Targeted Drug Delivery Using Polymeric Encapsulation for Enhanced Antineoplastic Activity

Abstract A non-repairable genomic mutation in cell cycle proteins can endow targeted cells with unlimited replicative potential, leading to the inappropriate overexpression of oncogenes or the formation of novel oncogenes, alongside the concurrent underexpression of tumor suppressor genes. This results in the development of neoplastic cells with invasive characteristics, commonly referred to as cancer cells. Current cancer therapies focus on targeted drug delivery systems designed to modify the drug release profile and ADME (absorption, distribution, metabolism, and excretion) properties, thereby minimizing side effects on non-cancerous cells. Bis(Iso-thiocyanatomethyl) Benzene, an antineoplastic compound, was isolated and purified from the leaves of Moringa oleifera, as reported in the literature. This compound was successfully encapsulated with a 68% efficiency (n = 3) into a polyvinyl alcohol matrix, resulting in the creation of nano/micro-sized "polymeric encapsulated sub-micron particles (PESP)" through a one-step modified binary nonsolvent conservation method. The details of this process have been documented in Indian patent file no: 544591. A single-dose cell viability assay revealed that the PESP-loaded compound inhibited the MDA-MB-231 cell line more effectively than the MCF-7 cell line, while demonstrating lower cytotoxicity towards peripheral blood mononuclear cells (PBMCs). In silico studies showed that the compound interacted with estrogen and epidermal growth factor receptors, inducing apoptosis in MDA-MB-231 cells via a caspase-dependent pathway. Additionally, the polyvinyl alcohol matrix enhanced the binding and bioavailability of the PESP, as confirmed by cell-based adhesion and soft agar colony formation assays. This advanced delivery system is thus considered a promising method for achieving targeted antineoplastic activity.