May 2025
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3 Reads
Colloids and Surfaces B Biointerfaces
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May 2025
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3 Reads
Colloids and Surfaces B Biointerfaces
May 2025
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11 Reads
Journal of Molecular Structure
January 2025
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52 Reads
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1 Citation
Colloids and Interfaces
A 2D imine-linked covalent organic framework (COF) with good biocompatibility was synthesized using o-Dianisidine and 1,3,5-Triformylbenzene. The synthesized COF was characterized by using the Fourier transform infrared (FTIR), thermogravimetry analysis (TGA), scanning electron microscopy (SEM), and transmission electron microscopy (TEM). The synthesized COF was subsequently utilized for the delivery of gemcitabine (Gem), an FDA-approved drug for the treatment of pancreatic cancer. The COF demonstrated a remarkable drug loading of 30 µg/mg and better drug release at pH 5.0. The biocompatibility of the COF was evaluated in the L929 (mouse fibroblast) cell line, while the cytotoxicity of the Gem-loaded COF (COF-Gem) was evaluated against the MIA-PaCa-2 and PANC-1 (pancreatic cancer) cell lines using MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. The results indicated that the COF was safe at concentrations up to 200 µg/mL, while the COF-Gem led to superior cytotoxicity as compared to native Gem, with IC50 values of 8.1 ± 1.2 µM in MIA-PaCa-2 cells and 6.0 ± 1.3 µM in PANC-1 cells after 48 h. This study offers a new perspective of utilizing COF as a promising delivery system for Gem delivery.
January 2025
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48 Reads
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1 Citation
Gemcitabine (GEM), a chemotherapeutic agent, is widely used to treat various neoplastic conditions, such as pancreatic, lung, breast, and ovarian cancer. However, its therapeutic effectiveness is often hindered by its short half‐life and susceptibility to enzymatic degradation. To address these limitations, in this research, five new conjugates of GEM were synthesized by conjugating its N‐4 amino group with five different acids [4‐decenoic acid (4Dec), lipoic acid (Lipo), lauric acid (Laur), 5‐benzyl N‐(tert‐butoxycarbonyl)‐ L‐glutamate (Glu), and decanoic acid (Dec)]. The anticancer potential of these conjugates was evaluated using CCK‐8 assay. Among the synthesized conjugates, 4Dec‐GEM demonstrated comparable cytotoxic activity to native GEM. The mechanistic insight of 4Dec‐GEM was investigated using annexin‐V FITC/propidium iodide staining, reactive oxygen species generation, and mitochondrial membrane potential loss assays. To further enhance its therapeutic efficacy, 4Dec‐GEM was encapsulated into poly(lactic‐co‐glycolic acid) (PLGA) nanoparticles using single‐emulsion method using high‐pressure homogenization. The developed nanoparticles were characterized by various techniques (TEM, FT‐IR, DSC, p‐XRD) and demonstrated successful entrapment of 4Dec‐GEM inside PLGA nanoparticles. Finally, the cytotoxicity of developed nanoparticles demonstrated improved anticancer activity as compared to native GEM in cancerous cell lines. Our study demonstrated that the combination of prodrug and nanoparticle approach can be a promising approach to augment the therapeutic efficacy of GEM.
December 2024
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28 Reads
Molecular Pharmaceutics
December 2024
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39 Reads
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2 Citations
International Journal of Biological Macromolecules
April 2024
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70 Reads
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11 Citations
Biotechnology Advances
March 2024
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33 Reads
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12 Citations
International Journal of Biological Macromolecules
February 2024
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46 Reads
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10 Citations
Drug Discovery Today
January 2024
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81 Reads
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3 Citations
In this study, a hybrid conjugate of formononetin (FMN) and vitamin E (VESylated‐FMN) was synthesized through succinic acid linker and investigated for its synergistic effect in diabetes. The conjugate was characterized through Ultra Performance Liquid Chromatography – Mass Spectrometry (UPLC‐MS), High‐Resolution Mass Spectrometry (HRMS), Nuclear Magnetic Resonance (NMR), and Differential Scanning Calorimetry (DSC). The ability of VESylated‐FMN to promote adipogenesis and ameliorate insulin resistance brought on by oxidative stress was evaluated in differentiated preadipocytes. Interestingly, VESylated‐FMN promoted intracellular glucose absorption, which in turn increased lipid and triglyceride accumulation and thereby encouraged adipogenesis. VESylated‐FMN attenuated oxidative stress and promoted cell survival by reducing reactive oxygen species (ROS) generation and reversing apoptosis. Additionally, VESylated‐FMN improved insulin sensitization by upregulating the gene and protein expression of insulin‐sensitizing markers. Overall, FMN in conjugation with vitamin E can effectively augment prior insulin sensitivity by reducing oxidative stress for efficient glycemic control in hyperglycemia.
... The synthesized COF was further explored for the delivery of Gemcitabine (Gem), a pyrimidine nucleoside analog. Gem is widely used, either alone or in combination with other chemotherapeutic agents or radiation therapy, to treat a range of cancers, including pancreatic, ovarian, bladder, breast, and non-small-cell lung cancers [24]. Further, Gem exhibits poor loading efficiency when entrapped into polymeric and lipid-based nanoparticles. ...
January 2025
... The study confirms SSG's suitability for 3D printing of OTFs. accurate dosing, enhanced oral absorption, improved bioavailability through minimization of drug degradation, better stability, dose tunability, portability, etc. [4]. Three-dimensional (3D) printing has become increasingly important in drug delivery since it offers a safer and more effective method for administering potent therapeutics [5,6]. ...
April 2024
Biotechnology Advances
... As already stated, the application of these 3D platforms and models is of particular interest in cancer research [9]. In fact, several studies have reported the 3D bioprinting of tumor models, as well as their use for anti-tumoral drug screening and testing, as recently summarized by Ruchika et al. [10] and Li et al. [11]. Furthermore, 3D bioprinting has been successfully explored for the development of 3D melanoma models using different cell lines. ...
February 2024
Drug Discovery Today
... This has also been shown to decrease the levels of the inflammatory cytokines IL-1β and TNF-α in mice fed a high-fat diet. This activity suppressed proinflammatory NF-κB signaling and increased the antiinflammatory action of Nrf-2/HO-1 in the hippocampus (Yang et al. 2019), (Kumar Dhritlahre et al. 2024). ...
January 2024
... The FTIR spectra of all the samples are shown in Figure 2. The characteristic peaks of the FTIR spectra of PT are as follows: 3272 cm −1 (-OH bond stretching vibration peak), 2928 cm −1 (-CH 2 -asymmetric stretching vibration peak), 1606 cm −1, 1573 cm −1 ,1513 cm −1 , and 1473 cm −1 (C═C stretching vibration peak in aromatic ring skeleton; Chhimwal et al., 2023). In the FTIR spectra of PT NEs and PT-VE-NEs, some peaks of PT appeared. ...
September 2023
Biomaterials Advances
... COFs consist well-defined and lightweight elements such as hydrogen (H), carbon (C), nitrogen (N), oxygen (O), and boron (B), possess electron-rich groups, a large surface area and highly stable structures, rendering them excellent reservoirs with ultrahigh loading ratios (Khan et al. 2023). As a result, they have been employed to effectively deliver different types of functional agents, including anti-cancer drugs, small interfering RNAs (siRNAs), radiosensitizers, sonosensitizers, photosensitizers, and small molecule inhibitors to the tumor site via the systemic route. ...
April 2023
Drug Discovery Today
... The chitosan powder exhibited a semicrystalline state, and the diffractogram of chitosan presented an almost halo pattern [77]. The PXRD pattern of ascorbic acid demonstrated that it is a crystalline substance, as evidenced by multiple sharp diffraction peaks that correspond to the crystalline diffraction lines described in the literature [78]. According to the diffractogram of metronidazole, the multiple sharp reflections reflected the crystalline form of the drug. ...
March 2023
... Therefore, there is an eagerness to develop a scientific method for the envelope material feasibility to provide scientific guidance. Recent advances in silico techniques have resulted in more powerful methods to analyze the host-guest interactions of IC, for example, molecular docking [34], molecular dynamic (MD) simulations [35], and umbrella sampling simulations [28], etc. Molecular docking provides information about the interactions between CDs and guest sites [17]. ...
March 2023
Journal of Molecular Liquids
... In a rodent model of epilepsy induced by pentylenetetrazol via an Nrf2 pathway, treatment with ALA improved behavioral dysfunction and significantly reduced the number of epileptic seizures . Unfortunately, as a drug candidate, ALA has poor pharmacokinetic properties that limit its therapeutic potential (Kumari et al., 2022;Salehi et al., 2019;Steliou et al., 2015;Usacheva et al., 2022). Ongoing efforts in design and chemical synthesis aim to overcome these deficiencies using ALA prodrugs prepared from analogues, derivatives or conjugates as potential therapeutics with more favorable pharmacological properties (Javaid et al., 2022;Kong et al., 2022;Kumari et al., 2022;Lv et al., 2022;Moos et al., 2022;Steliou et al., 2015;Wang et al., 2020;Zielonka et al., 2017). ...
June 2022
Journal of Agricultural and Food Chemistry
... Among current antitumor treatments, chemotherapy plays an essential role, but most chemical agents have low specificity for cancer cells, resulting in toxicity and side effects in the body [2]. To overcome these obstacles, many studies have focused on tumorspecific targeting systems, which are expected to play an important role in the next generation of chemotherapy treatments [3,4]. ...
April 2022
Drug Discovery Today