Search results for "Prodrug"
showing 10 items of 89 documents
Triplet stabilization for enhanced drug photorelease from sunscreen-based photocages
2021
[EN] Recently, sunscreen-based drug photocages have been introduced to provide UV protection to photoactive drugs, thus increasing their photosafety. Here, combined experimental and theoretical studies performed on a photocage based on the commercial UVA filter avobenzone (AB) and on the photosensitizing non-steroidal anti-inflammatory drug ketoprofen (KP) are presented unveiling the photophysical processes responsible for the light-triggered release. Particular attention is paid to solvent stabilization of the drug and UV filter excited states, respectively, which leads to a switching between the triplet excited state energies of the AB and KP units. Most notably, we show that the stabiliz…
Calixarene: A Versatile Material for Drug Design and Applications
2016
The therapy of various diseases by the drugs entrapped in calixarene derivatives is gaining attraction of researchers nowadays. Calixarenes are macrocyclic nano-baskets which belong to cavitands class of host-guest chemistry. They are the marvelous hosts with distinct hydrophobic three dimensional cavities to entrap and encapsulate biologically active guest drugs. Calixarene and its derivatives develop inclusion complexes with various types of drugs and vitamins for their sustained/targeted release. Calixarene and its derivatives are used as carriers for anti-cancer, anti-convulsant, anti-hypertensive, anthelmentic, anti-inflammatory, antimicrobial and antipsychotic drugs. They are the impo…
The role of red yeast rice (RYR) supplementation in plasma cholesterol control: A review and expert opinion.
2019
1. Preamble : Hypercholesterolemia is a major risk factor for atherosclerotic cardiovascular disease (ASCVD) [1]. Increased levels of low density lipoprotein cholesterol (LDL-C) are associated with an increased risk of coronary heart disease (CHD) and many clinical trials have shown that reducing LDL-C levels significantly reduced the CHD and CVD risk [[2], [3], [4], [5]]. Thus LDL-C-lowering is the main approach for the management of cardiovascular disease. Current guidelines suggest LDL-C levels targets based on the individual CV risk; such targets can be achieved by several means, which include both lifestyle changes and pharmacological approaches [6], with statins being the cornerstone …
Self-organized environment-sensitive inulin–doxorubicin conjugate with a selective cytotoxic effect towards cancer cells
2015
An inulin-based random copolymer bearing high dose doxorubicin (18.45% on a weight basis), INU-EDA-P, C-DOXO, was prepared by coupling doxorubicin with inulin though a citraconylamide bridge used as a pH sensitive spacer. A further conjugation with pentynoic acid via an amidic bond led to the hydrophobization of the copolymer which allows the acquisition of a self-assembling ability at low concentration (0.33 mg mL(-1)) combining both Pi-Pi stacking and London interactions. Drug release studies were carried out at different pH demonstrating a remarkable pH dependency, where the maximum release rate was observed at pH mimicking cancer tissue and lysosomal environments. Besides, by measuring …
Multiple cross-linked hydroxypropylcellulose–succinate–salicylate: prodrug design, characterization, stimuli responsive swelling–deswelling and susta…
2015
A hydroxypropylcellulose–succinic anhydride (HPC–SAn) conjugate was synthesized homogeneously at 80 °C for 6 h under N2 in N,N-dimethylacetamide (DMA). The HPC–SAn conjugate was further covalently linked with salicylic acid (SA) drug using the versatile reagent ZrOCl2·8H2O at 80 °C for 6 h. Multiple crosslinking of the benign HPC–SAn–SA conjugate was achieved using oxalyl chloride. The resultant cross-linked prodrug (CL-HPC–SAn–SA conjugate) was characterized using different spectroscopic techniques. UV/Vis analysis of the HPC–SAn–SA conjugate has indicated that it contains 26 mg of SA per 100 mg. CL-HPC–SAn–SA showed reasonably good swelling properties in water and at different physiologic…
Direct chemical grafted curcumin on halloysite nanotubes as dual-responsive prodrug for pharmacological applications
2016
Covalently functionalized halloysite nanotubes (HNTs) were successfully employed as dual-responsive nanocarriers for curcumin (Cur). Particularly, we synthesized HNT-Cur prodrug with a controlled curcumin release on dependence of both intracellular glutathione (GSH) and pH conditions. In order to obtain HNT-Cur produgs, halloysite was firstly functionalized with cysteamine through disulphide linkage. Afterwards, curcumin molecules were chemically conjugated to the amino end groups of halloysite via Schiff's base formation. The successful functionalization of halloysite was proved by thermogravimetric analysis, FT-IR spectroscopy, dynamic light scattering and scanning electron microscopy. Ex…
1,2,3-Oligotriazoles modified halloysite nanotubes as potential active biological species: synthesis and characterization
2022
In the last years, the development of nano-formulations for cancer treatment represents one of the major challenges of the scientific research. The prodrug strategy, that combines chemotherapeutic agents with nanocarriers such as halloysite nanotubes (HNTs), is a promising strategy both to improve the biological activity of the drug molecules and to reduce the side effects of drugs. Herein we report the synthesis and characterization of a HNTs prodrug based on 1,2,3-triazole units covalently linked to HNTs external surface, bearing different positively charged moieties, which could present interesting pharmacological activities.
124I Radiolabeling of a AuIII‐NHC Complex for In Vivo Biodistribution Studies†
2020
Abstract AuIII complexes with N‐heterocyclic carbene (NHC) ligands have shown remarkable potential as anticancer agents, yet their fate in vivo has not been thoroughly examined and understood. Reported herein is the synthesis of new AuIII‐NHC complexes by direct oxidation with radioactive [124I]I2 as a valuable strategy to monitor the in vivo biodistribution of this class of compounds using positron emission tomography (PET). While in vitro analyses provide direct evidence for the importance of AuIII‐to‐AuI reduction to achieve full anticancer activity, in vivo studies reveal that a fraction of the AuIII‐NHC prodrug is not immediately reduced after administration but able to reach the major…
Increased recovery of brain acetylcholinesterase activity in dichlorvos-intoxicated European eels Anguilla anguilla by bath treatment with N-acetylcy…
2003
Organophosphate (OP) pesticides are widely used as antiparasitic chemicals in finfish aquaculture. However, current antidotes cannot be applied to treat intoxicated fish. We showed in previous studies the importance of glutathione (GSH) metabolism in pesticide resistance of the European eel Anguilla anguilla L. The present work studied the effects of the antioxidant and glutathione pro-drug N-acetyl-l-cysteine (NAC) on the recovery of European eels exposed for 96 h to a sublethal concentration (0.17 mg l^-1; 20% of its 96 h LC50) of the OP pesticide dichlorvos (2,2-dichlorovinyl dimethyl phosphate; DDVP). This insecticide and acaricide decreased muscular GSH content and increased oxidised g…
Hydrophilic and Hydrophobic Polymeric Derivatives of Anti-Inflammatory Agents Such as Alclofenac, Ketoprofen, and Ibuprofen
1991
Macromolecular prodrugs of a hydrophilic polymer [α,β-poly( N- hydroxyethyl)-DL-aspartamide (PHEA)] was used as a drug carrier. Three poly- (HEA)-NSAID adducts were studied: poly(HEA)-Alclofenac, poly(HEA)-Keto profen, and poly(HEA)-Ibuprofen. Prodrugs with different drug content were synthesized both as water-soluble and water-insoluble agents. Hydrolysis of water-soluble adducts in a simulated gastric juice was studied.