Efficiency evaluation of the dimebon gel in experiment

2016 ◽  
Vol 10 (1) ◽  
pp. 0-0
Author(s):  
Степанова ◽  
E. Stepanova ◽  
Майорова ◽  
A. Mayorova ◽  
Хадарцев ◽  
...  

The article presents the characteristics of the Dimebon drug, different ways of drug delivery to organs and tissues. The purpose of this study was to determine the Dimebon gel effect on inflammation in experimental animals in comparison with other gels. It was found the criteria of evaluation and formulation of algorithms experiment. It was revealed the absence of systemic toxicity of the Dimebon gel, the severity of their de-congestant effect (77.04%) and a superior action with microcapsules Dimebon (69.63%). The Dimebon gel is not inferior to the Fenistil gel. This is explained by the action of the test Dimebon, because the effectiveness of gel base in 3,2 times is inferior to the subject gel. Regenerative activity the Dimebon gel is controlled burn time of rejection of the scab, which was lower by 2 days than when using the Fenistil gel and 4 days after the Dimebon gel microcapsules.

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3228
Author(s):  
Xiaotong Li ◽  
Minghong Jian ◽  
Yanhong Sun ◽  
Qunyan Zhu ◽  
Zhenxin Wang

In order to improve their bioapplications, inorganic nanoparticles (NPs) are usually functionalized with specific biomolecules. Peptides with short amino acid sequences have attracted great attention in the NP functionalization since they are easy to be synthesized on a large scale by the automatic synthesizer and can integrate various functionalities including specific biorecognition and therapeutic function into one sequence. Conjugation of peptides with NPs can generate novel theranostic/drug delivery nanosystems with active tumor targeting ability and efficient nanosensing platforms for sensitive detection of various analytes, such as heavy metallic ions and biomarkers. Massive studies demonstrate that applications of the peptide–NP bioconjugates can help to achieve the precise diagnosis and therapy of diseases. In particular, the peptide–NP bioconjugates show tremendous potential for development of effective anti-tumor nanomedicines. This review provides an overview of the effects of properties of peptide functionalized NPs on precise diagnostics and therapy of cancers through summarizing the recent publications on the applications of peptide–NP bioconjugates for biomarkers (antigens and enzymes) and carcinogens (e.g., heavy metallic ions) detection, drug delivery, and imaging-guided therapy. The current challenges and future prospects of the subject are also discussed.


2022 ◽  
Author(s):  
Nafeesa Khatoon ◽  
Zefei Zhang ◽  
Chunhui Zhou ◽  
Maoquan Chu

The enhanced and targeted drug delivery with low systemic toxicity and subsequent release of drugs is the major concern among researchers and pharmaceutics. Inspite of greater advancement and discoveries in...


2011 ◽  
Vol 7 (6) ◽  
pp. 665-673 ◽  
Author(s):  
Debbie Liao ◽  
Ze Liu ◽  
Wolfgang Wrasidlo ◽  
Tingmei Chen ◽  
Yunping Luo ◽  
...  

2021 ◽  
Author(s):  
Victoria O. Shipunova ◽  
Elena N. Komedchikova ◽  
Anna S. Sogomonyan ◽  
Polina A. Kotelnikova ◽  
Maxim P. Nikitin ◽  
...  

Abstract The conventional methods of treating cancer with chemo- and radiotherapy present plenty of serious problems, such as low therapeutic index and high systemic toxicity. The advanced cancer treatment strategies utilize nanoformulations of drugs that can enter a tumor due to the enhanced permeability and retention (EPR) effect. However, EPR fails in the treatment of several human diseases. Mainstream biomedical studies are focused on creating the drugs that would enter the tumor with higher effectiveness and require smaller doses for administration. A two-stage drug delivery system is an encouraging alternative solution. At first, the primary, non-toxic targeting module is delivered to the tumor cells, followed by injection of the second complementary targeting module at a considerably lower dose, thus decreasing systemic toxicity. To meet the challenge, we have developed a two-stage drug delivery system (DDS), mediated by the high-affinity binding of the Barnase*Barstar protein pair. Barnase and Barstar act as lego bricks linking the first and the second modules on the surface of the cancer cell. Barnase (12 kDa) is a natural ribonuclease from Bacillus amyloliquefaciens, while Barstar (10 kDa) is its natural inhibitor. The Barnase*Barstar is one of the strongest known protein*protein complexes with Kaff = 1014 M−1 exhibiting extraordinarily stability in severe conditions. Artificial scaffold polypeptide DARPin9_29 genetically fused with Barstar served is a first module of the developed two-step DDS. DARPin9_29 (14 kDa) specifically recognizes the tumor marker HER2 overexpressed on human breast cancer cells. As a second module, a therapeutic nano-cargo was developed based on fluorescent polymer PLGA nanoparticles loaded with diagnostic Nile Blue dye and the chemotherapeutic drug doxorubicin. This nano-PLGA structure was covalently coupled to Barnase. We showed two-stage efficient labeling of HER2-overexpressing cancer cells using the first non-toxic module DARPin9_29-Barstar and the second toxic nano-module PLGA-Barnase. We demonstrated the doxorubicin-induced cytotoxicity of this two-step DDS based on polymer nanoparticles and proteinaceous Barnase-Barstar interface and showed more than 10-fold therapeutic dose reduction versus free doxorubicin. We believe that the developed two-step DDS based on PLGA nano-cargo and protein interface will promote the creation of new-generation cancer treatment strategies.


2020 ◽  
Vol 26 (41) ◽  
pp. 7476-7519 ◽  
Author(s):  
Ana M.F. Phillips ◽  
Armando J.L. Pombeiro

: Transition metal complexes, of which the platinum(II) complex cisplatin is an example, have been used in medicine to treat cancer for more than 40 years. Although many successes have been achieved, there are problems associated with the use of these drugs, such as side effects and drug resistance. Converting them into prodrugs, to make them more inert, so that they can travel to the tumour site unchanged and release the drug in its active form only there, is a strategy which is the subject of much research nowadays. The new prodrugs may be activated and release the cytotoxic agent by differences in oxygen concentration or in pH, by the action of overexpressed enzymes, by differences in metabolic rates, etc., which characteristically distinguish cancer cells from normal ones, or even by the input of radiation, which can be visible light. Converting a metal complex into a prodrug may also be used to improve its pharmacological properties. In some cases, the metal complex is a carrier which transports the active drug as a ligand. Some platinum prodrugs have reached clinical trials. So far platinum, ruthenium and cobalt have been the most studied metals. This review presents the recent developments in this area, including the types of complexes used, the mechanisms of drug action and in some cases the techniques applied to monitor drug delivery to cells.


Physiology ◽  
1989 ◽  
Vol 4 (4) ◽  
pp. 146-151 ◽  
Author(s):  
G Gregoriadis

Understanding of the behavior and control of liposomes in vivo has led to their successful use as a drug delivery system in the treatment or prevention of a wide spectrum of diseases in experimental animals and, more recently, in clinical trials.


1939 ◽  
Vol 128 (850) ◽  
pp. 126-137 ◽  

For many years various experiments have been devised in order to find out whether an acquired characteristic can be inherited, but the results on the whole do not appear to have received general scientific sanction. C. P. Martin and Bradford Hill in recent years have both made surveys of this subject, but from different points of view. Martin (1937), in making a survey of the literature on the subject, points out many of the difficulties which confront the experimentalist and indicates possible causes for the apparent discrepancies in results. He also raises the possible existence of a temporary form of inheritance which obeys the Mendelian laws. Hill (1934) reviews a great deal of the work which has been done on the possibility of resistance to bacterial infection being inherited. He points out that much of this work is unconvincing, as it is very difficult in the case of bacterial infections to be quite sure that the offspring of the experimental animals have not been infected to some extent, as well as the parents. The experiments recorded in this paper have resulted from observations made in the course of our work on the propagation of Jensen’s rat sarcoma. This tumour is easily transplanted from one rat to another by subcutaneous inoculation of small grafts, and when a sensitive breed of rat is used the tumour very rarely retrogresses, provided a scrupulous technique is followed (Chambers and Scott 1930). Many years ago we noticed that the offspring of rats in which tumours had disappeared were not so susceptible to the tumour grafts as other rats of the same breed, and it seemed worth while to find out how far this apparently acquired characteristic was transmitted to the offspring. The data now recorded provide evidence in support of the view that this acquired characteristic is transmitted to the offspring to some extent.


2020 ◽  
Vol 22 (Supplement_3) ◽  
pp. iii412-iii412
Author(s):  
Taylor Dismuke ◽  
Timothy Gershon

Abstract CDK4/6 inhibition may be a promising therapy for medulloblastoma. All medulloblastoma subgroups show D-cyclin/CDK4/RB pathway activity, suggesting broad potential for efficacy. To address drug delivery and systemic toxicity limitations, we developed a nanoparticle formulation of CDK 4/6 inhibitor, palbociclib, in poly (2-oxazoline) micelles (POx-palbo). POx-palbo showed reduced systemic toxicity in transgenic mice engineered to develop medulloblastoma, allowing for higher dosing. Pharmacodynamic studies showed POx-palbo suppressed RB phosphorylation acutely and after 24hrs, the effect diminished. This inhibition produced a longer lasting suppression of SHH pathway activity, demonstrated by Gli-luc reporter tumor mice. Importantly, POx-palbo therapy, administered daily, reduced tumor growth and improved the survival of mice with medulloblastoma. While POx-palbo was clearly effective as a single agent, all mice treated with POx-palbo eventually developed progressive disease, as resistant populations of tumors cells emerged. To understand the mechanisms of resistance, we compared tumors early and late in the course of therapy. We found that after 5 days of treatment, palbociclib altered cell cycle progression to produce an extended period of S-phase and that the fractions of cell expressing the stem cell marker Olig2 were markedly increased. Based on these data, we propose that tumors respond to the initial suppressive effect of palbociclib by increasing the pool of Olig2+ stem cells, that these cells show discernably different cell cycle kinetics and are resistant to CDK4/6 inhibition. Combining POx-palbo with additional therapies that target Olig2+ stem cells, by disrupting their prolonged S-phase, or by disrupting Olig2 function, may lead to newly effective medulloblastoma treatment.


2014 ◽  
Vol 12 (3) ◽  
pp. 33-54
Author(s):  
Katarzyna Lisowska ◽  
Alexander Cortez

At the end of the year 2012, Food and Chemical Toxicology published a long-term study by Seralini et al., describing the safety evaluation of genetically modified NK603 maize and Roundup herbicide. Contrary to previous, short-term studies, this experiment revealed some negative effects of these substances on the health of experimental animals. GM feeds and Roundup generate revenue worth millions of dollars. This may be the reason why Seralini’s paper has became the subject of much heated criticism, mainly from parties linked to business and agro-biotechnology. After one year of debate, the editors of Food Chem Toxicol. decided to retract the paper, an unprecedented event given that the published article was peer-reviewed and there was no evidence of plagiarism or fraud. Here, we stress the results of Seralini’s study, discuss the methodological hints of that work and cite the commentaries on the whole situation.


2021 ◽  
Vol 18 ◽  
Author(s):  
Ritesh Kumar Tiwari ◽  
Lalit Singh ◽  
Vaibhav Rastogi

: The polyelectrolyte complexes (PECs) are adaptable definitions shaped by electrostatic interaction between biopolymers with inverse charges. Polyelectrolyte edifices comprise an exceptional class of polymeric mixtures comprising of polyions with inverse charges, which can be charged either cationically or anionically. Significant advancement has been made in the course of recent years towards new medication conveyance frameworks. The subject of broad essential and applied exploration has been on the marvel of interpolymer collaborations and polyelectrolyte complex development. Basically and applied polyelectrolytes raise on the grounds that the advantages of supportability are perceived in the scholarly world and in modern examination settings. Polyelectrolytes are a form of polymer that has endless ionizable practical arrangements. Ionized polyelectrolytes in arrangement can form a complex with oppositely charged particle called a polyelectrolyte complex. The review article emphasizes on PECs and their classification, characterization, as well as a critical analysis of the current research and applicability in drug delivery technology.


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