Hybrid Nanoparticles for Haloperidol Encapsulation: Quid Est Optimum?

The choice of drug delivery carrier is of paramount importance for the fate of a drug in a human body. In this study, we have prepared the hybrid nanoparticles composed of FDA-approved Eudragit L100-55 copolymer and polymeric surfactant Brij98 to load haloperidol-an antipsychotic hydrophobic drug used to treat schizophrenia and many other disorders. This platform shows good drug-loading efficiency and stability in comparison to the widely applied platforms of mesoporous silica (MSN) and a metal-organic framework (MOF). ZIF8, a biocompatible MOF, failed to encapsulate haloperidol, whereas MSN only showed limited encapsulation ability. Isothermal titration calorimetry showed that haloperidol has low binding with the surface of ZIF8 and MSN in comparison to Eudragit L100-55/Brij98, thus elucidating the striking difference in haloperidol loading. With further optimization, the haloperidol loading efficiency could reach up to 40% in the hybrid Eudragit L100-55/Brij98 nanoparticles with high stability over several months. Differential scanning calorimetry studies indicate that the encapsulated haloperidol stays in an amorphous state inside the Eudragit L100-55/Brij98 nanoparticles. Using a catalepsy and open field animal tests, we proved the prolongation of haloperidol release in vivo, resulting in later onset of action compared to the free drug

Moxifloxacin Metal Complexes: Synthesis, Characterisation, Antimicrobial and Antidiabetic Activities with Docking Studies

Six new metal complexes of Fe(III), Cu(II), and Hg(II) were synthesised, i.e., three (2, 4, and 5) with moxifloxacin (mono-ligand) and the other three (1, 3 and 6) with moxifloxacin and hydrazine (biligand). These were characterised through UV-Vis, FT-IR, elemental analysis (CHN), atomic absorption spectroscopy, TGA, scanning electron microscopy (SEM), and powder XRD studies. Further, all of these compounds were screened for their antimicrobial, cytotoxic, and antidiabetic potential. The study revealed that the synthesised metal complexes possess an excellent ability to become antifungal agents compared to moxifloxacin. Additionally, the cytotoxicity of compounds 1, 3, and 4 was in the acceptable range with much better antidiabetic potential as compared to the ligand moxifloxacin. Interestingly, the α-amylase inhibition activity of complexes 1 and 3 was found very close to the standard drug acarbose. Furthermore, the computational studies also authenticate the results of the antidiabetic potential of complexes 1, 3, and 4 by presenting the necessary interactions of these compounds with their respective binding sites. The overall results indicate that the antifungal and antidiabetic ability of moxifloxacin is enhanced significantly by complexation with the given metals and the secondary ligand, thereby making it a suitable lead compound for yet another avenue of an antifungal and antidiabetic agent in the field of drug discovery and development

Hybrid nanoparticles for haloperidol encapsulation: quid est optimum?

The choice of drug delivery carrier is of paramount importance for the fate of a drug in a human body. In this study, we have prepared the hybrid nanoparticles composed of FDA-approved Eudragit L100-55 copolymer and polymeric surfactant Brij98 to load haloperidol—an antipsychotic hydrophobic drug used to treat schizophrenia and many other disorders. This platform shows good drug-loading efficiency and stability in comparison to the widely applied platforms of mesoporous silica (MSN) and a metal–organic framework (MOF). ZIF8, a biocompatible MOF, failed to encapsulate haloperidol, whereas MSN only showed limited encapsulation ability. Isothermal titration calorimetry showed that haloperidol has low binding with the surface of ZIF8 and MSN in comparison to Eudragit L100-55/Brij98, thus elucidating the striking difference in haloperidol loading. With further optimization, the haloperidol loading efficiency could reach up to 40% in the hybrid Eudragit L100-55/Brij98 nanoparticles with high stability over several months. Differential scanning calorimetry studies indicate that the encapsulated haloperidol stays in an amorphous state inside the Eudragit L100-55/Brij98 nanoparticles. Using a catalepsy and open field animal tests, we proved the prolongation of haloperidol release in vivo, resulting in later onset of action compared to the free drug