30,044 results match your criteria oral bioavailability

Rethinking Remdesivir: Synthesis, Antiviral Activity and Pharmacokinetics of Oral Lipid Prodrugs.

Antimicrob Agents Chemother 2021 Jul 26:AAC0115521. Epub 2021 Jul 26.

Division of Infectious Diseases and Global Public Health, Departments of Medicine and Pediatrics; University of California San Diego, School of Medicine, 9500 Gilman Drive, La Jolla, CA 92093-0676, USA.

Remdesivir (RDV, GS-5734) is currently the only FDA-approved antiviral drug for the treatment of SARS CoV-2 infection. The drug is approved for use in adults or children 12-years or older who are hospitalized for the treatment of COVID-19 on the basis of an acceleration of clinical recovery for inpatients with this disease. Unfortunately, the drug must be administered intravenously, restricting its use to those requiring hospitalization for relatively advanced disease. Read More

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A Novel Nanomedicine Ameliorates Acute Inflammatory Bowel Disease by Regulating Macrophages and T-Cells.

Mol Pharm 2021 Jul 26. Epub 2021 Jul 26.

Institute of Traditional Chinese Veterinary Medicine, College of Veterinary Medicine, Nanjing Agricultural University, Nanjing 210095, P. R. China.

polysaccharide (RMP), one of the most important active components of , has been attracting increasing interest because of its potent bioactive properties, including anti-inflammatory, antitumor, and antidiabetic effects. Despite the great therapeutic potential of RMP, its inherent properties of low bioavailability and brief biological half-life have limited its applications to the clinic. Thus, RMP was packaged by poly(lactic--glycolic acid) (PLGA) nanoparticles to develop a novel anti-inflammatory nanomedicine (PLGA-RMP) in this study. Read More

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Antitumor efficacy of CHMFL-KIT-110 solid dispersion in mouse xenograft models of human gastrointestinal stromal tumors.

Cancer Chemother Pharmacol 2021 Jul 26. Epub 2021 Jul 26.

Institute of Clinical Pharmacology, Anhui Medical University, 81 Meishan Road, Hefei, 230032, China.

Purpose: CHMFL-KIT-110, a selective c-KIT kinase inhibitor for gastrointestinal stromal tumors (GISTs), possesses a poorly water-soluble, limiting the further development of the drug. This study was to investigate the antitumor efficacy of CHMFL-KIT-110 and CHMFL-KIT-110 solid dispersion (laboratory code: HYGT-110 SD) in GIST tumor xenograft models and to explore the PK/PD relationship of HYGT-110 SD.

Methods: Plasma concentrations of HYGT-110 and HYGT-110 SD were determined by LC-MS/MS in KM mice. Read More

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Study on the bioaccessibility and bioavailability of Cd in contaminated rice in vitro and in vivo.

J Food Sci 2021 Jul 26. Epub 2021 Jul 26.

Key Laboratory for Deep Processing of Major Grain and Oil of Ministry of Education, Wuhan Polytechnic University, Wuhan, Hubei, China.

Cadmium (Cd) is a widespread heavy metal pollutant in the environment that damages human health. In this study, the bioaccessibility and bioavailability of Cd in different Cd-contaminated rice (low pollution level cadmium rice (Rice-L, 0.111 mg/kg), medium pollution level cadmium rice (Rice-M, 0. Read More

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Orally Administrable Therapeutic Nanoparticles for the Treatment of Colorectal Cancer.

Front Bioeng Biotechnol 2021 7;9:670124. Epub 2021 Jul 7.

The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.

Colorectal cancer (CRC) is one of the most common and lethal human malignancies worldwide; however, the therapeutic outcomes in the clinic still are unsatisfactory due to the lack of effective and safe therapeutic regimens. Orally administrable and CRC-targetable drug delivery is an attractive approach for CRC therapy as it improves the efficacy by local drug delivery and reduces systemic toxicity. Currently, chemotherapy remains the mainstay modality for CRC therapy; however, most of chemo drugs have low water solubility and are unstable in the gastrointestinal tract (GIT), poor intestinal permeability, and are susceptible to P-glycoprotein (P-gp) efflux, resulting in limited therapeutic outcomes. Read More

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Starch Nanoparticles for Enhancement of Oral Bioavailability of a Newly Synthesized Thienopyrimidine Derivative with Anti-Proliferative Activity Against Pancreatic Cancer.

Drug Des Devel Ther 2021 16;15:3071-3093. Epub 2021 Jul 16.

Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt.

Purpose: This research aimed to improve water solubility and oral bioavailability of a newly synthesized thienopyrimidine derivative (TPD) with anti-pancreatic cancer activity by loading on starch nanoparticles (SNPs).

Methods: TPD was synthesized, purified and its ADME behavior was predicted using Swiss ADME software. A UV spectroscopy method was developed and validated to measure TPD concentration at various dosage forms. Read More

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Development & validation of LC-MS/MS assay for 5-amino-1-methyl quinolinium in rat plasma: Application to pharmacokinetic and oral bioavailability studies.

J Pharm Biomed Anal 2021 Jul 8;204:114255. Epub 2021 Jul 8.

Department of Pharmaceutical Sciences, Texas Southern University, Houston, TX, 77004, United States. Electronic address:

5-Amino-1-methyl quinolinium (5-AMQ) is a potent Nicotinamide N-methyl transferase (NNMT) inhibitor. NNMT is an enzyme that catalyzes the N-methylation of the endogenous substrate nicotinamide, as well as exogenous xenobiotics. NNMT is fundamental to cellular metabolism; NNMT is overexpressed in select tissues (e. Read More

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Design and synthesis of novel orally selective and type II pan-TRK inhibitors to overcome mutations by property-driven optimization.

Eur J Med Chem 2021 Jun 29;224:113673. Epub 2021 Jun 29.

Institute of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County, 350401, Taiwan, ROC; Department of Chemistry, National Tsing Hua University, No. 101, Sec. 2, Kuang-Fu Road, Hsinchu, 300044, Taiwan, ROC; Biomedical Translation Research Center, Academia Sinica, No. 99, Ln. 130, Sec. 1, Academia Road, Taipei City, 115202, Taiwan, ROC. Electronic address:

Rare oncogenic NTRK gene fusions result in uncontrolled TRK signaling leading to various adult and pediatric solid tumors. Based on the architecture of our multi-targeted clinical candidate BPR1K871 (10), we designed and synthesized a series of quinazoline compounds as selective and orally bioavailable type II TRK inhibitors. Property-driven and lead optimization strategies informed by structure-activity relationship studies led to the identification of 39, which showed higher (about 15-fold) selectivity for TRKA over AURA and AURB, as well as potent cellular activity (IC = 56. Read More

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pH-sensitive polymer-based carriers as a useful approach for oral delivery of therapeutic protein: A review.

Protein Pept Lett 2021 Jul 20. Epub 2021 Jul 20.

Department of Pharmaceutics, Faculty of Pharmacy, Kerman University of Medical Sciences, Kerman, Iran.

There are many proteins and enzymes in the human body, and their dysfunction can lead to disease. The use of proteins as a drug is common in various diseases such as diabetes. Proteins are hydrophilic molecules whose spatial structure is critical to their correct function. Read More

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Oral epigallocatechin gallate reduces intestinal nadolol absorption via modulation of Oatp1a5 and Oct1 transcriptional levels in spontaneously hypertensive rats.

Phytomedicine 2021 Jun 11;90:153623. Epub 2021 Jun 11.

Faculty of Medicine and Health Sciences, Universiti Tunku Abdul Rahman, 43000 Kajang, Bandar Sungai Long, Selangor, Malaysia. Electronic address:

Background: Concurrent use of epigallocatechin-3-gallate (EGCG) and medication may lead to botanical-drug interactions, subsequently therapeutic failure or drug toxicity. It has been reported that EGCG reduces plasma nadolol bioavailability in normotensive models. Nevertheless, evidence on the effects of EGCG on hypertensive model, and the possible underlying mechanism have not been elucidated. Read More

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Electrosprayed Chitosan Coated Alginate-Pectin Beads as Potential System for Colon- Targeted Delivery of Ellagic Acid.

J Sci Food Agric 2021 Jul 24. Epub 2021 Jul 24.

Food Engineering Department, Chemical, and Metallurgical Engineering Faculty, Yildiz Technical University, Istanbul, Turkey.

Background: Ellagic acid (EA), a potent dietary antioxidant, has limited bioavailability due to its rapid absorption in the stomach and small intestine, and EA is transformed to more bioavailable compounds, urolithins, in the colon. An encapsulation system that sustain the release of EA in the gastrointestinal system and deliver more EA into the colon could improve the oral bioavailability of EA. Electrosprayed EA-loaded alginate-pectin beads were produced and coated with low (LC) and high molecular weight chitosan (HC). Read More

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Lyophilized Composite Loaded with Meloxicam-Peppermint oil Nanoemulsion for Periodontal Pain.

Polymers (Basel) 2021 Jul 14;13(14). Epub 2021 Jul 14.

Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia.

Maintaining oral health helps to prevent periodontal inflammation and pain, which can progress into more detrimental issues if left untreated. Meloxicam (MX) is a commonly used analgesic for periodontal pain, but it can have adverse gastrointestinal effects and poor solubility. Therefore, this study aimed to enhance the solubility of MX by developing a self-nanoemulsifying drug delivery system (SNEDDS). Read More

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Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments.

Polymers (Basel) 2021 Jul 11;13(14). Epub 2021 Jul 11.

Institut des Sciences Analytiques et de Physico-Chimie pour l'Environnement et les Matériaux, University Pau & Pays Adour, 64000 Pau, France.

Olmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs) was developed and evaluated for cytotoxicity against the A549 lung cell lines and antihypertensive potential in a rat model. Four OLM-loaded NSs (ONS1-ONS4) were prepared and fully evaluated in terms of physicochemical properties. Read More

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Naturally Occurring Polyelectrolytes and Their Use for the Development of Complex-Based Mucoadhesive Drug Delivery Systems: An Overview.

Polymers (Basel) 2021 Jul 8;13(14). Epub 2021 Jul 8.

Departamento de Farmacia Galénica y Tecnología Alimentaria, Facultad de Farmacia, Universidad Complutense de Madrid, 28040 Madrid, Spain.

Biopolymers have several advantages for the development of drug delivery systems, since they are biocompatible, biodegradable and easy to obtain from renewable resources. However, their most notable advantage may be their ability to adhere to biological tissues. Many of these biopolymers have ionized forms, known as polyelectrolytes. Read More

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An Innovative Strategy for Oral Biofilm Control in Early Childhood Based on a Resveratrol-Cyclodextrin Nanotechnology Approach.

Materials (Basel) 2021 Jul 7;14(14). Epub 2021 Jul 7.

Department of Surgical Sciences, C.I.R. Dental School, University of Turin, 10126 Turin, Italy.

The purpose of this randomized controlled study was to evaluate the clinical efficacy of a novel oral spray containing resveratrol (RV) in controlling bacterial biofilm and gingival inflammation in early childhood. RV, a natural polyphenol, known for its anti-inflammatory and anti-infective activities, was included in a nanovector of 2-hydroxypropyl-beta-cyclodextrins (HPβCD) to improve its bioavailability. A total of 64 children between two and five years of age with plaque-induced gingivitis were randomly included in two equal groups. Read More

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Oxyresveratrol: Sources, Productions, Biological Activities, Pharmacokinetics, and Delivery Systems.

Molecules 2021 Jul 11;26(14). Epub 2021 Jul 11.

Department of Pharmacognosy and Pharmaceutical Botany, Faculty of Pharmaceutical Sciences, Chulalongkorn University, Bangkok 10330, Thailand.

Oxyresveratrol has recently attracted much research attention due to its simple chemical structure and diverse therapeutic potentials. Previous reviews describe the chemistry and biological activities of this phytoalexin, but additional coverage and greater accessibility are still needed. The current review provides a more comprehensive summary, covering research from 1955 to the present year. Read More

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The Effect of Liposomal Curcumin as an Anti-Inflammatory Strategy on Lipopolysaccharide e from Treated Endothelial Committed Neural Crest Derived Stem Cells: Morphological and Molecular Mechanisms.

Int J Mol Sci 2021 Jul 14;22(14). Epub 2021 Jul 14.

"Ss. Annunziata" Hospital, ASL 02 Lanciano-Vasto-Chieti, 66100 Chieti, Italy.

Curcumin, a yellow polyphenol extracted from the turmeric root is used as a diet supplement. It exhibits anti-inflammatory, antioxidant, and antitumor properties by modulating different intracellular mechanisms. Due to their low solubility in water, the curcumin molecules must be encapsulated into liposomes to improve the bioavailability and biomedical potential. Read More

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Identification of Dihydromyricetin and Metabolites in Serum and Brain Associated with Acute Anti-Ethanol Intoxicating Effects in Mice.

Int J Mol Sci 2021 Jul 12;22(14). Epub 2021 Jul 12.

Department of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers University, Piscataway, NJ 08854, USA.

Dihydromyricetin is a natural bioactive flavonoid with unique GABA receptor activity with a putative mechanism of action to reduce the intoxication effects of ethanol. Although dihydromyricetin's poor oral bioavailability limits clinical utility, the promise of this mechanism for the treatment of alcohol use disorder warrants further investigation into its specificity and druggable potential. These experiments investigated the bioavailability of dihydromyricetin in the brain and serum associated with acute anti-intoxicating effects in C57BL/6J mice. Read More

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Physicochemical Characterization and Biopharmaceutical Evaluation of ZWF: A Novel Anticancer Drug for the Treatment of Non-small Cell Lung Cancer.

AAPS PharmSciTech 2021 Jul 23;22(6):207. Epub 2021 Jul 23.

Key Laboratory of Drug-Targeting and Drug Delivery Systems of the Education Ministry, Sichuan Engineering Laboratory for Plant-Sourced Drug and Sichuan Research Center for Drug Precision Industrial Technology, West China School of Pharmacy, Sichuan University, Chengdu, 610041, People's Republic of China.

The orally available novel small molecule drug ZWF is under preclinical development for an anticancer purpose. The present study aimed to assess the viability of developing ZWF as a form of oral formulation for clinical application based on the principles of biopharmaceutics and pharmacokinetics. The crucial physicochemical properties of ZWF were determined by in vitro assays. Read More

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An integrated approach to uncover anti-tumor active materials of Curcumae Rhizoma-Sparganii Rhizoma based on spectrum-effect relationship, molecular docking, and ADME evaluation.

J Ethnopharmacol 2021 Jul 19;280:114439. Epub 2021 Jul 19.

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing, 102488, China; Beijing Key Laboratory for Quality Evaluation of Chinese Materia Medica, Beijing University of Chinese Medicine, Fangshan District, Beijing, 102488, China. Electronic address:

Ethnopharmacological Relevance: Curcumae Rhizoma-Sparganii Rhizoma (CR-SR), an ancient and classical herbal couple, has been extensively used for tumor treatment in clinic of traditional Chinese medicines (TCMs).

Aim Of The Study: The study aimed to uncover the anti-tumor active materials of CR-SR water decoction (CR:SR = 1:1) via an integrated approach of spectrum-effect relationship, molecular docking, and ADME evaluation.

Materials And Methods: The anti-tumor activities toward A549, HepG2, Hela, BGC-823, and MCF-7 cells of the different polar elution fractions (DPEFs) of CR, SR, and CR-SR were determined by Cell Counting Kit-8 (CCK-8) assay. Read More

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Pharmacokinetic variables of medium molecular weight cross linked chitosan nanoparticles to enhance the bioavailability of 5-fluorouracil and reduce the acute oral toxicity.

Drug Deliv 2021 Dec;28(1):1569-1584

Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan.

To prepare glutaraldehyde-based cross-linked medium molecular weight chitosan nanoparticles encapsulated with 5-Fluorouracil (5-FU), to overcome dosing frequency as well as reducing acute oral toxicity and poor bioavailability of the drug. Medium molecular weight chitosan nanoparticles (MMWCH-NPs) were prepared by reverse micelles method based on glutaraldehyde (GA) cross-linking and optimized by the process as well as formulation variables like a various drug to polymer ratio, cross-linker volumes, varying stirring speeds (rpm), different time of rotation/stirring, respectively and their effects on the mean particles size distribution and entrapment efficiency %EE and %LC of NPs. Characterization of formulations was done by FTIR studies, TEM, PXRD, TGA, Stability, and dissolution drug release studies were performed by dialysis bag technique at both pH (1. Read More

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December 2021

Development of EQ-6, a Novel Analogue of Ethoxyquin to Prevent Chemotherapy-Induced Peripheral Neuropathy.

Neurotherapeutics 2021 Jul 21. Epub 2021 Jul 21.

School of Medicine, Johns Hopkins University, 855 N. Wolfe St., Suite 248, Baltimore, MD, 21205, USA.

Chemotherapy-induced peripheral neuropathy (CIPN) is a common and often dose-limiting side effect of many cancer drugs. Because the onset of neuronal injury is known, it is an ideal clinical target to develop neuroprotective strategies. Several years ago, we had identified ethoxyquin as a potent neuroprotective drug against CIPN through a phenotypic drug screening and demonstrated a novel mechanism of action, inhibition of chaperone domain of heat shock protein 90. Read More

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Pharmacokinetics and Biologic Activity of Apixaban in Healthy Dogs.

Front Vet Sci 2021 5;8:702821. Epub 2021 Jul 5.

Department of Clinical Sciences, Cornell University College of Veterinary Medicine, Ithaca, NY, United States.

Thrombosis is common in critically ill dogs and causes considerable morbidity and mortality. The direct factor Xa inhibitor apixaban is safe, efficacious, and convenient in humans. This study aimed to determine the pharmacokinetics (PK), bioactivity, protein binding, and bioavailability of apixaban following intravenous (IV) and oral (PO) administration to healthy dogs. Read More

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Strategies to improve insulin delivery through oral route: A review.

Curr Drug Deliv 2021 Jul 20. Epub 2021 Jul 20.

Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education and Research, Sri Shivarathreshwara Nagara, Bannimantap, Mysuru- 570015, Karnataka, India.

Diabetes mellitus is found to be among the most suffered and lethal diseases for mankind. Diabetes mellitus type-1 is caused by the demolition of pancreatic islets responsible for the secretion of insulin. Insulin is the peptide hormone (anabolic] that regulates the metabolism of carbohydrates, fats, and proteins. Read More

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Phase 1 Study Evaluating the Effects of the Proton Pump Inhibitor Rabeprazole and Food on the Pharmacokinetics of Lorlatinib in Healthy Participants.

Clin Pharmacol Drug Dev 2021 Jul 20. Epub 2021 Jul 20.

Pfizer Inc., La Jolla, California, USA.

Lorlatinib is approved worldwide as treatment for anaplastic lymphoma kinase-positive and c-ros oncogene 1-positive non-small cell lung cancer. The objectives of this phase 1, open-label crossover study (NCT02569554) in healthy adult participants were to determine (1) the effects of the proton pump inhibitor (PPI) rabeprazole on lorlatinib pharmacokinetics (PK), (2) the effects of a high-fat meal on lorlatinib PK, and (3) the relative bioavailability of an oral solution to tablet formulation of lorlatinib under fasted conditions. Participants were followed on-study for ≥50 days after the first dose of lorlatinib. Read More

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Bioavailability of a Capsaicin Lipid Multi-particulate Formulation in Rats.

Eur J Drug Metab Pharmacokinet 2021 Jul 21. Epub 2021 Jul 21.

Lonza Consumer Health Inc., Morristown, NJ, USA.

Background And Objective: Because of the stomach-burning sensation it induces, capsaicin has been used at relatively low doses as a nutritional supplement, which has limited its bioavailability. The objective of this study was to investigate the serum bioavailability of capsaicin supplementation with or without a lipid multi-particulate (LMP) formulation.

Methods: Thirty-five rats were divided into five groups and administered capsaicin at either 0. Read More

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The Challenging Pharmacokinetics of Mitotane: An Old Drug in Need of New Packaging.

Eur J Drug Metab Pharmacokinet 2021 Jul 21. Epub 2021 Jul 21.

Functional Polymer Materials, Chair for Chemical Technology of Material Synthesis, Institute for Functional Materials and Biofabrication, Faculty of Chemistry and Pharmacy, University of Würzburg, Röntgenring 11, 97070, Würzburg, Germany.

Adrenocortical carcinoma (ACC) is a malignant tumor originating from the adrenal gland cortex with a heterogeneous but overall dismal prognosis in advanced stages. For more than 50 years, mitotane has remained a cornerstone for the treatment of ACC as adjuvant and palliative therapy. It has a very poor aqueous solubility of 0. Read More

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Enhancement of bioavailability through transdermal drug delivery of paliperidone palmitate-loaded nanostructured lipid carriers.

Ther Deliv 2021 Aug 21;12(8):583-596. Epub 2021 Jul 21.

Faculty of Pharmacy, The Maharaja Sayajirao University of Baroda, Vadodara, Gujarat, 390001, India.

The work describes enhanced bioavailability of paliperidone palmitate through transdermal delivery using nanostructured lipid carriers (NLC). NLCs were formulated by nanoprecipitation method followed by incorporation in transdermal patch and physicochemical characterization. NLCs showed high percentage entrapment efficiency of 83. Read More

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A Pharmacokinetic Evaluation of a Pectin-Based Oral Multiparticulate Matrix Carrier of Carbamazepine.

Adv Pharmacol Pharm Sci 2021 3;2021:5527452. Epub 2021 Jul 3.

Department of Pharmaceutics and Microbiology, School of Pharmacy, University of Ghana, Accra, Ghana.

Background: Carbamazepine is a drug used in the treatment of neurological disorders such as epilepsy. However, due to its erratic absorption, oral bioavailability is often poor. There is, therefore, the need to develop alternative formulations for carbamazepine with better pharmacokinetic characteristics. Read More

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Concomitant oral intake of purified clinoptilolite tuff (G-PUR) reduces enteral lead uptake in healthy humans.

Sci Rep 2021 Jul 20;11(1):14796. Epub 2021 Jul 20.

Department of Clinical Pharmacology, Medical University of Vienna, Währinger Gürtel 18-20, 1090, Vienna, Austria.

Lead exposure can cause substantial organ damage. Enteral lead absorption may be reduced by concomitant intake of clinoptilolite tuff, a zeolite from natural sources. This study aimed to assess the effect of purified clinoptilolite tuff (G-PUR) on enteral lead uptake in adults using stable lead isotope Pb as a tracer. Read More

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