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      Stabilizers influence drug–polymer interactions and physicochemical properties of disulfiram-loaded poly-lactide-co-glycolide nanoparticles

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          Abstract

          Aim:

          Stabilizers are known to be an integral component of polymeric nanostructures. Ideally, they manipulate physicochemical properties of nanoparticles. Based on this hypothesis, we demonstrated that disulfiram (drug) and Poly-lactide-co-glycolide (polymer) interactions and physicochemical properties of their nanoparticles formulations are significantly influenced by the choice of stabilizers.

          Methodology:

          Electron microscopy, differential scanning calorimetry, x-ray diffraction, Raman spectrum analysis, isothermal titration calorimetry and in silico docking studies were performed.

          Results & discussion:

          Polysorbate 80 imparted highest crystallinity while Triton-X 100 imparted highest rigidity, possibly influencing drug bioavailability, blood-retention time, cellular uptake and sustained drug release. All the molecular interactions were hydrophobic in nature and entropy driven. Therefore, polymeric nanoparticles may be critically manipulated to streamline the passive targeting of drug-loaded nanoparticles.

          Lay abstract

          Polymeric nanoparticles are futuristic drug-delivering platforms that have many potential advantages above conventional drug-delivery tools. They are mainly composed of a polymer, stabilizer and the therapeutic ingredient. A number of researches are on-going to improvise various characteristics of polymeric nanoparticles, in order to enhance its efficacy. The current study is one such domain where we emphasize on identifying potential stabilizing factors that are involved in nanoparticles formation and their drug entrapment and release properties.

          Most cited references23

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          Biodegradation and hydrolysis rate of aliphatic aromatic polyester

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            A simple click by click protocol to perform docking: AutoDock 4.2 made easy for non-bioinformaticians

            Recently, bioinformatics has advanced to the level that it allows almost accurate prediction of molecular interactions that hold together a protein and a ligand in the bound state. For instance, the program AutoDock has been developed to provide a procedure for predicting the interaction of small molecules with macromolecular targets which can easily separate compounds with micromolar and nanomolar binding constants from those with millimolar binding constants and can often rank molecules with finer differences in affinity. AutoDock can be used to screen a variety of possible compounds, searching for new compounds with specific binding properties or testing a range of modifications of an existing compound. The present work is a detailed outline of the protocol to use AutoDock in a more user-friendly manner. The first step is to retrieve required Ligand and Target.pdb files from major databases. The second step is preparing PDBQT format files for Target and Ligand (Target.pdbqt, Ligand.pdbqt) and Grid and Docking Parameter file (a.gpf and a.dpf) using AutoDock 4.2. The third step is to perform molecular docking using Cygwin and finally the results are analyzed. With due confidence, this is our humble claim that a researcher with no previous background in bioinformatics research would be able to perform molecular docking using AutoDock 4.2 program by following stepwise guidelines given in this article.
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              Tumor-targeting multi-functional nanoparticles for theragnosis: new paradigm for cancer therapy.

              Theragnostic nanoparticles (NPs) contain diagnostic and therapeutic functions in one integrated system, enabling diagnosis, therapy, and monitoring of therapeutic response at the same time. For diagnostic function, theragnostic NPs require the inclusion of noninvasive imaging modalities. Among them, optical imaging has various advantages including sensitivity, real-time and convenient use, and non-ionization safety, which make it the leading technique for theragnostic NPs. For therapeutic function, theragnostic NPs have been applied to chemotherapy, photodynamic therapy, siRNA therapy and photothermal therapy. In this review, we present a recent progress reported in the development and applications of theragnostic NPs for cancer therapy. More specifically, we will focus on theragnostic NPs related with optical imaging, highlighting promising strategies based on optical imaging techniques. Copyright © 2012 Elsevier B.V. All rights reserved.
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                Author and article information

                Journal
                Future Sci OA
                Future Sci OA
                FSO
                Future Science OA
                Future Science Ltd (London, UK )
                2056-5623
                February 2018
                13 December 2017
                : 4
                : 2
                : FSO263
                Affiliations
                [1 ]Department of Biological Sciences, Aliah University, Kolkata, 700 156, India
                [2 ]Department of Biochemistry & Molecular Biology, School of Life Sciences, Pondicherry University, Puducherry, 605 014, India
                [3 ]Interdisciplinary Programme for Life Sciences, Pondicherry University, Puducherry, 605 014, India
                [4 ]Department of Biotechnology, School of Life Sciences, Pondicherry University, Puducherry, 605 014, India
                Author notes
                *Author for correspondence: Tel.: +91 967 7847337; Fax: +91 4132655255; ruks2k2@ 123456gmail.com
                Article
                10.4155/fsoa-2017-0091
                5778387
                644dae75-8f1f-4941-a01e-3bbc764f7db8
                © 2017 Rukkumani Rajagopalan

                This work is licensed under a Creative Commons Attribution 4.0 License

                History
                : 17 July 2017
                : 06 October 2017
                Categories
                Research Article

                drug delivery,drug–polymer interaction,nanoparticles,plga,polymer degradation,stabilizers

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