In the realm of modern therapeutics, the development of polymeric delivery vehicles has revolutionized drug administration, offering a sophisticated approach to controlled and sustained drug release
Accurately measuring drug and its release kinetics in both in vitro and in vivo environments is crucial for enhancing therapeutic effectiveness while minimizing potential side effects. Nevertheless, the real-time visualization of drug release from microspheres to monitor potential overdoses remains a challenge. The primary objective of this investigation was to employ fluorescence imaging for the real-time monitoring of drug release from microspheres in vitro, thereby simplifying the laborious analysis associated with the detection of drug release. Two distinct varieties of microspheres were fabricated, each encapsulating different drugs within PLGA polymers. Cy5 was selected as the donor, and Cy7 was selected as the acceptor for visualization and quantification of the facilitated microsphere drug release through the application of the fluorescence resonance energy transfer (FRET) principle. The findings from the in vitro experiments indicate a correlation between the FRET fluorescence alterations and the drug release profiles of the microspheres.
To overcome the poor bioaccessibility of Coenzyme Q10 (CoQ10), we developed a polyethylene glycol-based dripping pill (DP) solid dispersion system. The optimized formulation achieved an amorphous state, resulting in uniform morphology, significantly accelerated dissolution, and enhanced oral bioavailability compared to crystalline CoQ10. In an isoproterenol-induced oxidative cardiac stress model, CoQ10 DPs showed enhanced in vivo bioactivity by alleviating cardiac remodeling and oxidative injury. Mechanistically, the enhanced delivery interrupted the oxidative stress-inflammation loop, evidenced by the clearance of reactive oxygen species (ROS) and restoration of superoxide dismutase (SOD) activity. This study presents a robust formulation strategy to maximize the bioactivity of lipophilic nutrients for functional food applications.