scholarly journals Retinoids Delivery Systems in Cancer: Liposomal Fenretinide for Neuroectodermal-Derived Tumors

2021 ◽  
Vol 14 (9) ◽  
pp. 854
Author(s):  
Veronica Bensa ◽  
Enzo Calarco ◽  
Elena Giusto ◽  
Patrizia Perri ◽  
Maria Valeria Corrias ◽  
...  
Keyword(s):  
Side Effects ◽  
Therapeutic Agents ◽  
Delivery Systems ◽  
Target Cells ◽  
Pharmacological Properties ◽  
Biological Processes ◽  
Synthetic Compounds ◽  
Water Sensitivity ◽  
Proliferation And Apoptosis ◽  
Therapeutic Results

Retinoids are a class of natural and synthetic compounds derived from vitamin A. They are involved in several biological processes like embryogenesis, reproduction, vision, growth, inflammation, differentiation, proliferation, and apoptosis. In light of their important functions, retinoids have been widely investigated for their therapeutic applications. Thus far, their use for the treatment of several types of cancer and skin disorders has been reported. However, these therapeutic agents present several limitations for their widespread clinical translatability, i.e., poor solubility and chemical instability in water, sensitivity to light, heat, and oxygen, and low bioavailability. These characteristics result in internalization into target cells and tissues only at low concentration and, consequently, at an unsatisfactory therapeutic dose. Furthermore, the administration of retinoids causes severe side-effects. Thus, in order to improve their pharmacological properties and circulating half-life, while minimizing their off-target uptake, various retinoids delivery systems have been recently developed. This review intends to provide examples of retinoids-loaded nano-delivery systems for cancer treatment. In particular, the use and the therapeutic results obtained by using fenretinide-loaded liposomes against neuroectodermal-derived tumors, such as melanoma, in adults, and neuroblastoma, the most common extra-cranial solid tumor of childhood, will be discussed.

Clinical Pharmacology and Pharmacokinetics of Fluoxetine: A Review

1988 ◽  
Vol 153 (S3) ◽  
pp. 47-50 ◽  
Author(s):  
R. F. Bergstrom ◽  
L. Lemberger ◽  
N. A. Farid ◽  
R. L. Wolen
Keyword(s):  
Clinical Pharmacology ◽  
Antidepressant Drug ◽  
Therapeutic Agents ◽  
Systematic Evaluation ◽  
Pharmacological Properties ◽  
Lead Compound ◽  
Serotonin Uptake Inhibitors ◽  
Synthetic Compounds ◽  
Structure Activity ◽  
Complex Process

Drugs are discovered by a variety of approaches, which include a systematic evaluation of synthetic compounds, using extensive structure activity relationships. After a lead compound which possesses desirable pharmacological properties is found, through the exhaustive screening of a variety of compounds, a number of congeners are then synthesised and tested, using specific physiological or biochemical models of therapeutic agents. The discovery of fluoxetine involved this complex process, and led to the description in the literature of one of the first selective serotonin uptake inhibitors (Wonget al, 1974); it was subsequently tested clinically, and these studies demonstrated its effectiveness and safety as an antidepressant drug (Chouinard, 1985). This paper reviews the published information relevant to fluoxetine's pharmacology and pharmacokinetics in man.

On Cancer Nanotechnology

2010 ◽  
Vol 441 ◽  
pp. 307-332
Author(s):  
Rita Bosetti ◽  
Lode Vereeck
Keyword(s):  
Quality Of Life ◽  
Cancer Research ◽  
Side Effects ◽  
Cancer Biology ◽  
Causes Of Death ◽  
Poor Quality ◽  
Therapeutic Agents ◽  
Target Cells ◽  
Patients Experience

Although governments invest billions of dollars in cancer research, cancer remains one of the major causes of death worldwide (Liu et al., 2007). During the last decades, outstanding results have been attained in fundamental cancer biology but, unfortunately, they have not been translated in even distantly comparable progressions in the clinic. The main reason for this gap being the inability to administer therapeutic agents so that they can reach target cells without or with minimal side-effects (Ferrari, 2005). Today, scientists are faced with the recognition that very few molecules reach the desired locations and thus fail to selectively reach the target cells. Consequently, patients experience a very poor quality of life (Ferrari, 2004; Ferrari, 2005; Chan, 2006).

scholarly journals Recent Updates in the Treatment of Neurodegenerative Disorders Using Natural Compounds

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Mahmood Rasool ◽  
Arif Malik ◽  
Muhammad Saeed Qureshi ◽  
Abdul Manan ◽  
Peter Natesan Pushparaj ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Side Effects ◽  
Neurodegenerative Diseases ◽  
Neurodegenerative Disorders ◽  
Therapeutic Agents ◽  
Chronic Illnesses ◽  
Biological Processes ◽  
Brain Disorders ◽  
Synthetic Drugs ◽  
The Central Nervous System

Neurodegenerative diseases are characterized by protein aggregates and inflammation as well as oxidative stress in the central nervous system (CNS). Multiple biological processes are linked to neurodegenerative diseases such as depletion or insufficient synthesis of neurotransmitters, oxidative stress, abnormal ubiquitination. Furthermore, damaging of blood brain barrier (BBB) in the CNS also leads to various CNS-related diseases. Even though synthetic drugs are used for the management of Alzheimer’s disease, Parkinson’s disease, autism, and many other chronic illnesses, they are not without side effects. The attentions of researchers have been inclined towards the phytochemicals, many of which have minimal side effects. Phytochemicals are promising therapeutic agents because many phytochemicals have anti-inflammatory, antioxidative as well as anticholinesterase activities. Various drugs of either synthetic or natural origin applied in the treatment of brain disorders need to cross the BBB before they can be used. This paper covers various researches related to phytochemicals used in the management of neurodegenerative disorders.

A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer

2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza
Keyword(s):  
Side Effects ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Present Review ◽  
Pharmacological Properties ◽  
Important Group ◽  
Wide Range ◽  
Anti Inflammatory

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

Cationic Antimicrobial Peptides for Tuberculosis: A Mini-Review

2019 ◽  
Vol 20 (9) ◽  
pp. 885-892
Author(s):  
Sara Silva ◽  
Nuno Vale
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Amino Acid ◽  
Antimicrobial Peptides ◽  
Resistance Mechanisms ◽  
Therapeutic Agents ◽  
Pharmacological Properties ◽  
Therapeutic Activity ◽  
Alternative Strategies ◽  
Cationic Antimicrobial Peptides ◽  
Specific Amino Acid

Cationic antimicrobial peptides (CAMPs) can be considered as new potential therapeutic agents for Tuberculosis treatment with a specific amino acid sequence. New studies can be developed in the future to improve the pharmacological properties of CAMPs and also understand possible resistance mechanisms. This review discusses the principal properties of natural and/or synthetic CAMPs, and how these new peptides have a significant specificity for Mycobacterium tuberculosis. Also, we propose some alternative strategies to enhance the therapeutic activity of these CAMPs that include coadministration with nanoparticles and/or classic drugs.

Nanoparticle-based Drug Delivery Systems for Targeted Epigenetics Cancer Therapy

2020 ◽  
Vol 21 (11) ◽  
pp. 1084-1098
Author(s):  
Fengqian Chen ◽  
Yunzhen Shi ◽  
Jinming Zhang ◽  
Qi Liu
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Cancer Therapy ◽  
Drug Delivery Systems ◽  
Therapeutic Index ◽  
Delivery Systems ◽  
Epigenetic Therapy ◽  
Cancer Therapies ◽  
Therapeutic Benefits ◽  
High Therapeutic Index

This review summarizes the epigenetic mechanisms of deoxyribonucleic acid (DNA) methylation, histone modifications in cancer and the epigenetic modifications in cancer therapy. Due to their undesired side effects, the use of epigenetic drugs as chemo-drugs in cancer therapies is limited. The drug delivery system opens a door for minimizing these side effects and achieving greater therapeutic benefits. The limitations of current epigenetic therapies in clinical cancer treatment and the advantages of using drug delivery systems for epigenetic agents are also discussed. Combining drug delivery systems with epigenetic therapy is a promising approach to reaching a high therapeutic index and minimizing the side effects.

Synthesis and Biological Properties of some New Lead Sulphonamide and Carboxamide Scaffolds Bearing Coumarin Moiety (Mini Review)

2020 ◽  
Vol 20 ◽  
Author(s):  
Cosmas Chinweike Eze ◽  
Mercy Amarachukwu Ezeokonkwo ◽  
Benjamin Ebere Ezema ◽  
Abraham Efeturi Onoabedje ◽  
David Izuchukwu Ugwu
Keyword(s):  
Biological Properties ◽  
Therapeutic Agents ◽  
Amide Group ◽  
Pharmacological Properties ◽  
Important Class ◽  
Synthetic Route ◽  
Therapeutic Activities

: Coumarin, sulphonamide and amide scaffolds exhibit diverse pharmacological features and constitute an important class of therapeutic agents. In this review, we have discussed the synthesis, biological properties, and SAR of coumarins containing sulphonamide or amide group in the last seven years. Many reviews on the therapeutic activities of coumarins, sulphonamides, and amides have been published, hence the authors focused on coumarin-linked sulphonamide or amide scaffolds. The review provides information on the synthetic route to new coumarins containing sulphonamide or amide groups with improved pharmacological properties.

Bridging the Gap of Drug Delivery in Colon Cancer: The Role of Chitosan and Pectin Based Nanocarriers System

2020 ◽  
Vol 17 (10) ◽  
pp. 911-924
Author(s):  
Rohitas Deshmukh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Targeted Drug Delivery ◽  
Targeted Delivery ◽  
Therapeutic Agent ◽  
Therapeutic Agents ◽  
Delivery Systems ◽  
Target Tissue ◽  
Polymer Carriers

Colon cancer is one of the most prevalent diseases, and traditional chemotherapy has not been proven beneficial in its treatment. It ranks second in terms of mortality due to all cancers for all ages. Lack of selectivity and poor biodistribution are the biggest challenges in developing potential therapeutic agents for the treatment of colon cancer. Nanoparticles hold enormous prospects as an effective drug delivery system. The delivery systems employing the use of polymers, such as chitosan and pectin as carrier molecules, ensure the maximum absorption of the drug, reduce unwanted side effects and also offer protection to the therapeutic agent from quick clearance or degradation, thus allowing an increased amount of the drug to reach the target tissue or cells. In this systematic review of published literature, the author aimed to assess the role of chitosan and pectin as polymer-carriers in colon targeted delivery of drugs in colon cancer therapy. This review summarizes the various studies employing the use of chitosan and pectin in colon targeted drug delivery systems.

scholarly journals Combined Method to Remove Endotoxins from Protein Nanocages for Drug Delivery Applications: The Case of Human Ferritin

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 229
Author(s):  
Filippo Silva ◽  
Leopoldo Sitia ◽  
Raffaele Allevi ◽  
Arianna Bonizzi ◽  
Marta Sevieri ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Biological Fluids ◽  
Affinity Purification ◽  
Delivery Systems ◽  
Point Of View ◽  
Uniform Structure ◽  
Structure Stability ◽  
Target Cells ◽  
Clinical Phase ◽  
Main Challenge

Protein nanocages represent an emerging candidate among nanoscaled delivery systems. Indeed, they display unique features that proved to be very interesting from the nanotechnological point of view such as uniform structure, stability in biological fluids, suitability for surface modification to insert targeting moieties and loading with different drugs and dyes. However, one of the main concerns regards the production as recombinant proteins in E. coli, which leads to a product with high endotoxin contamination, resulting in nanocage immunogenicity and pyrogenicity. Indeed, a main challenge in the development of protein-based nanoparticles is finding effective procedures to remove endotoxins without affecting protein stability, since every intravenous injectable formulation that should be assessed in preclinical and clinical phase studies should display endotoxins concentration below the admitted limit of 5 EU/kg. Different strategies could be employed to achieve such a result, either by using affinity chromatography or detergents. However, these strategies are not applicable to protein nanocages as such and require implementations. Here we propose a combined protocol to remove bacterial endotoxins from nanocages of human H-ferritin, which is one of the most studied and most promising protein-based drug delivery systems. This protocol couples the affinity purification with the Endotrap HD resin to a treatment with Triton X-114. Exploiting this protocol, we were able to obtain excellent levels of purity maintaining good protein recovery rates, without affecting nanocage interactions with target cells. Indeed, binding assay and confocal microscopy experiments confirm that purified H-ferritin retains its capability to specifically recognize cancer cells. This procedure allowed to obtain injectable formulations, which is preliminary to move to a clinical trial.

scholarly journals Brain-specific inhibition of mTORC1 eliminates side effects resulting from mTORC1 blockade in the periphery and reduces alcohol intake in mice

2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Yann Ehinger ◽  
Ziyang Zhang ◽  
Khanhky Phamluong ◽  
Drishti Soneja ◽  
Kevan M. Shokat ◽  
...  
Keyword(s):  
Side Effects ◽  
Inhibitory Action ◽  
Alcohol Use Disorder ◽  
Alcohol Intake ◽  
Therapeutic Agents ◽  
Adverse Side Effects ◽  
Mtorc1 Activation ◽  
Potential Use ◽  
Heavy Alcohol Intake ◽  
Alcohol Dependent

AbstractAlcohol Use Disorder (AUD) affects a large portion of the population. Unfortunately, efficacious medications to treat the disease are limited. Studies in rodents suggest that mTORC1 plays a crucial role in mechanisms underlying phenotypes such as heavy alcohol intake, habit, and relapse. Thus, mTORC1 inhibitors, which are used in the clinic, are promising therapeutic agents to treat AUD. However, chronic inhibition of mTORC1 in the periphery produces undesirable side effects, which limit their potential use for the treatment of AUD. To overcome these limitations, we designed a binary drug strategy in which male mice were treated with the mTORC1 inhibitor RapaLink-1 together with a small molecule (RapaBlock) to protect mTORC1 activity in the periphery. We show that whereas RapaLink-1 administration blocked mTORC1 activation in the liver, RapaBlock abolished the inhibitory action of Rapalink-1. RapaBlock also prevented the adverse side effects produced by chronic inhibition of mTORC1. Importantly, co-administration of RapaLink-1 and RapaBlock inhibited alcohol-dependent mTORC1 activation in the nucleus accumbens and attenuated alcohol seeking and drinking.

Sign in / Sign up

Export Citation Format

Share Document