prague, Czech Republic
Interests: nature compounds; drug delivery system; formulation; oncological diseases; neurodegenerative diseases

Special Issue Information

Dear Colleagues,

Despite tremendous research efforts and advances, cancer unfortunately continues to take its terrible toll. Given its complexity and heterogeneity, it is difficult to choose the right molecular target and the appropriate method of targeting. The side effects of the therapies used are very harmful for the patients and can strongly decrease their therapeutic potential. Additionally, the long delay between discovery and application and the enormous financial requirements of pharmaceutical research are significant limiting factors. They could be used also as nature agents, but their effectivity can be often limited due to low solubility and bioactivity.

On the other hand, some promising strategies (drug delivery system, reformulation, repurposing, and combination therapy) are studied and used for overcoming the above obstacles. For example, commercially available liposomal formulations display significantly lower levels of cardiotoxicity of doxorubicin and can sometimes improve the bioactivity of nature compounds. The combination of polyphenolic compounds and anticancer therapies can display a strong synergic anticancer effect and lower side effects.

This Special Issue, “The Novel Approach in the Anticancer Agents: From Design to Formulation”, invites researchers to contribute with original research or updated review articles that are focused on an increase in the effectivity of clinically used drugs and nature agents by DDS, formulation, or their combination, and repurposing used drugs for cancer treatment. Nevertheless, articles, inspired structure motifs of used anticancer agents, and/or studies of interesting molecular targets are also welcomed.

I would like to dedicate this Special Issue to the memory of my supervisor, prof. Vladimír Král Dr.Sc., whose lifelong approach is displayed by this philosophy. This Special Issue will honor his memory.

Dr. Zdeněk Kejik
Guest Editor

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Keywords

  • drug delivery systems
  • formulation and reformulation drug and nature agents
  • drug repurposing
  • combination therapy
  • molecular docking

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Published Papers (1 paper)

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15 pages, 3014 KiB  
Article
Improving Cancer Targeting: A Study on the Effect of Dual-Ligand Density on Targeting of Cells Having Differential Expression of Target Biomarkers
by Nayer Sultana and Allan E. David
Int. J. Mol. Sci. 2023, 24(17), 13048; https://doi.org/10.3390/ijms241713048 - 22 Aug 2023
Viewed by 1130
Abstract
Silica nanoparticles with hyaluronic acid (HA) and folic acid (FA) were developed to study dual-ligand targeting of CD44 and folate receptors, respectively, in colon cancer. Characterization of particles with dynamic light scattering showed them to have hydrodynamic diameters of 147–271 nm with moderate [...] Read more.
Silica nanoparticles with hyaluronic acid (HA) and folic acid (FA) were developed to study dual-ligand targeting of CD44 and folate receptors, respectively, in colon cancer. Characterization of particles with dynamic light scattering showed them to have hydrodynamic diameters of 147–271 nm with moderate polydispersity index (PDI) values. Surface modification of the particles was achieved by simultaneous reaction with HA and FA and results showed that ligand density on the surface increased with increasing concentrations in the reaction mixture. The nanoparticles showed minimal to no cytotoxicity with all formulations showing ≥ 90% cell viability at concentrations up to 100 µg/mL. Based on flow cytometry results, SW480 cell lines were positive for both receptors, the WI38 cell line was positive for CD44 receptor, and Caco2 was positive for the folate receptor. Cellular targeting studies demonstrated the potential of the targeted nanoparticles as promising candidates for delivery of therapeutic agents. The highest cellular targeting was achieved with particles synthesized using folate:surface amine (F:A) ratio of 9 for SW480 and Caco2 cells and at F:A = 0 for WI38 cells. The highest selectivity was achieved at F:A = 9 for both SW480:WI38 and SW480:Caco2 cells. Based on HA conjugation, the highest cellular targeting was achieved at H:A = 0.5–0.75 for SW480 cell, at H:A = 0.75 for WI38 cell and at H:A = 0.5 for Caco2 cells. The highest selectivity was achieved at H:A = 0 for both SW480:WI38 and SW480:Caco2 cells. These results demonstrated that the optimum ligand density on the nanoparticle for targeting is dependent on the levels of biomarker expression on the target cells. Ongoing studies will evaluate the therapeutic efficacy of these targeted nanoparticles using in vitro and in vivo cancer models. Full article
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