Human serum albumin-based propulsive Piperlongumine-loaded nanoparticles: Formulation development, characterization and anti-cancer study

Piperlongumine (PL) is a naturally occurring bioactive plant alkaloid, endowed with potential pharmacological activities, such as anti-inflammatory, antidiabetic, anti-atherosclerotic, anticancer and antibacterial properties. However, its hydrophobicity impose limitations in achieving great therapeutic efficacy. In the present study we have formulated Piperlongumine-loaded human serum albumin nanoparticles (PLNP) by desolvation method to enhance its bioavailability and anticancer potential. The resulting PLNPs were analyzed by Dynamic Light Scattering (DLS), High-resolution Transmission Electron Microscopy (HR-TEM), Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD). The HR-TEM images confirmed the formation of spherical-shaped nanoparticles, with an average particle size of 105 nm. Further encapsulation of Piperlongumine in human serum albumin nanoparticle was confirmed by FTIR and the nature of encapsulation was characterized by XRD. PLNP showed a sustained drug release profile and higher anti-cancer efficacy against HCT 116 colorectal cancer cells. The PLNP synthesized were stable up to 3 months. The AO/EtBr staining, Hoechst 33342 assays, colony formation assay and mRNA expression studies revealed that the PLNP induced more apoptosis as compared to pure PL, in HCT 116 cells. Thus, PLNP can be used to enhance the therapeutic potential of pure Piperlongumine and a better therapeutic approach to treat colorectal cancer.