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The aim of this study was to investigate the combined influence of 3 independent variables in the preparation of temozolomide bearing Non-PEGylated and PEGylated nanoparticles by emulsification solvent evaporation method. A 3 factor 2 level design was used to derive a polynomial quadratic model and construct contour plots to predict responses. the independent variables selected were concentration of drug (A), concentration of PLGA/PEG-PLGA (B), pVA concentration in aqueous phase (C) and sonication time (D) and evaluated for percentage drug entrapment (PDE) and particle size (PS). A 34 factorial design was used with 4 factors (A, B, C and D) at 3 levels and experimental trials were performed at all 82 possible combinations. In the present work, 28 runs are considered as the preliminary trials revealed that on increasing drug concentration from 2.5 to 5 mg the percent drug entrapment increases, but on further increasing the drug concentration (i.e., to 7.5 mg) no significant effect on the percent drug entrapment and particle size was observed. the 34 factorial design was used to derive a polynomial quadratic model and construct contour plots to predict responses. Contour plots were constructed to show the effects of A, B, C and D on the PDE and pS. [ABSTRACT FROM AUTHOR]

Polymer-based nanotechnologies are proposed to be an alternative for drug administration, delivery and targeting to those of conventional formulations. The blood brain barrier is frequently a rate-limiting factor in determining permeation of a drug into brain. In this study, the surface-engineered long-circulating PLGA nanoparticles (NPs) were assessed for brain-specific delivery. Long circulating NPs of PLGA- and PEG-synthesised copolymer were prepared by emulsification solvent evaporation method. Further, the surface of PEGylated NPs was modified by anchoring transferrin (Tf) ligand for receptor-mediated targeting to brain. NPs were characterised for shape and size, zeta potential, entrapment efficiency and in vitro drug release. In vitro cytotoxicity studies were performed on human cancer cell lines. Confocal Laser Scanning Microscopy studies show the enhanced uptake of Tf-appended PEGylated NPs and their localisation in the brain tissues. Hence, the specific role of Tf ligand on PEGylated NPs for brain delivery was confirmed. [ABSTRACT FROM AUTHOR]