scholarly journals Micelle-forming HPMA copolymer conjugates of ritonavir bound via a pH-sensitive spacer with improved cellular uptake designed for enhanced tumor accumulation

2016 ◽  
Vol 4 (47) ◽  
pp. 7620-7629 ◽  
Author(s):  
E. Koziolová ◽  
D. Machová ◽  
R. Pola ◽  
O. Janoušková ◽  
P. Chytil ◽  
...  
Keyword(s):  
Chemical Characterization ◽  
Controlled Drug Release ◽  
Biological Evaluation ◽  
Hpma Copolymer ◽  
Design Synthesis ◽  
Drug Conjugates ◽  
Physico Chemical ◽  
Tumor Accumulation ◽  
Polymer Drug Conjugates ◽  
Hpma Copolymer Conjugates

We describe design, synthesis, physico-chemical characterization and preliminary biological evaluation of micelle-forming polymer drug conjugates with controlled drug release intended for tumor treatment.

scholarly journals Polymeric Nanogels as Drug Delivery Systems

2018 ◽  
pp. S305-S317 ◽  
Author(s):  
J. KOUSALOVÁ ◽  
T. ETRYCH
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Tumor Tissue ◽  
Controlled Drug Delivery ◽  
Biological Evaluation ◽  
Polymer Nanoparticles ◽  
Biologically Active ◽  
Design Synthesis ◽  
Physico Chemical ◽  
Solid Tumor Tissue

The present review focuses on the description of the design, synthesis and physico-chemical and biological evaluation of polymer nanogels. Nanogels are robust swollen cross-linked polymer nanoparticles that can be used as highly efficient and biodegradable carriers for the transport of drugs in controlled drug delivery. In this article, various types of nanogels are described and methods for their preparation discussed. The possibility of using synthesized nanosystems for targeting are reviewed to show the potential of tailored structures to reach either solid tumor tissue or direct tumor cells. Finally, the methods for encapsulation or attachment of biologically active molecules, e.g. drugs, proteins, are described and compared.

scholarly journals Polymer conjugates with potential biological activity based on new derivatives of 2-mercaptobenzoxazole-synthesis and characterization

2013 ◽  
Vol 11 (11) ◽  
pp. 1808-1815 ◽  
Author(s):  
Rǎdiţa Aparaschivei ◽  
Valeriu Şunel ◽  
Mihaela Holban ◽  
Marcel Popa ◽  
Jacques Desbrieres
Keyword(s):  
Controlled Drug Release ◽  
Biologically Active ◽  
Synthesis And Characterization ◽  
Polymeric Support ◽  
Polymer Conjugates ◽  
Drug Conjugates ◽  
Laboratory Screening ◽  
Ft Ir ◽  
Polymer Drug Conjugates ◽  
Derivatives Of

AbstractNew potentially biologically active compounds derived from 2-mercapto-benzoxazole were synthesized and coupled on polymeric support of poly (maleic anhydride-alt-vinyl acetate) for the preparation of polymer-drug conjugates with controlled drug release. All compounds were characterized by elemental and spectroscopy (FT-IR, 1H-NMR) analysis. The toxicological tests recommend the products for further laboratory screening.

Design, Synthesis, and Biological Evaluation of Antibody−Drug Conjugates Comprised of Potent Camptothecin Analogues

2009 ◽  
Vol 20 (6) ◽  
pp. 1242-1250 ◽  
Author(s):  
Patrick J. Burke ◽  
Peter D. Senter ◽  
David W. Meyer ◽  
Jamie B. Miyamoto ◽  
Martha Anderson ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Synthesis And Biological Evaluation ◽  
Camptothecin Analogues ◽  
Antibody Drug

Physico-chemical characterization and biological evaluation of two fibroin materials

2012 ◽  
Vol 8 (11) ◽  
pp. 874-885 ◽  
Author(s):  
Antonella Motta ◽  
Paola Segnana ◽  
Lucia Verin ◽  
Silvia La Monica ◽  
Claudia Fumarola ◽  
...  
Keyword(s):  
Chemical Characterization ◽  
Biological Evaluation ◽  
Physico Chemical

scholarly journals Green and Synthetic Metallic Nanoparticles - Obtaining, Characterization and Biological Evaluation in Association with Lupeol

2020 ◽  
Vol 71 (5) ◽  
pp. 299-304
Author(s):  
Flavia Bociort ◽  
Adelina Cheveresan ◽  
Razvan Dragoi ◽  
Alina Heghes ◽  
Camelia Szuhanek ◽  
...  
Keyword(s):  
Colon Cancer ◽  
Gold Nanoparticles ◽  
Cancer Cells ◽  
Metallic Nanoparticles ◽  
Chemical Characterization ◽  
Biological Evaluation ◽  
Colon Cancer Cells ◽  
Lemon Balm ◽  
Physico Chemical ◽  
Average Size

The field of metal nanotechnology continues to draw the attention of researchers from different areas due to the outstanding properties of nanoparticles. The main aims of this research were to obtain and to study two types of gold nanoparticles; different obtaining pathways (the chemical synthesis and the biosynthesis based on an aqueous extract of lemon balm) were involved in this research. The chemically synthesized nanoparticles were loaded with lupeol. After a preliminary physico-chemical characterization, the compounds obtained were tested in order to evaluate the effects on the viability of colon cancer cells. The formulation of these new gold nanoparticles with average size between 38 and 82 nm, with a good stability against the tendency to form agglomerations according to the Zeta potential values, was confirmed by UV-Vis spectra; the particles containing lupeol have show the best activity against the colon cancer cells.

Designing polymer conjugates as lysosomotropic nanomedicines

2007 ◽  
Vol 35 (1) ◽  
pp. 56-60 ◽  
Author(s):  
R. Duncan
Keyword(s):  
Drug Delivery ◽  
Clinical Trials ◽  
Molecular Mass ◽  
Anticancer Agents ◽  
Synthetic Polymer ◽  
Water Soluble ◽  
Hpma Copolymer ◽  
Polymer Conjugates ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Marriage of cell biology (the concept of ‘lysosomotropic drug delivery’) and the realization that water-soluble synthetic polymers might provide an ideal platform for targeted drug delivery led to the first synthetic polymer–drug conjugates that entered clinical trials as anticancer agents. Conceptually, polymer conjugates share many features with other macromolecular drugs, but they have the added advantage of the versatility of synthetic chemistry that allows tailoring of molecular mass and addition of biomimetic features. Conjugate characteristics must be optimized carefully to ensure that the polymeric carrier is biocompatible and that the polymer molecular mass enables tumour-selective targeting followed by endocytic internalization. The polymer–drug linker must be stable in transit, but be degraded at an optimal rate intracellularly to liberate active drug. Our early studies designed two HPMA [N-(2-hydroxypropyl)methacrylamide] copolymer conjugates containing doxorubicin that became the first synthetic polymer–drug conjugates to be tested in phase I/II clinical trials. Since, a further four HPMA copolymer–anticancer drug conjugates (most recently polymer platinates) and the first polymer-based γ-camera imaging agents followed. Polymer–drug linkers cleaved by lysosomal thiol-dependent proteases and the reduced pH of endosomes and lysosomes have been used widely to facilitate drug liberation. It is becoming clear that inappropriate trafficking and/or malfunction of enzymatic activation can lead to new mechanisms of clinical resistance. Recent studies have described HPMA copolymer conjugates carrying a combination of both endocrine and chemotherapy that are markedly more active than individual conjugates carrying a single drug. Moreover, current research is investigating novel dendritic polymer architectures and novel biodegradable polymers as drug carriers that will provide improved drug delivery and imaging probes in the future. The present paper reviews the clinical status of polymeric anticancer agents, the rationale for the design of polymer therapeutics and discusses the benefits and challenges of lysosomotropic delivery.

scholarly journals Design, synthesis, chemical characterization, biological evaluation, and docking study of new 1,3,4-oxadiazole homonucleoside analogs

2020 ◽  
Vol 39 (8) ◽  
pp. 1088-1107 ◽  
Author(s):  
Az-Eddine El Mansouri ◽  
Mohamed Maatallah ◽  
Hassan Ait Benhassou ◽  
Abdeladim Moumen ◽  
Ahmad Mehdi ◽  
...  
Keyword(s):  
Chemical Characterization ◽  
Docking Study ◽  
Biological Evaluation ◽  
Design Synthesis

Design, synthesis and biological evaluation of phenol-linked uncialamycin antibody-drug conjugates

2020 ◽  
Vol 30 (1) ◽  
pp. 126782 ◽  
Author(s):  
Yam B. Poudel ◽  
Chetana Rao ◽  
Srikanth Kotapati ◽  
Madhura Deshpande ◽  
Lourdes Thevanayagam ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Antibody Drug Conjugates ◽  
Drug Conjugates ◽  
Synthesis And Biological Evaluation ◽  
Antibody Drug
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