Polyphenol-assisted facile assembly of bioactive nanoparticles for targeted therapy of heart diseases

It remains a great challenge for targeted therapy of heart diseases. To achieve desirable heart targeting, we developed a polyphenol-assisted nanoprecipitation/self-assembly approach for facile engineering of functional nanoparticles. Three different materials were employed as representative carriers, while gallic acid, catechin, epigallocatechin gallate, and tannic acid (TA) served as typical polyphenols with varied numbers of phenolic hydroxyl groups. By optimizing different parameters, such as polyphenol types and the weight ratio of carrier materials and polyphenols, well-defined nanoparticles with excellent physicochemical properties can be easily prepared. Regardless of various carrier materials, TA-derived nanoparticles showed potent reactive oxygen species-scavenging activity, especially nanoparticles produced from a cyclodextrin-derived bioactive material (TPCD). By internalization into cardiomyocytes, TPCD/TA nanoparticles (defined as TPTN) effectively protected cells from hypoxic-ischemic injury. After intravenous injection, TPTN considerably accumulated in the injured heart in two murine models of ventricular fibrillation cardiac arrest in rats and myocardial hypertrophy in mice. Correspondingly, intravenously delivered TPTN afforded excellent therapeutic effects in both heart diseases. Preliminary experiments also revealed good safety of TPTN. These results substantiated that TPTN is a promising nanotherapy for targeted treatment of heart diseases, while polyphenol-assisted self-assembly is a facile but robust strategy to develop heart-targeting delivery systems.

Automated summary

Developing targeted therapy for heart diseases remains a significant challenge. A polyphenol-assisted nanoprecipitation/self-assembly method was developed to easily engineer functional nanoparticles for heart targeting. By using different carrier materials and polyphenols, well-defined nanoparticles with excellent properties can be prepared efficiently. TA-derived nanoparticles showed potent ROS-scavenging activity, especially those produced from a cyclodextrin-derived bioactive material. Moreover, these nanoparticles effectively protected cardiomyocytes from hypoxic-ischemic injury and showed promising therapeutic effects in murine models of heart diseases.