Preparation, characterization and in vitro anticancer efficacy of biotin-conjugated, silibinin loaded bovine serum albumin nanoparticles

Abstract

Silibinin (SBN) is a natural, plant-derived bioactive flavonolignan, possessing wide range of pharmaceutical activities including anticancer. However, poor aqueous solubility and low oral bioavailability restrict its clinical applications. Protein based nanomedicines have emerged as a potential solution to improve the delivery of hydrophobic anticancer agents like SBN. Further, Biotin functionalization of delivery vehicle can provide the added advantage of increased aqueous solubility, controlled drug release and site-specific delivery at the tumor. In the present work, we have prepared biotin conjugated bovine serum albumin nanoparticles (Biotin@BSA-NPs) for the efficient delivery of SBN to cancer cells. The prepared SBN loaded Biotin@BSA-NPs (Biotin@SBN-BSA-NPs) showed nanoscale size (∼157 nm), high monodispersity (PDI 0.102), high encapsulation efficiency (∼83%), and controlled pH-dependent drug release. Biotin@SBN-BSA-NPs reveals dose-dependent and time-dependent cytotoxicity against human cervical cancer (HeLa) cells. The cellular uptake study, MTT assay and AO-EtBr staining assay demonstrate that Biotin@SBN-BSA-NPs had significant anticancer potential, induction of apoptosis and higher uptake compared to pure SBN. Thus, prepared Biotin@SBN-BSA-NPs could be a potential targeted drug delivery system for hydrophobic anticancer bioactive compounds like SBN.