scholarly journals Highly Efficient Prodrugs: Design and Therapeutic Applications

2020 ◽  
Vol 36 (6) ◽  
pp. 985-1000
Author(s):  
Ashutosh Pal ◽  
Bimal Krishna Banik

Prodrug is a very powerful way for the improvement of biopharmaceutical, physicochemical, or pharmacokinetic possessions of pharmacologically dynamic mediators. Prodrug is a pharmacologically not an active compound, which can be converted into an active drug by biotransformation which is metabolic and such process the efficiency of drugs gets improved with specific target delivery. The conversion of a prodrug to drug may happen before concentration, after concentration, or at a precise part of the physique. This approach has many advantages over drug administration which is in our convention. In this review, different types of carriers, which can be used for prodrug synthesis are summarized. Examples of both marketed and investigational prodrugs from several promoieties are discussed not only for their advantages and uses but also their prospects. The purpose of this review is to introduce in detail the foundation behind the use of the prodrug methodology from past to present, and at the same time, to consider the possible consequences, which may evolve from insufficient initiation of prodrugs. Furthermore, the concept of prodrug and the classifications of prodrugs will be discussed in this article and it is expected that this review will be helpful for medicinal chemists for their research in the upcoming days.

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Jiaqi Wang ◽  
Yan Chen ◽  
Qinyao Xu ◽  
Miaomiao Cai ◽  
Qian Shi ◽  
...  

AbstractSuperhydrophobic sponges have considerable potential for oil/water separation. Most of the methods used for superhydrophobic modification of sponges require toxic or harmful solvents, which have the drawbacks of hazardous to environment, expensive, and complex to utilize. Moreover, the hydrophobic layer on the surface of sponge is often easily destroyed. In this paper, a highly efficient superhydrophobic sponge with excellent reusability was developed by using a facile, simple and environmentally friendly dopamine biomimetic bonding method. Different types of sponges, such as melamine, polyethylene or polyurethane sponge wastes, were used as raw materials to prepare superhydrophobic sponges, which possess the advantages of inexpensive and abundant. The effects of different dopamine polymerization time and different hydrophobic agent dosage on the hydrophobicity and oil absorption capacity of melamine sponges were optimized. The study results showed that the water contact angle of the superhydrophobic sponge could reach 153° with excellent organic solvent absorption capacity of 165.9 g/g. Furthermore, the superhydrophobic sponge retained approximately 92.1% of its initial absorption capacity after 35 reutilization cycles. More importantly, the dopamine biomimetic bonding superhydrophobic modification method can be used for different types of sponges. Therefore, a universally applicable, facile, simple and environmentally friendly superhydrophobic modification method for sponges was developed.


2019 ◽  
Vol 2 (1) ◽  
Author(s):  
Denise Barcelos ◽  
Karina Funabashi ◽  
Susana Mazloum ◽  
Mariana Fernandes ◽  
Leonardo Cardili

Abstract Gastrointestinal Stromal Tumors (GIST) present different types of mutations that may or may not be sensitive to specific target therapy. The laboratory procedure required to prepare histological sections traditionally demands multiple steps, making the process prone to contamination by exogenous genetic material (DNA). An eventual contamination of the biological sample with exogenous DNA may jeopardize subsequent analysis of mutations. The Short Tandem Repeat (STR) technique is frequently used in forensic science fields and presents a potential application in surgical pathology, especially in situations of suspected sample exchange. In the present study, the objective is to verify the possible contamination by exogenous DNA in gastric GIST samples and to evaluate if the presence of contamination can interfere in the detection of the mutations of interest. We assessed eight gastric GISTs by the Sanger sequencing and STR sequence analyses. Seven samples presented more than one profile, a result interpreted as contamination. Our results indicate that exogenous DNA contamination occurred in most of the samples studied and that this was more frequent in samples obtained from the slides than those obtained from the block. The presence of contamination did not inhibit the detection of the mutations of interest for a specific target therapy. Furthermore, the histologic block revealed to be more advantageously when compared to the slide for molecular pathology diagnosis.


1984 ◽  
Vol 17 (2) ◽  
pp. 89-93 ◽  
Author(s):  
Thaisa de Almeida Maria ◽  
Leny de Sousa Filardi ◽  
Zigman Brener

An electron microscopy study shows that the administration of a single dose (500 mg/kg, p.o.) of 2-amino-5-(1-methyl-5-nitro-2-imidazolyl)-1, 3, 4-thiadiazole induces in mice infected with Trypanosoma cruzi results in degenerative lesions of the intracellular stages. Ultrastructural alterations are detected as early as 6 hours after the drug administration and destruction of the parasites occurs within 18 - 36 hours. Trypomastigotes are cleared from the bloodstream 4 to 6 hours after treatment. The combined effect on both developmental stages is apparently responsible for the in vivo ejfects of this drug which is the most active drug ever tested in our laboratory in experimental Chagas' disease.


Author(s):  
Balaji O ◽  
Amita D ◽  
Sereen Rt ◽  
Navin Ap

Spinal muscular atrophy (SMA), a neurological condition which is genetically mediated is the second most common infantile disease causing morbidity and mortality next to cystic fibrosis. It is of five different types with each type having different severity outcomes. For almost three decades, only supportive measures were advocated in the treatment of SMA. Recently, Biogen’s Spinraza came out as the first disease modifying therapy to treat infantile as well as adult SMA. This review throws light on the pharmacological aspects of the drug; its approval by Food and Drug Administration and various completed clinical trials as well ongoing clinical trials.


2016 ◽  
Vol 45 (4) ◽  
pp. 1455-1466 ◽  
Author(s):  
Lígia S. Nobre ◽  
Hélia Jeremias ◽  
Carlos C. Romão ◽  
Lígia M. Saraiva

Transition metal carbonyl complexes used as CO-releasing molecules (CORMs) for biological and therapeutic applications may exhibit interesting antimicrobial activity.


Author(s):  
Jean-Marie Exbrayat ◽  
Claire Brun

In animals, the sound vibrations are captured by the auditory cells, then transformed into electrical signals and conveyed to the nervous centers where they can be interpreted such as music. A lot of studies concern the effect of sound on the auditory cells and on the brain. Nevertheless, musical vibrations also affect other cells types in several organisms. These researches being not of the same nature, they need to be classified in order to provide elements of understanding the effects of music on cell biology. A lot of works were done on the effects of music on non-auditory cells. Effects on growth, apoptosis, immune system, protein activities in animal, plant and bacterial cells have been shown. These effects are of a physiological nature and require molecules and physicochemical mechanisms. Some works were performed on vegetal or animal total organisms, others directly on cells themselves, using cell cultures. Few works concern eukaryotic unicellular organisms. Results of these studies show music and sound exert effects on the physiology. But the experiments and results are still well disparate, with effects of different types of music on organisms via auditory on non-auditory cells, sometimes involving both auditory and non-auditory cells. Whatever the large variation of results, the study of the effects of sound and especially music on the cells is a subject on the future, considering the immense possibilities offered by music in modulating physiology, with potential therapeutic applications.


Author(s):  
Kamanashis Das ◽  
Md. Yasin ◽  
Ishrak Jahan ◽  
Tahira Akter ◽  
Saiful Islam ◽  
...  

In order to prepare the sustained release tablet with levo-salbutamol sulphate we have used these excipients methylcellulose, PVPK30, magnesium stearate, talc, isopropyl alcohol, microcrystalline cellulose, lactose, HPMCK100, HPMCK4M. Here our approach was for making the sustained released matrix tablet by two ways, one is to make the tablet granules floating and the second one is by retarding the release of the levo-salbutamol sulphate from the matrix. We have already discussed the relationship with delaying the gastric transit time and the active drug absorption, if the tablet granules are floating in our introduction part. Since the above mentioned excipients are floating in nature so formulations with those excipients are supposed to be floating. We also showed a list of excipients those are used in the preparation of floating tablets. Now the second observation which was the release rate, among the three different formulations (mentioned in the introduction) we found different types of release. Since our objective is to prepare a sustained released tablet which will give a prolong release time, in that prospect two among the three formulations were disqualified (though we have not done the kinetic study). We observed desired effect in the formulation-2 during the preparation of experiment.


Nanoscale ◽  
2015 ◽  
Vol 7 (34) ◽  
pp. 14460-14468 ◽  
Author(s):  
Hyoung Won Baac ◽  
Jong G. Ok ◽  
Taehwa Lee ◽  
L. Jay Guo

We demonstrate nano-structural characteristics of carbon nanotube (CNT)–polydimethylsiloxane (PDMS) composite films that can be used as highly efficient and robust ultrasound transmitters for diagnostic and therapeutic applications.


2019 ◽  
Vol 21 (19) ◽  
pp. 5291-5297 ◽  
Author(s):  
Qiaoling Liu ◽  
Xinhui Zhao ◽  
Dongkun Yu ◽  
Haitao Yu ◽  
Yibin Zhang ◽  
...  

Two types of novel deep eutectic solvents with different functional groups were designed for highly efficient dissolution of different types of lignin.


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