An 18 kDa TSPO specific ligand-based polymeric nanoformulation: synthesis, computational and biological studies

Abstract

An 18 kDa translocator protein (TSPO) serves as a promising target for drug delivery and imaging applications. In this investigation, we have encapsulated MCBP, a TSPO compound based on acetamidobenzoxazolone, within a poly(D,L-lactic-co-glycolic acid) (PLGA) polymer to evaluate the effectiveness of MCBP–PLGA-NP as a targeted carrier for drug delivery. Our investigation involves the analysis of ADME (absorption, distribution, metabolism, and excretion) and other pertinent factors, conducted through photo-physical studies with serum albumin. In order to evaluate the compatibility of the formulation loaded with MCBP with red blood cells (RBCs), we utilized a hemolysis test. The findings indicate that the formulation is compatible with blood (hemocompatible) and does not cause hemolysis. Additionally, the cytotoxicity of the nanoformulation was assessed using the SRB assay, revealing a non-cytotoxic nature, suggesting its potential safety for biological systems. Imaging studies with ^99mTc-labeled MCBP–PLGA-NP provided insights into the specificity and distribution patterns of this nanoparticle. Overall, our results highlighted the potential of MCBP–PLGA-NP as an efficient and safe targeted drug delivery carrier.