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Siyad M.A.,Rajiv Gandhi Center for Biotechnology Poojappura | Vinod Kumar G.S.,Rajiv Gandhi Center for Biotechnology Poojappura
Amino Acids | Year: 2013

Poly(N,N-bisethylamine) dendrimers with high content of poly(ethylene glycol) were synthesized on 3-(Acryloyloxy)-2-hydroxypropylmethacrylate- crosslinked polystyrene (PS-AHMA) resin and tested in various conditions of solid phase peptide synthesis. The dendritic templates were generated to the second generation on cross-linker active site of 3-(Acryloyloxy)-2- hydroxypropylmethacrylate (AHMA). First generation dendrimer was designed by series of four-stage reactions, such as Schiff base incorporation, acidolytic cleavage, diazotization and thionyl chloride treatment and same synthetic routes were followed for second generation also. Poly(ethylene glycol) (PEG1000) has been grafted to second-generation dendrimer and used to check various physico-chemical parameters in Fmoc/Boc peptide synthetic conditions. The utility of PEGylated dendrimer support was demonstrated by synthesizing biologically potent linear as well as disulfide-bonded peptide by Fmoc method. © 2012 Springer-Verlag Wien. Source


Ashwanikumar N.,Rajiv Gandhi Center for Biotechnology Poojappura | Kumar N.A.,Cancer Research Programme | Nair S.A.,Cancer Research Programme | Vinod Kumar G.S.,Rajiv Gandhi Center for Biotechnology Poojappura
RSC Advances | Year: 2014

In the present study, we report a phenylalanine (Phe)-containing self-assembling peptide nanofibrous material (RATEA-F8) for the delivery of the drug 5-fluorouracil (5-FU) and leucovorin (LV), which exhibit synergistic actions against colon cancer. Solid phase peptide synthesis, followed by morphological characterisation of the material, depicts a facile formation of nanofiber in a time-dependent manner. Structural analysis and physical characterisation of the material were performed by transmission electron microscopy (TEM), circular dichriosm, spectrofluorimetry and oscillatory rheology. The in vitro release was also studied for 5-FU, LV and a model molecule namely Phe. The facile cellular uptake (monitored using confocal microscopy) and significant amount of cytotoxicity displayed by the drug entrapped peptide nano material further confirms the efficacy of the developed system for the drug delivery purpose. © 2014 The Royal Society of Chemistry. Source


Pillai J.J.,Rajiv Gandhi Center for Biotechnology Poojappura | Devika N.C.,Rajiv Gandhi Center for Biotechnology Poojappura | Ashwanikumar N.,Rajiv Gandhi Center for Biotechnology Poojappura | Kumar G.S.V.,Rajiv Gandhi Center for Biotechnology Poojappura
RSC Advances | Year: 2015

Herein we report curcumin entrapped nanoparticles of PLGA-PEG copolymer which were conjugated with folic acid (PPF copolymer) for site specific targeting since many cancer cells exhibit external folic acid binding receptors. The PPF copolymer was synthesised by two steps using DCC/NHS chemistry and characterized by FT-IR and 1H-NMR techniques. The curcumin was encapsulated in PPF by single emulsion-solvent evaporation method. The nanoparticles were characterised by TEM and DLS for their size and morphology. The thermal properties were assessed by DSC data. In vitro release kinetics measurements of the drug from the nanoparticles showed a controlled release pattern over a period of time. The MTT assay depicted a high amount of cytotoxicity of PPF nanocurcumin in HeLa cells. Cellular uptake studies demonstrated the efficacy of surface engineering with folate over free nanoparticles. Furthermore, the biological evaluations, for example AO/EB staining, DAPI staining, and clonogenic assay of the nanoparticles confirm the efficacy and mechanism by which the cytotoxicity was induced. © 2015 The Royal Society of Chemistry. Source

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