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Topic Review
Copper Chelators and cDDP Resistance
The platinum (Pt)-containing antitumor drugs including cisplatin (cis-diamminedichloroplatinum II, cDDP), carboplatin, and oxaliplatin, have been the mainstay of cancer chemotherapy. These drugs are effective in treating many human malignancies. The major cell-killing target of Pt drugs is DNA. Recent findings underscored the important roles of Pt drug transport system in cancer therapy. It was demonstrated that by reducing cellular Cu bioavailable levels by Cu chelators, hCtr1 is transcriptionally upregulated by transcription factor Sp1, which binds the promoters of Sp1 and hCtr1. In contrast, elevated Cu poisons Sp1, resulting in suppression of hCtr1 and Sp1, constituting the Cu-Sp1-hCtr1 mutually regulatory loop.
  • 479
  • 21 Jun 2021
Topic Review
Conventional Liposomal Formulation Methods
Liposome-based drug delivery systems are nanosized spherical lipid bilayer carriers that can encapsulate a broad range of small drug molecules (hydrophilic and hydrophobic drugs) and large drug molecules (peptides, proteins, and nucleic acids). They have unique characteristics, such as a self-assembling bilayer vesicular structure. There are various methods used in the preparation of lipid-based nanocarriers such as liposomes. The method of preparation affects critical parameters such as size of vesicle and size distribution, permeability, lamellarity, and entrapment efficiency. Entrapment of compounds is performed by two main techniques; passive loading where drug entrapment occurs during the liposome formation, and active loading where drug entrapment is after the liposome formation.
  • 1.8K
  • 15 May 2023
Topic Review
Contemporary Antiretroviral Drugs
Contemporary antiretroviral agents afford enhanced potency and safety for patients living with HIV. Newer antiretroviral drugs are often better tolerated than those initially approved in the early stages of the HIV epidemic. While the safety profile has improved, adverse drug reactions still occur. We have segregated the antiretroviral agents used in contemporary practice into class groupings based on their mechanism of antiviral activity (non-nucleoside reverse transcriptase inhibitors, nucleoside reverse transcriptase inhibitors, integrase inhibitors, protease inhibitors, and entry inhibitors) while providing a review and discussion of the hepatoxicity seen in the most relevant clinical literature published to date. Clinical literature for individual agents is discussed and agent comparisons afforded within each group in tabular format.
  • 430
  • 25 May 2021
Topic Review
Computational Methods in Drug Screening and Design
Drug development is one of the most significant processes in the pharmaceutical industry. Various computational methods have dramatically reduced the time and cost of drug discovery. 
  • 658
  • 18 Nov 2021
Topic Review
Composition of Lipid–Polymer Hybrid Nanoparticles
Lipid nanoparticles (LNPs) are spherical vesicles composed of ionizable lipids that are neutral at physiological pH. Despite their benefits, unmodified LNP drug delivery systems have substantial drawbacks, including a lack of targeted selectivity, a short blood circulation period, and in vivo instability. lipid–polymer hybrid nanoparticles (LPHNPs) are the next generation of nanoparticles, having the combined benefits of polymeric nanoparticles and liposomes. LPHNPs are being prepared from both natural and synthetic polymers with various techniques, including one- or two-step methods, emulsification solvent evaporation (ESE) method, and the nanoprecipitation method. Varieties of LPHNPs, including monolithic hybrid nanoparticles, core–shell nanoparticles, hollow core–shell nanoparticles, biomimetic lipid–polymer hybrid nanoparticles, and polymer-caged liposomes, have been investigated for various drug delivery applications.
  • 749
  • 08 Sep 2023
Topic Review
Complex Pharmacological Properties of Non-Selective Opioid Modulator Buprenorphine
Buprenorphine has high affinity for the mu-opioid receptor (MOR), delta (DOR), and kappa (KOR) and intermediate affinity for the nociceptin (NOR). Buprenorphine’s active metabolite, norbuprenorphine, crosses the blood–brain barrier, is a potent metabolite that attenuates the analgesic effects of buprenorphine due to binding to NOR, and is responsible for the respiratory depressant effects. The area under the concentration curves are very similar for buprenorphine and norbuprenorphine, which indicates that it is important to consider this metabolite. 
  • 282
  • 07 Nov 2023
Topic Review
Combination Therapy for Glioblastoma
Aggressive glioblastoma (GBM) has no known treatment as a primary brain tumor. Since the cancer is so heterogeneous, an immunosuppressive tumor microenvironment (TME) exists, and the blood–brain barrier (BBB) prevents chemotherapeutic chemicals from reaching the central nervous system (CNS), therapeutic success for GBM has been restricted. Drug delivery based on nanocarriers and nanotechnology has the potential to be a handy tool in the continuing effort to combat the challenges of treating GBM. Combination therapies may be enhanced by using nanotechnology-based delivery techniques. Nano-chemotherapy, nano-chemotherapy–radiation, nano-chemotherapy–phototherapy, and nano-chemotherapy–immunotherapy for GBM.
  • 611
  • 02 Nov 2022
Topic Review
Combination Therapies in Alzheimer’s Disease
Alzheimer’s disease (AD) is the leading cause of dementia worldwide. Until now, available therapeutic agents for AD treatment only provide symptomatic treatment. Since AD pathogenesis is multifactorial, use of a multimodal therapeutic intervention addressing several molecular targets of AD-related pathological processes seems to be the most practical approach to modify the course of AD progression. It has been demonstrated through numerous studies, that the clinical efficacy of combination therapy (CT) is higher than that of monotherapy. It is indeed difficult to combine several pharmacophores into a single molecule.  It is essential to carry out long-duration randomized controlled trials to establish whether CT delays disease progression in early AD stages. Other factors also need to be assessed in CT, such as its potential neuroprotective effects, cost-effectiveness, and a more exhaustive estimation of its potential benefits on the patients at the end-stage of AD.
  • 808
  • 28 Oct 2020
Topic Review
Colloidal Systems
Preparing a suitable formulation for parenteral administration is already a difficult task; this, coupled with poor water-soluble new chemical entity (NCE), complicates this situation even further. Making a micro/nano emulsion with a suitable surfactant not only increases the drug solubility but also the cell membrane permeability. This succinct entry delves into various aspects of biphasic micro/nano emulsion systems for parenteral drug delivery including the structure of the biphasic colloidal systems, characterization parameters, stability issues, regulatory considerations, and applications in life sciences.
  • 986
  • 20 Feb 2021
Topic Review
Cobalt–Chromium Dental Alloys
Co–Cr dental alloys consist of Co, Cr and also other metals (e.g., gallium, iron, molybdenum, nickel, ruthenium, tungsten). Since the 1990s, regulations have emerged to protect European patients and also monitor recent scientific knowledge. The use of metals and, therefore, dental alloys has been highly regulated by directives and regulations. Europe has, therefore, developed a regulatory package to protect all players involved in alloys, whether they are metal producers, manufacturers of alloys and medical devices, healthcare professionals and patients. Objective information is provided about Co–Cr dental alloys, with regard to both the latest toxicological data and regulatory developments from 2020–2025. The release of metal ions and the problem of wear particles are also discussed. With the recent change of regulatory status of Co, it is necessary to know the many repercussions (economic, technical etc.) of their use precisely in order to then allow actors to modify their daily work. The legislative changes also bring the need to propose new alternatives to Co-Cr dental alloys.  
  • 1.0K
  • 21 Jan 2021
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