Formulation and evaluation of polymeric nanoparticles to improve in vivo chemotherapeutic efficacy of mangiferin against breast cancer.

Abstract

Mangiferin (Mgf), a naturally occurring polyphenol, can act as an apoptosis inducer for various cancer cells. Thus, it is holding the prospect of being a promising chemotherapeutic agent. However, a discrepancy between the in vitro results and in vivo observations seems to exist that apprehends its potential usefulness. The in vivo chemotherapeutic capacity of Mgf is greatly challenged because of the unfavorable pharmacokinetic credentials. The present study aims to overcome the biopharmaceutical limitations and improve the chemotherapeutic efficacy by incorporating it within nano-scale delivery system. Stable and sphere-shaped Mgf-loaded poly(lactic-co-glycolic) acid (PLGA) nanoparticles (MNPs) were formulated using the nanoprecipitation method and characterized. Further, MNPs were assessed through multiple in vitro and in vivo preclinical evaluations for their chemotherapeutic efficacy, with an ambition to improve the performance in the biological system. Sphere-shaped MNPs exhibited satisfactory drug loading and release profile. The Mgf-loaded nanoformulation also exhibited better cytotoxic potential against breast cancer cells compared to native Mgf owing to its better penetrability into cancer cells. MNPs were also found to confer superior in vivo chemotherapeutic efficacy in breast cancer-bearing mice evidenced by the reduction of tumor load. Improved anti-cancer potential of MNPs over free Mgf was also established through different bioassays. Moreover, the nanoparticles did not confer systemic toxicity to levels of concern. To conclude, the current study pleads for MNPs as a safe and efficacious tool in the fight against breast cancer for futuristic translations.