Compound 1 [3,3-bis(4-pyridylmethyl)-1-phenylindolin-2-one] is an experimental cognition-enhancing drug now being developed for cognitive disorders. Oral bioavailability of 1 in rats was less than 10% of the dose. Nasal dosing improved bioavailability to greater than 50%. Brain levels of total radioactivity were measured after iv and nasal doses of radiolabeled 1. The ratio of AUCbrain:AUCplasma was the same by both routes, so nasal dosing did not enhance brain delivery. This is in contrast to other reports of large molecular weight substances and metals gaining direct access to the brain through the nasal epithelium.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1002/jps.2600790904 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Nephrotoxic effect of cypermethrin ameliorated by nanocurcumin through antioxidative mechanism.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Department of Pharmacology and Toxicology, College of Pharmacy, Jazan University, 45142, Jazan, Saudi Arabia.
Cypermethrin is a pyrethroid showing nephrotoxicity by generating ROS-impaired oxidative stress and changes in inflammatory and apoptotic markers. The harmful consequences are intended to be mitigated by the imbalance between oxidants and antioxidants. The anti-inflammatory and antioxidant possessions of nanocurcumin (NC) with improved bioavailability ameliorate Cyp toxicity in rat kidneys.
View Article and Find Full Text PDFEvaluation of the Effect of Virgin Rice Bran Oil (VRBO) on DoxorubicinInduced Cardiotoxicity in Wistar Rats.
Curr Cardiol Rev
January 2025
Department of Nutrition, Société Francophone de Nutrithérapie et de Nutrigénétique Appliquée, Villeurbanne, France.
Objective: The usage of doxorubicin (DOX), an antineoplastic drug that is frequently used for the cure of cancer, is restricted to maximal doses due to its cardiac toxicity. Reactive oxygen species produced by DOX result in lipid peroxidation and organ failure, ultimately resulting in cardiomyopathy. Due to its high polyphenol content, virgin rice bran oil (VRBO) is a diet nutritional supplement with a strong antioxidant.
View Article and Find Full Text PDFPreparation and characterization of tildipirosin-loaded solid lipid nanoparticles for the treatment of intracellular infections.
Biomater Sci
January 2025
School of Chemistry, Chemical Engineering and Life Science, Hubei Key Laboratory of Nanomedicine for Neurodegenerative Diseases, Wuhan University of Technology, 122 Luoshi Road, Wuhan 430070, China.
To enhance the antibacterial efficacy of tildipirosin against (S.A.) infections, optimized solid lipid nanoparticles loaded with tildipirosin (SLN-TD) were developed, using docosanoic acid (DA), octadecanoic acid (OA), hexadecanoic acid (HA), and tetradecanoic acid (TA) as lipid components.
View Article and Find Full Text PDFDevelopment and optimization of raloxifene hydrochloride loaded lipid nanocapsule based hydrogel for transdermal delivery.
Ther Deliv
January 2025
Institute of Pharmaceutical Research, GLA University, Mathura, India.
Aim: Development and optimization of raloxifene hydrochloride loaded lipid nanocapsule hydrogel for transdermal delivery.
Method: A 3 Box-Behnken Design and numerical optimization was performed to obtain the optimized formulation. Subsequently, the optimized raloxifene hydrochloride loaded lipid nanocapsule was developed using phase inversion temperature and characterized for physicochemical properties.
A focus on chasing pharmaceutical polymorphs to design better oral drug formulations.
Chem Sci
January 2025
Yusuf Hamied Department of Chemistry, University of Cambridge Lensfield Road Cambridge CB2 1EW UK
The pharmaceutical industry cares about reducing toxic side effects of drugs in oral formulation. The best solution is to reduce the drug dose. To do so, drugs are required to have high aqueous solubility to ensure good bioavailability.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!