The evolution of polymer conjugation and drug targeting for the delivery of proteins and bioactive molecules

2020 ◽  
Author(s):  
Antonella Grigoletto ◽  
Tommaso Tedeschini ◽  
Elena Canato ◽  
Gianfranco Pasut
Keyword(s):  
Drug Targeting ◽  
Bioactive Molecules ◽  
Polymer Conjugation

scholarly journals Extracellular Vesicles—Connecting Kingdoms

2019 ◽  
Vol 20 (22) ◽  
pp. 5695 ◽  
Author(s):  
Eric Woith ◽  
Gregor Fuhrmann ◽  
Matthias F. Melzig
Keyword(s):  
Extracellular Vesicles ◽  
Drug Targeting ◽  
Plant Diseases ◽  
Bioactive Molecules ◽  
Biological Research ◽  
Animal Cells ◽  
Comprehensive Overview ◽  
Comprehensive Knowledge ◽  
Applied Biology

It is known that extracellular vesicles (EVs) are shed from cells of almost every type of cell or organism, showing their ubiquity in all empires of life. EVs are defined as naturally released particles from cells, delimited by a lipid bilayer, and cannot replicate. These nano- to micrometer scaled spheres shuttle a set of bioactive molecules. EVs are of great interest as vehicles for drug targeting and in fundamental biological research, but in vitro culture of animal cells usually achieves only small yields. The exploration of other biological kingdoms promises comprehensive knowledge on EVs broadening the opportunities for basic understanding and therapeutic use. Thus, plants might be sustainable biofactories producing nontoxic and highly specific nanovectors, whereas bacterial and fungal EVs are promising vaccines for the prevention of infectious diseases. Importantly, EVs from different eukaryotic and prokaryotic kingdoms are involved in many processes including host-pathogen interactions, spreading of resistances, and plant diseases. More extensive knowledge of inter-species and interkingdom regulation could provide advantages for preventing and treating pests and pathogens. In this review, we present a comprehensive overview of EVs derived from eukaryota and prokaryota and we discuss how better understanding of their intercommunication role provides opportunities for both fundamental and applied biology.

Cardiological Biopharmaceuticals in the Conception of Drug Targeting Delivery: Practical Results and Research Perspectives

Acta Naturae ◽  
2012 ◽  
Vol 4 (3) ◽  
pp. 72-81 ◽  
Author(s):  
A. V. Maksimenko
Keyword(s):  
Cell Adhesion Molecules ◽  
Drug Targeting ◽  
Interventional Procedures ◽  
Target Localization ◽  
Clinical Use ◽  
Protein Conjugates ◽  
Research Perspectives ◽  
Significant Interest ◽  
Targeting Delivery ◽  
Molecular Sizes

The results of the clinical use of thrombolytic and antithrombotic preparations developed on the basis of protein conjugates obtained within the framework of the conception of drug targeting delivery in the organism are considered. A decrease has been noted in the number of biomedical projects focused on these derivatives as a result of various factors: the significant depletion of financial and organizational funds, the saturation of the pharmaceutical market with preparations of this kind, and the appearance of original means for interventional procedures. Factors that actively facilitate the conspicuous potentiation of the efficacy of bioconjugates were revealed: the biomedical testing of protein domains and their selected combinations, the optimization of molecular sizes for the bioconjugates obtained, the density of target localization, the application of cell adhesion molecules as targets, and the application of connected enzyme activities. Enzyme antioxidants and the opportunity for further elaboration of the drug delivery conception via the elucidation and formation of therapeutic targets for effective drug reactions by means of pharmacological pre- and postconditioning of myocardium arouse significant interest.

Anticancer Nano Formulation of Imatinib with Chitosan Polymer

2019 ◽  
Vol 9 (01) ◽  
pp. 58-64
Author(s):  
Senthilnathan B ◽  
Billy Graham R ◽  
Chaarmila Sherin C ◽  
Vivekanandan K ◽  
Bhavya E
Keyword(s):  
Drug Release ◽  
Drug Targeting ◽  
Bone Marrow Failure ◽  
Lymphoblastic Leukemia ◽  
Release Profile ◽  
Nano Particles ◽  
Drug Release Profile ◽  
Study Results ◽  
Mast Cell Disease ◽  
Nano Formulation

Objective: Drug targeting is the capacity of the dosage form. In which the therapeutic agent acts specifically to desired site of action in the non-targeted tissue with the help of Nano particles is called as the drug targeting. IMATINIB is a used to treat cancer by chemo therapy. Cancers like chronic myeloid leukemia cancer (CML) and acute lymphoblastic leukemia cancer (ALL) and other specific types of gastrointestinal stromal cell tumor (GIST) systemic mast cell disease and Bone marrow failure disorder. It is administered by oral root. For ATP, Tyrosine kinase is act as a binding site. Methodology: The drug IMATINIB is loaded in the polymer chitosan, poly-(D) glucosamine is a bio compactible, bio degradable, nontoxic, antimicrobial and soluble in solvents. This preparation is done by emulsion-droplet coalescence method. Content of the Drug, Size of the particle and Zeta potential, Encapsulation efficiency and Drug release testing are described for this formulation in this study. Results: The Imatinib Nano particles were formulated and evaluated for its invitro drug release profile. Based on the invitro drug release profile of Imatinib nano particles formulation (INP1 – INP5) formulation INP3 was selected as the best formulation in which the particle size was 285.9nm. The invitro % drug release of INP3 formulation was 99.76 ± 0.82 and it was found to be the suitable formulation to manage the cancer. Conclusion: Hence it is concluded that the newly formulated controlled release nanoparticle drug delivery system of Imatinib may be idol and effective by allowing the drug to release continuously for 24 hrs.

Bifluoride Ion Mediated SuFEx Trifluoromethylation of Sulfonyl Fluorides and Iminosulfur Oxydifluorides

2018 ◽  
Author(s):  
Christopher J. Smedley ◽  
Bing Gao ◽  
Suhua Li ◽  
Qinheng Zheng ◽  
Andrew Molino ◽  
...  
Keyword(s):  
Breast Cancer Cells ◽  
Catalytic Mechanism ◽  
Bioactive Molecules ◽  
Chromatographic Purification ◽  
Rapid Exchange ◽  
Nucleophilic Displacement ◽  
Sulfur Fluoride ◽  
Reactions With Nucleophiles ◽  
New Generation ◽  
Selection Of

Sulfur-Fluoride Exchange (SuFEx) is the new generation click chemistry transformation exploiting the unique properties of S-F bonds and their ability to undergo near-perfect reactions with nucleophiles. We report here the first SuFEx based protocol for the efficient synthesis of pharmaceutically important triflones and bis(trifluoromethyl)sulfur oxyimines from the corresponding sulfonyl fluorides and iminosulfur oxydifluorides, respectively. The new protocol involves the rapid exchange of the S-F bond with trifluoromethyltrimethylsilane (TMSCF<sub>3</sub>) upon activation with potassium bifluoride in anhydrous DMSO. The reaction tolerates a wide selection of substrates and proceeds under mild conditions without need for chromatographic purification. A tentative catalytic mechanism is proposed supported by DFT calculations, involving formation of the free trifluoromethyl anion followed by nucleophilic displacement of the S-F through a five-coordinate intermediate. The preparation of a benzothiazole derived bis(trifluoromethyl)sulfur oxyimine with cytotoxic selectivity for MCF7 breast cancer cells demonstrates the utility of this methodology for the late-stage functionalization of bioactive molecules.<br>

Reductive Cleavage of Secondary Sulfonamides: Converting Terminal Functional Groups into Versatile Synthetic Handles

2019 ◽  
Author(s):  
Patrick Fier ◽  
Suhong Kim ◽  
Kevin M. Maloney
Keyword(s):  
Functional Groups ◽  
Late Stage ◽  
Reductive Cleavage ◽  
Bioactive Molecules ◽  
General Method

Sulfonamides are pervasive in drugs and agrochemicals, yet are typically considered as terminal functional groups rather than synthetic handles. To enable the general late-stage functionalization of secondary sulfonamides, we have developed a mild and general method to reductively cleave the N-S bonds of sulfonamides to generate sulfinates and amines, components which can further react <i>in-situ</i> to access a variety of other medicinally relevant functional groups. The utility of this platform is highlighted by the selective manipulation of several complex bioactive molecules.

Sign in / Sign up

Export Citation Format

Share Document