Development of surface conjugated block co polymeric micelles as targeted therapeutics: characterization and in-vitro cell viability

Erlotinib is epidermal growth factor receptor inhibitor used as anticancer first line therapy to treat non-small cell lung cancer. However, its low water solubility, along with adverse drug reactions from deposition in normal cells, limits its use in therapy. Biotin conjugated Pluronic F68-Polycaprolactone has been proven to improve pharmacokinetics of drug and reduce its toxicity. In this study Block co-polymer (Biotin- Pluronic F68-PCL) were synthesized and characterized for the structural conformation by FTIR and NMR Spectroscopy. Quality by design, a statistical tool was applied for optimization of various parameters that impact micelle size, entrapment efficiency and zeta potential. Design matrix generated using Minitab software and graphical presentation via contour plot revealed science-based development of formulation and resulted in requisite micellar size of 115.1 nm and entrapment efficiency of 94% ± 2.34 in ratio 1:5. Drug release of optimized block co-polymeric micelles was found to be slow and controlled release and is approximately pH dependent. The MTT cell assay and cellular uptake on A549 cell line shows better cell inhibition of Biotin conjugated Pluronic F68-PCL compared to pluronic F68-PCL and untreated erlotinib. In nutshell, Biotinylated block co-polymeric micelles would be platform delivery for targeting anticancer agent to treat non-small cell lung cancer.