Encapsulation of Ellipticine in poly-(3-hydroxybutyrate-co-3-hydroxyvalerate) based nanoparticles and its in vitro application

Biodegradable, biocompatible, renewable and non-toxic polyhydroxyalkanoates (PHAs) based nanoparticles are the novel nanotherapeutic tool which are used for the encapsulation of antineoplastic drugs for cancer therapy. In this study, poly-3-hydroxybutyrate-co-5 mol% 3-hydroxyvalerate (PHBV-S), poly-3-hydroxybutyrate-co-11 mol% 3-hydroxyvalerate (PHBV-11) and poly-3-hydroxybutyrate-co-15 mol% 3-hydroxyvalerate (PHBV-15) were used as a nanocarrier for encapsulation of Ellipticine (EPT). EPT is a model anticancer drug. Physicochemical characteristics such as particle size, its morphology and zeta potential of blank and EPT loaded PHBV-S, PHBV-11 and PHBV-15 nanoparticles were studied. In vitro cytotoxicity tests confirmed that the blank PHBV-S, PHBV-11 and PHBV-15 nanoparticles were demonstrating significant biocompatibility without affecting the survival of cancer cell line A549. The loading efficiency of EPT in PHBV nanoparticles was observed in the range of 39.32 to 45.65%. The % inhibition of cancer cell line A549 ranged from 64.28 to 67.77% in comparison to EPT alone in which % inhibition found to be ≤ 45.11%. The IC50 value for each of three different formulations of EPT loaded PHBV nanoparticles ranged from 1.00 to 1.31 μg/mL. The order of % inhibition of cancer cell line A549 for drug loaded nanoparticles was EPT-PHBV-15 > EPT-PHBV-S > EPT-PHBV-11. This system had demonstrated a great potential to increase the cytotoxic effect of EPT by increasing its bioavailability.