Abstract The Naphthol AS-E Phosphate (NASEP) potentially reduce cell-growth, and proliferation making a suitable candidate in anti-cancer therapies. The short synthetic amino acid sequence Gly-Arg-Gly-Asp-Ser pentapeptide (GRGDS) and low-molecular-weight heparin (LMWH) functionalized metal-organic-framework (MOF) were prepared using 5-steps method, i.e., vapor diffusion of potassium hydroxide and gamma-cyclodextrin (γ-CD) to prepare γ-Cyclodextrin metal organic framework (CD-MOF; polymerization of CD-MOF (CDF); biofunctionalization of CDF with GRGDS (RGD-CDF); preparation of cystamine-LMWH complex (Cys-LMWH); and finally GRGDS and LMWH functionlized MOF (RGD-CDF-LMWH that had abbreviated as RCL) using RGD-CDF and Cys-LMWH. Then, NASEP impregnated to RCL (RCL-NASEP). The refined RCL-NASEP were investigated using scanning electron microscopy (SEM), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance spectroscopy ( 1 HNMR), and estimated for drug release, antioxidant, anti-inflammatory, cytotoxicity, pharmacokinetics, and stability test. The nanoparticles had a particle dimension of 202.34 ± 4.31 nm, zeta potential of −21.91 ± 0.81 mV, PDI of 0.270 ± 0.15, entrapment efficiency of 79.16 ± 1.2 %, and loading of 13.58 ± 1.0 %. It had good storage stability at 4 °C at 60 ± 5 % RH. The RCL-NASEP has sustained release over extended period. RCL-NASEP diminished viable cells to 34.52 ± 2.51 % at 8 µM concentration in A549 cells with IC50 value of 3.29 µM reported after 24 h. The RCL-NASEP showed anti-inflammatory and antioxidant effect and their IC 50 value were 60.07 ± 0.34 and 220.07 ± 1.42 μg/mL. The bio-distribution analysis revealed a higher concentration of RCL-NASEP in the lung tissues. The pharmacokinetic parameters (C max , T 1/2 , AUC) estimated were higher for RCL-NASEP than NASEP after intravenous administration of a single-dose of 1 mg/kg in mice.
Sarma et al. (Thu,) studied this question.