The Preparation Of PLGA-PLL-Peg Nanoparticles Simultaneously Loaded With Daunorubicin and Tetrandrine By Modified Double-Emulsion Method

A functional polymer composed of PLGA, PLL and PEG was synthesized, which was used as carrier material for fabricating drug delivery system of nanoparticles. PLGA-PLL-PEG nanoparticles simultaneously loaded with daunorubicin (DNR) and tetrandrine (Tet) were prepared in order to inhibit MDR activity and enhance the antitumor activity of DNR. A modified double-emulsion solvent evaporation/diffusion method was used to increase the incorporation of DNR (hydrophilic) and Tet (hydrophobic) into PLGA-PLL-PEG nanoparticles (NPs). The influence of various processing parameters on particle size and drug loadings were investigated systematically, such as the molecular weight, such as the molecular weight and concentration of PLGA-PLL-PEG, volume ratio of acetone to dichloromethane, PVA concentration in the external aqueous phase, the volume ratio of internal aqueous phase to external aqueous phase and the surfactants of internal aqueous phase. The particle size of the nanoparticles produced by optimized formulation and preparation was 213.0±12 nm (n = 3) with low polydispersity index (0.075 ± 0.023, n = 3). Transmission electron microscopy (TEM) examination showed that the morphology of the prepared nanoparticles was spherical in shape with a smooth surface. The drug loadings were 3.63±0.15% for DNR and 4.27±0.13% for Tet (n = 3). The entrapment efficiencies were 70.23±1.91% for DNR and 86.5±0.7% for Tet (n = 3). The release of DNR and Tet were sustained over one week. The PLGA-PLL-PEG-NPs formulation was potentially useful for hydrophilic and hydrophobic drugs that require efficient delivery to cancer cells. Disclosures: No relevant conflicts of interest to declare.