RESUMEN
Ceftriaxone sodium belongs to the third-generation cephalosporin group and is used intramuscular and intravenous route as a broad-spectrum antibiotic. This research aims to prepare biocompatible hydrogels for targeted delivery of ceftriaxone sodium by parental route. Different proportions of polymers (natural and synthetic) in the presence of cross-linker were synthesized by solvent casting method. Ceftriaxone sodium was loaded in hydrogels in different concentrations and its drug release behavior was evaluated along with swelling and biodegradation analysis. The characterization of hydrogel was done by scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) to analyze surface morphology and functional groups involved in the formation of dextrin/Na-alginate/PVA hydrogels loaded with the drug. Thermogravimetric analysis (TGA) was confirmed by thermal stability and degradation pattern of loaded and unloaded hydrogels. The drug-loaded samples presented promising antimicrobial activity against S. aureus and P. multocida and their cytotoxic nature was also studied. Drug release analysis using simulated intestinal fluid (SIF) and phosphate buffer saline(PBS) for the circulatory system shows the consistent release of the drug. The findings unveiled the development of a biocompatible and innovative hydrogel, which has potential advantages for biomedical application, particularly in enhancing the therapeutic efficacy of ceftriaxone sodium drug.
RESUMEN
BACKGROUND: Orlistat (ORL) is an effective irreversible inhibitor of the lipase enzyme, and it possesses anticancer effects and limited aqueous solubility. This study was designed to improve the aqueous solubility, oral absorption, and tissue distribution of ORL via the formulation of nanocrystals (NCs). METHODS: ORL-NC was prepared using the liquid antisolvent precipitation method (bottom-up technology), and it demonstrated significantly improved solubility compared with that of the blank crystals (ORL-BCs) and untreated ORL powder. The biodistribution and relative bioavailability of ORL-NC were investigated via the radiolabeling technique using Technetium-99m (99mTc). Female Swiss albino mice were used to examine the antitumor activity of ORL-NC against solid Ehrlich carcinoma (SEC)-induced hepatic damage in mice. RESULTS: The prepared NCs improved ORL's solubility, bioavailability, and tissue distribution, with evidence of 258.70% relative bioavailability. In the in vivo study, the ORL-NC treatment caused a reduction in all tested liver functions (total and direct bilirubin, AST, ALT, and ALP) and improved modifications in liver sections that were marked using hematoxylin and eosin staining (H&E) and immunohistochemical staining (Ki-67 and ER-α) compared with untreated SEC mice. CONCLUSIONS: The developed ORL-NC could be considered a promising formulation approach to enhance the oral absorption tissue distribution of ORL and suppress the liver damage caused by SEC.
RESUMEN
There is a need for new antimicrobial systems due to increased global resistance to current antimicrobials. Pomegranate rind extract (PRE) and Zn (II) ions both possess a level of antimicrobial activity and work has previously shown that PRE/Zn (II) in combination possesses synergistic activity against Herpes simplex virus and Micrococcus luteus. Here, we determined whether such synergistic activity extended to other, more pathogenic, bacteria. Reference strains of methicillin-resistant Staphylococcus aureus (MRSA), Staphylococcus epidermidis, Escherichia coli, and Pseudomonas aeruginosa were cultured and subjected to challenge by PRE, Zn (II), or PRE + Zn (II), in time-kill assays. Data were obtained independently by two researchers using different PRE preparations. Statistically significant synergistic activity for PRE + Zn (II) was shown for all four bacterial strains tested compared to untreated controls, although the extent of efficacy and timescales varied. Zn (II) exerted activity and at 1 h, it was not possible to distinguish with PRE + Zn (II) combination treatment in all cases. PRE alone showed low activity against all four bacteria. Reproducible synergistic bactericidal activity involving PRE and Zn (II) has been confirmed. Potential mechanisms are discussed. The development of a therapeutic system that possesses demonstrable antimicrobial activity is supported which lends itself particularly to topical delivery applications, for example MRSA infections.
