Search

Spinal cord injury (SCI) is a severe neurodegenerative disease caused by mechanical and biological factors, manifesting as a loss of motor and sensory functions. Inhibition of injury expansion and even reversal of injury in the acute damage stage of SCI are important strategies for treating this disease. Hydrogels and nanoparticle (NP)‐based drugs are the most effective, widely studied, and clinically valuable therapeutic strategies in the field of repair and regeneration. Hydrogels are 3D flow structures that fill the pathological gaps in SCI and provide a microenvironment similar to that of the spinal cord extracellular matrix for nerve cell regeneration. NP‐based drugs can easily penetrate the blood‐spinal cord barrier, target SCI lesions, and are noninvasive. Hydrogels and NPs as drug carriers can be loaded with various drugs and biological therapeutic factors for slow release in SCI lesions. They help drugs function more efficiently by exerting anti‐inflammatory, antioxidant, and nerve regeneration effects to promote the recovery of neurological function. In this review, the use of hydrogels and NPs as drug carriers and the role of both in the repair of SCI are discussed to provide a multimodal strategic reference for nerve repair and regeneration after SCI. [ABSTRACT FROM AUTHOR]

A series of oral prodrugs based on the structure of gemcitabine (2′,2′-difluorodeoxycytidine) were synthesised by introducing an amide group at the N4-position of the cytidine ring. A total of 16 compounds were obtained, and their chemical and biological characteristics were evaluated. The half-maximal inhibitory concentrations (IC50s) for most of these compounds were higher than that of gemcitabine in vitro. Compounds 5d and 5m, the representative compounds, were examined in terms of their physiological stabilities and pharmacokinetics. Compound 5d showed good stability in PBS and simulated intestinal fluid, and an analysis of its pharmacokinetics in mice suggested that the introduction of an amide group to gemcitabine could greatly improve its bioavailability. Further evaluation of compound 5d in vivo showed that this compound possesses higher activity than gemcitabine against the growth of HepG2 human hepatocellular carcinoma cells and HCT-116 colon adenocarcinoma cells with less toxicity to animals. These results suggest that compound 5d could be further developed as a potential oral anticancer agent for clinical applications in which gemcitabine is currently used. [ABSTRACT FROM AUTHOR]