Novel glucosamine-loaded thermosensitive hydrogels based on poloxamers for osteoarthritis therapy by intra-articular injection.

Glucosamine (GlcN) is a common drug used to treat osteoarthritis (OA). To prolong the action time of glucosamine on OA and improve its therapeutic effect, this research explored the potential application of GlcN-loaded thermosensitive hydrogels based on poloxamer 407 and poloxamer 188 for OA therapy by intra-articular injection. The thermosensitive hydrogels were prepared by cold method, and the effects of P407, P188, and GlcN on sol-gel transition temperature (Tsol-gel) were compared. After screening was performed, the optimized formulation showed good temperature sensitivity, and Tsol-gel was approximately 35 °C. In vitro release tests showed that GlcN was slowly released from the thermosensitive hydrogels. After the gels were intra-articularly administered to treat OA in rabbits, the degree of swelling and inflammatory factors were significantly decreased in the hydrogel group compared with those in the OA model group (P < 0.05). Histological results showed that the GlcN-administered group had a good repair effect on damaged cartilage. At the same dose, the effect of the thermosensitive hydrogels was better than that of the aqueous solution. Therefore, GlcN-loaded thermosensitive hydrogels based on poloxamers are promising sustainable delivery systems for OA therapy by intra-articular injection.

Isobologram Analysis: A Comprehensive Review of Methodology and Current Research.

Drug combination is a common method for clinical disease treatment. Whether the combination of drugs is reasonable often affects the result of the disease treatment. Many methods have been used to evaluate interaction between drugs to date. Isobologram analysis has been mathematically proven and widely used to evaluate drug interactions. In this paper, the principle of isobologram analysis and its application in drug interaction evaluation are summarized. The applications of the similar cotoxicity coefficient and fractional inhibitory concentration index in the evaluation of drug interaction are also reviewed. This work is expected to evaluate the effect of formulations scientifically and provide scientific judgment standards for the development of formulations and clinical drug compatibility.

Preparation of cefquinome sulfate cationic proliposome and evaluation of its efficacy on Staphylococcus aureus biofilm.

Staphylococcus aureus (S. aureus) has the propensity to form biofilms, which eventually cause antibiotic resistance and treatment failure. Cefquinome sulfate (CS) is an animal-specific antibacterial agent for S. aureus infection. In this work, CS cationic proliposomes (CSCPs) were prepared by solid-dispersion method combined with effervescent hydration to eradicate bacterial biofilm and improve the antibacterial effect of the drug. CSCPs were readily dispersed in water, thereby forming CS cationic liposomes (CSCLs) as a white, uniform suspension. The CSCLs had an encapsulation efficiency (EE) of 63.21%, a drug loading of 4.04%, an average particle size of 201.5 nm, and a positive zeta-potential of 65.29 mV. In vitro release studies showed that CSCLs had good sustained-release behavior. The CS and CSCL minimal inhibitory concentration (MIC) of S. aureus type culture strain were 1 and 0.48 g/mL, respectively. The eradication effect of CS on bacterial biofilm (BBF) was relatively weak during culture in drug-containing medium for 8 h-24 h. However, the CSCL eradication effect on BBF increased gradually, and the clearance rate of CSCLs on BBF was about twice that of CS. The clearance rate reached 81.30% with 2.5 × MIC in 24 h. All these results indicated that CSCLs can significantly improve the eradication effect of cefquinome on biofilm to inhibit bacterial growth.