323,580 results match your criteria drug release


Rational design of synthetically tractable HDAC6/HSP90 dual inhibitors to destroy immune-suppressive tumor microenvironment.

J Adv Res 2022 Jun 22. Epub 2022 Jun 22.

School of Pharmacy, College of Pharmacy, Taipei Medical University, Taipei 110031, Taiwan; TMU Research Center of Drug Discovery, Taipei Medical University, Taipei 110031, Taiwan. Electronic address:

Introduction: The tumor microenvironment is mainly flooded with immunosuppressive cells and inhibitory cytokines, resulting in the inability of effective immune cells to infiltrate and recognize tumors and even the loss of anti-cancer ability.

Objectives: We propose a novel HDAC6/HSP90 dual inhibitory strategy as well as a chemoimmunotherapeutic agent that does not only kill tumor cells but also destroys the tumor microenvironment and enhances anti-cancer immunity.

Methods: A hybrid scaffold construction approach was leveraged to furnish a series of rationally designed resorcinol-based hydroxamates as dual selective HDAC6/HSP90 inhibitors. Read More

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Sustained drug delivery strategies for treatment of common substance use disorders: Promises and challenges.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Department of Pharmaceutical Sciences, Bill Gatton College of Pharmacy, East Tennessee State University, Johnson City, TN 37614, USA. Electronic address:

Substance use disorders (SUDs) are a leading cause of death and other ill health effects in the United States and other countries in the world. Several approaches ranging from detoxification, behavioral therapy, and the use of antagonists or drugs with counter effects are currently being applied for its management. Amongst these, drug therapy is the mainstay for some drug abuse incidence, as is in place specifically for opioid abuse or alcohol dependence. Read More

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Prebiotic-like cyclodextrin assisted silybin on NAFLD through restoring liver and gut homeostasis.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China. Electronic address:

Non-alcoholic fatty liver disease (NAFLD) is the most common chronic liver disease with no currently approved treatment. The natural compound silybin (SLN) has versatile hepatoprotective efficacy with negligible adverse effects; however, poor absorption limits its clinical applications. Gut microbiota has been proposed to play a crucial role in the pathophysiology of NAFLD and targeted for disease control. Read More

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Leveraging the therapeutic, biological, and self-assembling potential of peptides for the treatment of viral infections.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Department of Chemical and Biomolecular Engineering, The Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218, United States of America; Institute for NanoBioTechnology, The Johns Hopkins University, 3400 N Charles Street, Baltimore, MD 21218, United States of America; Deptartment of Oncology and Sidney Kimmel Comprehensive Cancer Center, The Johns Hopkins University School of Medicine, Baltimore, MD 21205, United States of America; Center for Nanomedicine, The Wilmer Eye Institute, The Johns Hopkins University School of Medicine, 400 North Broadway, Baltimore, MD 21231, United States of America. Electronic address:

Peptides and peptide-based materials have an increasing role in the treatment of viral infections through their use as active pharmaceutical ingredients, targeting moieties, excipients, carriers, or structural components in drug delivery systems. The discovery of peptide-based therapeutic compounds, coupled with the development of new stabilization and formulation strategies, has led to a resurgence of antiviral peptide therapeutics over the past two decades. The ability of peptides to bind cell receptors and to facilitate membrane penetration and subsequent intracellular trafficking enables their use in various antiviral systems for improved targeting efficiency and treatment efficacy. Read More

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35 years of discussions with Prof. Maeda on the EPR effect and future directions.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Former President of Japan Society of Drug Delivery System, 5-3-13, Otsuka, Bunkyo-ku, Tokyo, 112-0012, Japan, Visiting Scientist, Department of Immune Medicine, National Cancer Center Research Institute 5-1-1, Tsukiji, Chuo-ku, Tokyo 104-0045, Japan. Electronic address:

In May 2021, 35 years after first announcing the enhanced permeability and retention (EPR) effect, Dr. Maeda passed away. As a theoretical pillar of high molecular weight drug delivery systems (DDS) with high biocompatibility, the EPR effect has been proven worldwide in experimental mouse models. Read More

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Transitioning from a lab-scale PLGA microparticle formulation to pilot-scale manufacturing.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Purdue University, Departments of Biomedical Engineering and Pharmaceutics, West Lafayette, IN 47907, USA. Electronic address:

The complexity of scale-up manufacturing of PLGA microparticles creates a significant challenge when transitioning from benchtop-scale formulation development into larger clinical scale batches. Minor changes in the initial formulation composition (e.g. Read More

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3D printing of a controlled fluoride delivery device for the prevention and treatment of tooth decay.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Institute of Pharmaceutical Sciences, Department of Chemistry and Applied Biosciences, ETH Zurich, Vladimir-Prelog-Weg 3, 8093 Zurich, Switzerland. Electronic address:

Dental decay is a highly prevalent chronic disease affecting people from all ages. Clinically, fluoride supplementation is the primary strategy in the prevention of dental decay. However, the current existing self-application formulations such as gels or mouthwashes are rapidly cleared after administration, resulting in modest efficacy even after repeated applications. Read More

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Organic quantum dots: An ultrasmall nanoplatform for cancer theranostics.

J Control Release 2022 Jun 22. Epub 2022 Jun 22.

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKMs NMIMS, V. L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra 400056, India. Electronic address:

Tumours are the second leading cause of death globally, generating alterations in biological interactions and, as a result, malfunctioning of crucial genetic traits. Technological advancements have made it possible to identify tumours at the cellular level, making transcriptional gene variations and other genetic variables more easily investigated. Standard chemotherapy is seen as a non-specific treatment that has the potential to destroy healthy cells while also causing systemic toxicity in individuals. Read More

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pH-responsive Mannose-modified ferrocene Metal-Organic frameworks with rare earth for Tumor-targeted synchronous Chemo/Chemodynamic therapy.

Bioorg Med Chem 2022 Jun 14;69:116885. Epub 2022 Jun 14.

Shaanxi Key Laboratory of Natural Products and Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling 712100, China. Electronic address:

The combination of chemodynamic therapy (CDT) and chemotherapy is a promising strategy to achieve enhanced anticancer effects. Metal-organic frameworks (MOFs), as multifunctional drug delivery vehicles, have received extensive attention in the biomedical field. Carbohydrate has excellent biocompatibility and targeting ability, which can be used as a targeting ligand due to a specific recognition with glycoprotein receptors that overexpress on cancer cell membranes. Read More

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Multi-responsive mesoporous polydopamine composite nanorods cooperate with nano-enzyme and photosensitizer for intensive immunotherapy of bladder cancer.

Immunology 2022 Jun 25. Epub 2022 Jun 25.

Provincial Clinical Medical College of Fujian Medical University, Fuzhou, China.

Bladder cancer is a common malignancy in the urinary system. Defects of drug molecules in bladder during treatment, such as passive diffusion, rapid clearance of periodic urination, poor adhesion and permeation abilities, lead to low delivery efficiency of conventional drugs and high recurrence rate of disease. In this study, we designed multi-responsive mesoporous polydopamine (PDA) composite nanorods cooperating with nano-enzyme and photosensitizer for intensive immunotherapy of bladder cancer. Read More

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Luliconazole Nail Lacquer for the Treatment of Onychomycosis: Formulation, Characterization and In Vitro and Ex Vivo Evaluation.

AAPS PharmSciTech 2022 Jun 24;23(6):175. Epub 2022 Jun 24.

Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (BHU), Varanasi, 221005, India.

Onychomycosis is the most common fungal infection of the nail affecting the skin under the fingertips and the toes. Currently, available therapy for onychomycosis includes oral and topical therapies, either alone or in combination. Oral antifungal medication has been associated with poor drug bioavailability and potential gastrointestinal and systemic side effects. Read More

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Engineering 2D Silicene-Based Mesoporous Nanomedicine for In Vivo Near-Infrared-Triggered Analgesia.

Adv Sci (Weinh) 2022 Jun 24:e2202735. Epub 2022 Jun 24.

Department of Anesthesiology, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200127, P. R. China.

The utilization of local anesthetics for postoperative analgesia represents an effective approach, but generally suffers from short half-lives and brachychronic local neurotoxicity. A desirable anesthetic with controllable and sustainable drug-releasing performance for adequate analgesia effect is highly required. In this work, the core/shell-structured two-dimenional (2D) silicene nanosheets coated with mesoporous silica layer (abbreviated as [email protected]) have been rationally constructed as localized drug-delivery system in sciatic nerve block to achieve on-demand release of loaded ropivacaine (RP) in mesoporous silica layer for local analgesia. Read More

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In-Use Stability Assessment of FDA Approved Metformin Immediate Release and Extended Release Products for N-Nitrosodimethylamine and Dissolution Quality Attributes.

Int J Pharm 2022 Jun 21:121923. Epub 2022 Jun 21.

Irma Lerma Rangel College of Pharmacy, Texas A&M Health Science Center, Texas A&M University, College Station, TX 77843, USA. Electronic address:

Metformin is a widely used first-line oral antidiabetic agent. TheFood and Drug Administration (FDA) confirmed the presence of the ofN-nitrosodimethylamine (NDMA) impurity, a carcinogenic, above the acceptable daily intake (ADI, 96 ng/day) in certain metformin products. The objective of the present study was to assess in-use stability of commercial metformin products for NDMA and dissolution quality attributes. Read More

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An analytical quality by design approach towards a simple and novel HPLC-UV method for quantification of the antifibrotic peptide N-acetyl-seryl-aspartyl-lysyl-proline.

Anal Biochem 2022 Jun 21:114793. Epub 2022 Jun 21.

University College London School of Pharmacy, 29-39 Brunswick Square, London, WC1N 1AX, UK. Electronic address:

N-acetyl-seryl-aspartyl-lysyl proline (Ac-SDKP) is a tetrapeptide possessing anti-fibrotic, angiogenic, anti-inflammatory, anti-apoptotic, and immunomodulatory properties. Currently, the main method to quantify the peptide is liquid chromatography-tandem mass spectrometry (LC-MS/MS) and enzyme-linked immunosorbent assay (ELISA), both of which are labour intensive and require expensive equipment and consumables. Furthermore, these techniques are generally utilised to detect very low or trace concentrations, such as in biological samples. Read More

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Raddeanin A synergistically enhances the anti-tumor effect of MAP30 in multiple ways, more than promoting endosomal escape.

Toxicol Appl Pharmacol 2022 Jun 21:116139. Epub 2022 Jun 21.

Department of Applied Biology, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China; State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China. Electronic address:

Biomacromolecules such as proteins and nucleic acids are very attractive due to their high efficiency and specificity as cancer therapeutics. In fact, the endocytosed macromolecules are often trapped in the endosomes and cannot exhibit pharmacological effects well. Many strategies have been used to address this bottleneck, and one promising approach is to exploit the endosomal escape-promoting effect of triterpenoid saponins to aid in the release of biomacromolecules. Read More

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Vascular bursts-mediated tumor accumulation and deep penetration of spherical nucleic acids for synergistic radio-immunotherapy.

J Control Release 2022 Jun 21. Epub 2022 Jun 21.

Xiangya School of Pharmaceutical Sciences, Central South University, Changsha, Hunan 410013, China; Key Laboratory of Biological Nanotechnology of National Health Commission, Changsha 410008, Hunan, China. Electronic address:

While nanomedicines have attracted great interests for tumor therapy, their targeting and intra-tumoral penetrating efficiencies have been questioned. Here, we report a two-step low-dose radiotherapy (RT) strategy to realize significant accumulation and deep penetration of spherical nucleic acids (SNAs)-based nanomedicine for synergistic radio-immunotherapy. The first step RT was employed to recruit large amounts of macrophages into tumor. Read More

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Sustained delivery approaches to improving adaptive immune responses.

Adv Drug Deliv Rev 2022 Jun 21:114401. Epub 2022 Jun 21.

Department of Bioengineering, Stanford University, Stanford, 94305, USA; Department of Materials Science & Engineering, Stanford University, Stanford, 94305, USA; Department of Pediatrics (Endocrinology), Stanford University, Stanford, 94305, USA; ChEM-H Institute, Stanford University, Stanford CA 94305, USA; Woods Institute for the Environment, Stanford University, Stanford CA 94305, USA. Electronic address:

The immune system is one of the most important, complex biological networks regulating and protecting human health. Its precise modulation can prevent deadly infections and fight cancer. Accordingly, prophylactic vaccines and cancer immunotherapies are some of the most powerful technologies to protect against potential dangers through training of the immune system. Read More

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Bioreducible polyethylenimine core-shell nanostructures as efficient and non-toxic gene and drug delivery vectors.

Bioorg Med Chem 2022 Jun 17;69:116886. Epub 2022 Jun 17.

Department of Biomedical Science, Acharya Narendra Dev College, University of Delhi, Kalkaji, New Delhi 110019, India; Delhi School of Skill Enhancement & Entrepreneuship Development, Institute of Eminence, University of Delhi, Delhi-110007, India. Electronic address:

Low molecular weight branched polyethylenimine (LMW bPEIs 1.8 kDa) have received considerable attention for the fabrication of nucleic acid carriers due to their biocompatible and non-toxic nature. However, due to the inadequate nucleic acid complexation ability and transportation across the cell membrane, these show poor transfection efficacy, limiting their clinical applications. Read More

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Abuse Potential of Lemborexant, a Dual Orexin Receptor Antagonist, Compared With Zolpidem and Suvorexant in Recreational Sedative Users.

J Clin Psychopharmacol 2022 Jun 24. Epub 2022 Jun 24.

Eisai Inc, Nutley, NJ.

Background: Lemborexant (LEM) is a dual orexin receptor antagonist approved for the treatment of insomnia in adults in multiple countries including the the United States, Japan, Canada, Australia and several Asian countries.

Procedures: This was a randomized, single-dose, single-center, double-blind, active-control, 6-way crossover study to evaluate LEM abuse potential. The study assessed oral doses of LEM 10 mg (LEM10), 20 mg (LEM20), and 30 mg (LEM30) compared with placebo (PBO), zolpidem (ZOL) immediate release 30 mg, and suvorexant (SUV) 40 mg. Read More

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Drug Eluting Embolization Particles for Permanent Contraception.

ACS Biomater Sci Eng 2022 Jun 24. Epub 2022 Jun 24.

Department of Bioengineering, University of Washington, 3720 15th Avenue Northeast, Seattle, Washington 98105, United States.

Medical technology that blocks the fallopian tubes nonsurgically could increase access to permanent contraception and address current unmet needs in family planning. To achieve total occlusion of the fallopian tube via scar tissue formation, acute trauma to the tubal epithelium must first occur followed by a sustained and ultimately fibrotic inflammatory response. Here, we developed drug-eluting fiber-based microparticles that provide tunable dose and release of potent sclerosing agents. Read More

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pH/Thermal-Sensitive Nanoplatform Capable of On-Demand Specific Release to Potentiate Drug Delivery and Combinational Hyperthermia/Chemo/Chemodynamic Therapy.

ACS Appl Mater Interfaces 2022 Jun 24. Epub 2022 Jun 24.

Fujian Provincial Key Laboratory of Innovative Drug Target Research, School of Pharmaceutical Sciences, Xiamen University, Xiamen 361102, P. R. China.

Therapeutic platforms with spatiotemporal control were recently of considerable interest. However, the site-specific regulation of chemotherapeutics release remains an enormous challenge. Herein, a versatile nanoplatform capable of tumor-specific delivery and controlled drug release, coined as PDDFe, was constructed for elevating cancer theranostics. Read More

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Natural Polyphenols-Platinum Nanocomplexes Stimulate Immune System for Combination Cancer Therapy.

Nano Lett 2022 Jun 24. Epub 2022 Jun 24.

Zhejiang Key Laboratory of Smart BioMaterials and Center for Bionanoengineering, College of Chemical and Biological Engineering, Zhejiang University, Hangzhou 310027, China.

Nanocarriers have been employed extensively to enhance drug delivery efficacy and reduce the side effect. However, carrier materials for drug delivery have challenging aspects, including safety concerns, low drug content, complexity in preparation, and low reproducibility. Herein, we propose a facile, universal, and green preparation way to use natural polyphenols to build platinum nanocomplex with stable structure, proper size, and high Pt content. Read More

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Promoting gene transfection by ROS responsive silicon nanowire arrays.

J Mater Chem B 2022 Jun 24. Epub 2022 Jun 24.

Key Lab of Health Chemistry and Molecular Diagnosis of Suzhou, Department of polymer Science and Engineering, College of Chemistry, Chemical Engineering and Materials Science, Soochow University, Suzhou 215123, P. R. China.

The development of a fast and safe reactive oxygen species (ROS)-responsive vector is generally limited by the intracellular unstable ROS concentration, and a relatively long time is still needed for the complete intracellular release of drugs or genes induced by ROS. In this work, a gene transfection platform based on ROS-responsive silicon nanowire arrays (SN) is developed, to promote the gene transfection efficiency for several cell lines. Briefly, the surface of the ROS generating system, gold nanoparticle modified SN (SN-Au), is grafted with poly[(2-acryloyl)ethyl(-boronic acid benzyl)diethylammonium bromide] (B-PDEAEA), an oxidation-responsive charge-reversal cationic polymer. Read More

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Multifunctional Magnetic Nanoparticles for MRI-guided Co-delivery of Erlotinib and L-Asparaginase to Ovarian Cancer.

J Microencapsul 2022 Jun 24:1-31. Epub 2022 Jun 24.

Research Center for Pharmaceutical Nanotechnology, Tabriz University of Medical Sciences, Tabriz, Iran.

Aim(s): The use of magnetic nanoparticles (MNPs) in biomedical applications has been wildly opted due to their unique properties. The objective of this study was to evaluate the effects of aptamer-armed MNPs in ovarian cancer treatment and as T2 weighted MRI contrast agent.

Methods: Here, we designed MNPs loaded with erlotinib (ERL/SPION-Val-PEG) and conjugated them with anti-mucin16 (MUC16) aptamer to introduce new image-guided nanoparticles (NPs) for targeted drug delivery as well as non-invasive magnetic resonance imaging (MRI) contrast agents. Read More

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Controlled Bioactive Delivery Using Degradable Electroactive Polymers.

Biomacromolecules 2022 Jun 24. Epub 2022 Jun 24.

Department of Chemistry, Faculty of Science and Technology, Lancaster University, Bailrigg, Lancaster LA1 4YB, U.K.

Biomaterials capable of precisely controlling the delivery of agrochemicals/biologics/drugs/fragrances have significant markets in the agriscience/healthcare industries. Here, we report the development of degradable electroactive polymers and their application for the controlled delivery of a clinically relevant drug (the anti-inflammatory dexamethasone phosphate, DMP). Electroactive copolymers composed of blocks of polycaprolactone (PCL) and naturally occurring electroactive pyrrole oligomers (e. Read More

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Formulation Development and in-vitro Evaluation of Escitalopram Fast Dissolving Tablets.

Cent Nerv Syst Agents Med Chem 2022 Jun 24. Epub 2022 Jun 24.

Guru Gobind Singh College of Pharmacy, Yamuna Nagar-135001, Haryana, India.

Background: Escitalopram, a selective serotonin reuptake inhibitor (SSRI), acts by increasing the serotonin level in the brain and is used widely for the management of depression and anxiety disorders. However, the poor dissolution rate of escitalopram due to less water solubility is a consequential problem confronting the pharmaceutical industry in developing pharmaceutical dosage forms for oral delivery systems.

Objective: The present work aims to deliver a novel formulation for improving the dissolution profile and, thus, the bioavailability of escitalopram. Read More

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Biomass-derived isosorbide-based thermoresponsive hydrogel for drug delivery.

Soft Matter 2022 Jun 24. Epub 2022 Jun 24.

Departmento de Química Orgánica, Universidad de La Laguna, Avda. Astrofísico Francisco Sánchez 3, La Laguna 38206, Tenerife, Spain.

Herein, we describe the design and synthesis of a new variety of bio-based hydrogel films using a Cu(I)-catalyzed photo-click reaction. These films exhibited thermal-triggered swelling-deswelling and were constructed by crosslinking a triazide derivative of glycerol ethoxylate and dialkyne structures derived from isosorbide, a well-known plant-based platform molecule. The success of the click reaction was corroborated through infrared spectroscopy (FTIR) and the smooth surface of the obtained films was confirmed by scanning electron microscopy (SEM). Read More

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Block Co-PolyMOC Micelles and Structural Synergy as Composite Nanocarriers.

ACS Appl Mater Interfaces 2022 Jun 24. Epub 2022 Jun 24.

Department of Chemistry, The University of Hong Kong, Pokfulam Road, Hong Kong SAR 999077, China.

Conventional micelles of amphiphilic block copolymers (BCPs) disassemble into individual polymer chains upon dilution to a critical concentration, which causes the premature release of the encapsulated drugs and reduces the drug's bioavailability. Here, by integrating the emerging metal-organic cage (MOC) materials with BCPs, we introduce a new type of composite micellar nanoparticles, block co-polyMOC micelles (or BCPMMs), that are self-assembled in essence yet remarkably stable against dilution. BCPMMs are fabricated a stepwise assembly strategy that combines MOCs and BCPs in a well-defined, unimolecular core-shell structure. Read More

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Stimuli-responsive prodrug of non-steroidal anti-inflammatory drug diclofenac: self-immolative drug release with turn-on near-infrared fluorescence.

Chem Commun (Camb) 2022 Jun 24. Epub 2022 Jun 24.

Department of Chemistry, Indian Institute of Technology Guwahati, Guwahati-781039, Assam, India.

Reactive oxygen species (ROS)-responsive near infrared (NIR) fluorogenic prodrug DCI-ROS is developed for the self-immolative release of diclofenac (DCF) with turn-on fluorescence. The non-toxic prodrug exhibited turn-on red fluorescence with endogenous ROS in cancer cells and inhibited COX-2 expression in the inflammation-induced macrophage cells. The prodrug strategy thus would be helpful for the controlled fluorogenic delivery of DCF for inflammatory diseases. Read More

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Poly-β-Cyclodextrin-coated neodymium-containing copper sulfide nanoparticles as an effective anticancer drug carrier.

J Microencapsul 2022 Jun 24:1-26. Epub 2022 Jun 24.

Centre for Nanoscience and Genomics.

This study aims at tuning the properties of the nanoparticles by incorporating neodymium, exploring the sustained release of drug, and the anticancer activity on breast cancer cells. The crystal characteristics of NdCuS nanoparticles are analyzed using X-ray diffraction. The morphology and size of the nanoparticles were characterized using Transmission Electron Microscope and particle size analyzer. Read More

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