Synthesis of targeted drug delivery system for fluorouracil using sulfadiazine as the carrier.

Di Yi Jun Yi Da Xue Xue Bao

Department of Oncology, Zhujiang Hospital, First Military Medical University, Guangzhou 510282, China.

Published: November 2002

Objective: To synthesize a targeted drug delivery system for 5-fluorouracil (5Fu) using sulfadiazine (SF) as a carrier with reduced side-effects and strong antitumor activity.

Methods: SF-poly (ethylene glycol) (PEG) conjugate was initially synthesized. 5Fu was subjected to reaction with trichloromethyl chloroformate to prepare chloroformyl 5Fu, which was linked to a spacer hydroxyl group of PEG that served as a macromolecular linking arm between SF and 5Fu. The content of 5Fu in the conjugate was determined by ultraviolet spectrophotometry. Spectrum of ultraviolet and infrared along with differential scanning calorimetry were employed to identify the structure of the conjugate of SFPEG-end capped 5Fu.

Results: The drug loading content of the conjugate was 3.2 %, and structural analysis confirmed the linkage between 5Fu and SF via PEG.

Conclusion: Targeted drug delivery system for 5Fu using SF as a carrier has been successfully synthesized by this means.

Download full-text PDF

Source

Publication Analysis

Top Keywords

targeted drug
12
drug delivery
12
delivery system
12
sulfadiazine carrier
8
5fu
7
synthesis targeted
4
drug
4
system fluorouracil
4
fluorouracil sulfadiazine
4
carrier objective
4

Similar Publications

Rare dual MYH9-ROS1 fusion variants in a patient with lung adenocarcinoma: A case report.

Medicine (Baltimore)

January 2025

Department of Respiratory and Critical Care Medicine, Zhongshan City People's Hospital, Zhongshan, Guangdong Province, China.

Rationale: ROS proto-oncogene 1 (ROS1) fusion is a rare but important driver mutation in non-small cell lung cancer, which usually shows significant sensitivity to small molecule tyrosine kinase inhibitors. With the widespread application of next-generation sequencing (NGS), more fusions and co-mutations of ROS1 have been discovered. Non-muscle myosin heavy chain 9 (MYH9) is a rare fusion partner of ROS1 gene as reported.

View Article and Find Full Text PDF

Amphibian-Derived Peptides as Natural Inhibitors of SARS-CoV-2 Main Protease (Mpro): A Combined In Vitro and In Silico Approach.

Chem Biodivers

January 2025

Universidad Nacional del Litoral Facultad de Bioquimica y Ciencias Biologicas, Química Orgánica, Ciudad Universitaria. Paraje el Pozo S/N, Argentina, 3000, Santa Fe, ARGENTINA.

The COVID-19 pandemic, caused by the SARS-CoV-2 virus, has highlighted the urgent need for novel therapeutic agents targeting viral enzymes such as the main protease (Mpro), which plays a crucial role in viral replication. In this study, we investigate the inhibitory potential of 23 peptides isolated from the skin of amphibians belonging to the Hylidae and Leptodactylidae families against SARS-CoV-2 Mpro. Five peptides demonstrated significant inhibition using a colorimetric Mpro inhibition assay, with IC50 values ranging from 41 to 203 µM.

View Article and Find Full Text PDF

Background: To assess the impact of attaining aggressive beta-lactam pharmacokinetic/pharmacodynamic (PK/PD) targets on clinical efficacy in critical orthotopic liver transplant (OLT) recipients with documented early Gram-negative infections.

Methods: OLT recipients admitted to the post-transplant ICU between June 2021 and May 2024 having documented Gram-negative infections treated with targeted therapy continuous infusion (CI) beta-lactams, and undergoing therapeutic drug monitoring (TDM)-guided beta-lactam dosing adjustment in the first 72 hours were prospectively enrolled. Free steady-state concentrations (fCss) of beta-lactams (BL) and/or of beta-lactamase inhibitors (BLI) were calculated, and aggressive PK/PD target attainment was measured.

View Article and Find Full Text PDF

Purpose: Treatment of peripheral artery disease (PAD) in the region below the knee (BTK) is dissatisfying as failure of treated target lesions (TLF) is frequent and diagnostic imaging is often challenging. In the BTK-region metallic drug-eluting stents (mDES) yielded best results concerning primary patency (PP), but also annihilate signal in magnetic resonance angiography (MR-A). A recently introduced non-metallic drug eluting bioresorbable Tyrocore® vascular scaffold (deBVS), that offers an option for re-treatment of lesions due to its full degradation within 3-4 years after placement, was investigated with respect to its compatibility with MR-A to unimpededly depict previously treated target lesions.

View Article and Find Full Text PDF

Introduction: Tuberculosis remains a major public health problem, primarily in low- and middle-income countries. Evaluating treatment outcomes and investigating factors associated with them are essential for the treatment and control of tuberculosis. Hence, this study aims to assess the TB treatment outcomes and associated factors in Bosaso, Puntland, Somalia.

View Article and Find Full Text PDF

Want 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!