Aim: To make delivery improvements via delivery systems for 6-(4-morpholino-3-(trifluoromethyl)phenyl)pyridazin-3(2H)-one (DZO) - a model compound of hydrophobic antitumor candidate pyridazinone derivatives.
Materials & Methods: Methoxy poly(ethylene glycol)-poly(D,L-lactide) (MPEG-PDLLA) micelle was employed as a vector, and DZO was encapsulated in. The DZO-loaded micelles were characterized in detail and its cytotoxicity, maximum tolerated dose (MTD) and pharmacokinetic experiments were done. In vivo anticancer activity was studied through a subcutaneous 4T1 tumor model.
Results: Compared with free DZO, the DZO-loaded micelles possessed a sustained release property, an improved MTD, better pharmacokinetic parameters and an enhanced antitumor activity for subcutaneous 4T1 model in vivo.
Conclusion: An effective injectable delivery system for DZO was developed successfully.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2217/nnm.15.66 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
An sp2 Carbon-Conjugated Covalent Organic Framework for Fusing Lipid Droplets and Engineered Macrophage Therapy.
Angew Chem Int Ed Engl
January 2025
University of Macau, Institute of Chinese Medical Sciences, Avenida da Universidade, N22, Taipa, CHINA.
Engineered immune cell therapy has proven to be a transformative cancer treatment despite the challenges of its prohibitive costs and manufacturing complexity. In this study, we propose a concise "lipid droplet fusion" strategy for engineering macrophages. Because of the integration of hydrophobic alkyl chains and π-conjugated structures, the mildly synthesized sp2C-conjugated covalent organic framework (COF) UM-101 induced lipid droplet fusion and metabolic reprogramming of macrophages, thus promoting their antitumor classical activation.
View Article and Find Full Text PDFSodium hyaluronate microcapsules to promote antitumor selectivity of anacardic acid.
Int J Biol Macromol
January 2025
Laboratory of Polymers and Materials Innovation, Department of Organic and Inorganic Chemistry, Federal University of Ceará, Campus of Pici, 60440-900 Fortaleza, CE, Brazil. Electronic address:
Anacardic acid (AA) is a phenolic lipid extracted from cashew nutshell liquid that has antitumor activity. Given the high hydrophobicity of this compound and aiming to create efficient vehicle for its administration in aqueous systems, the objective of the present work was to develop a microcapsule (MCAA) by spray dryer technique, based on the polysaccharide sodium hyaluronate (SH), containing AA as its core, encapsulated from nanoemulsion. The Encapsulation Efficiency of MCAA presented a value equal to 95.
View Article and Find Full Text PDFBiocompatible nanoparticles self-assembled by PEGylated polyphosphoesters for combination of photodynamic therapy and hypoxia-activated chemotherapy against breast cancer.
Front Pharmacol
December 2024
Department of Radiology, Tianjin Key Laboratory of Functional Imaging and Tianjin Institute of Radiology, Tianjin Medical University General Hospital, Tianjin, China.
Introduction: Although photodynamic therapy (PDT) shows considerable potential for cancer treatment due to its precise spatial control and reduced toxicity, effectively eliminating residual cells under hypoxic conditions remains challenging because of the resistance conferred by these cells.
Methods: Herein, we synthesize an amphiphilic PEGylated polyphosphoester and present a nanocarrier (NP) specifically designed for the codelivery of hydrophobic photosensitizer (chlorin e6, Ce6) and hypoxia-activated prodrugs (tirapazamine, TPZ). We investigate the antitumor effect of NP on both cellular and animal level.
A Nanotheranostic Agent for Synergistic Antitumor Chemo/Phototherapy Prepared by Paclitaxel-Induced Self-Assembly of PEGylated Human Serum Albumin with Prolonged Circulation.
ACS Omega
December 2024
Key Laboratory of Chemical Biology of Natural Products (Ministry of Education), Institute of Biochemical and Biotechnological Drugs, School of Pharmaceutical Sciences, Shandong University, Jinan, Shandong 250012, China.
The integration of different therapies to enhance the efficacy and minimize adverse reactions has become popular recently. This approach leverages the complementary mechanisms of action of different treatments, which can lead to better therapeutic outcomes and reduced side effects. Human serum albumin (HSA) exhibits excellent drug loading ability and is often used for biomimetic tumor delivery in multidrug nanocarriers.
View Article and Find Full Text PDFLight-Controlled Intracellular Synthesis of Poly(luciferin) Polymers Induces Cell Paraptosis.
J Am Chem Soc
January 2025
Department of Radiology, Molecular Imaging Program at Stanford, Stanford University School of Medicine, Stanford, California 94305, United States.
Accumulation of misfolded proteins challenges cellular proteostasis and is implicated in aging and chronic disorders. Cancer cells, moreover, face an elevated level of basal proteotoxic stress; hence, exacerbating endoplasmic reticulum (ER) stress has been shown to induce programmed cell death while enhancing anticancer immunogenicity. We hypothesize that hydrophobic abiotic macromolecules can trigger a similar stress response.
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!