scholarly journals HPMA-Based Polymer Conjugates for Repurposed Drug Mebendazole and Other Imidazole-Based Therapeutics

Polymers ◽  
2021 ◽  
Vol 13 (15) ◽  
pp. 2530
Author(s):  
Martin Studenovský ◽  
Anna Rumlerová ◽  
Libor Kostka ◽  
Tomáš Etrych
Keyword(s):  
Chemical Properties ◽  
Drug Repurposing ◽  
Water Soluble ◽  
Biologically Active ◽  
Lysosomal Hydrolases ◽  
Polymer Carrier ◽  
Design Synthesis ◽  
Polymer Conjugates ◽  
Synthetic Strategy ◽  
Physico Chemical

Recently, the antitumor potential of benzimidazole anthelmintics, such as mebendazole and its analogues, have been reported to have minimal side effects, in addition to their well-known anti-parasitic abilities. However, their administration is strongly limited owing to their extremely poor solubility, which highly depletes their overall bioavailability. This study describes the design, synthesis, and physico-chemical properties of polymer-mebendazole nanomedicines for drug repurposing in cancer therapy. The conjugation of mebendazole to water-soluble and biocompatible polymer carrier was carried out via biodegradable bond, relying on the hydrolytic action of lysosomal hydrolases for mebendazole release inside the tumor cells. Five low-molecular-weight mebendazole derivatives, differing in their inner structure, and two polymer conjugates differing in their linker structure, were synthesized. The overall synthetic strategy was designed to enable the modification and polymer conjugation of most benzimidazole-based anthelmintics, such as albendazole, fenbendazole or albendazole, besides the mebendazole. Furthermore, the described methodology may be suitable for conjugation of other biologically active compounds with a heterocyclic N-H group in their molecules.

Amorphous and Crystalline Particulates: Challenges and Perspectives in Drug Delivery

2017 ◽  
Vol 23 (3) ◽  
pp. 350-361 ◽  
Author(s):  
Hisham Al-Obaidi ◽  
Mridul Majumder ◽  
Fiza Bari
Keyword(s):  
Crystal Engineering ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Chemical Properties ◽  
Pharmaceutical Product ◽  
Water Soluble ◽  
Amorphous Form ◽  
Physico Chemical ◽  
Water Soluble Drugs ◽  
Amorphous Drug

Crystalline and amorphous dispersions have been the focus of academic and industrial research due to their potential role in formulating poorly water-soluble drugs. This review looks at the progress made starting with crystalline carriers in the form of eutectics moving towards more complex crystalline mixtures. It also covers using glassy polymers to maintain the drug as amorphous exhibiting higher energy and entropy. However, the amorphous form tends to recrystallize on storage, which limits the benefits of this approach. Specific interactions between the drug and the polymer may retard this spontaneous conversion of the amorphous drug. Some studies have shown that it is possible to maintain the drug in the amorphous form for extended periods of time. For the drug and the polymer to form a stable mixture they have to be miscible on a molecular basis. Another form of solid dispersions is pharmaceutical co-crystals, for which research has focused on understanding the chemistry, crystal engineering and physico-chemical properties. USFDA has issued a guidance in April 2013 suggesting that the co-crystals as a pharmaceutical product may be a reality; but just not yet! While some of the research is still oriented towards application of these carriers, understanding the mechanism by which drug-carrier miscibility occurs is also covered. Within this context is the use of thermodynamic models such as Flory-Huggins model with some examples of studies used to predict miscibility.

scholarly journals Status and Speciation of Silicon and Its Interaction with Physico-Chemical Properties

2021 ◽  
pp. 1-11
Author(s):  
Isaiah Ufuoma Efenudu ◽  
Ehi Robert Orhue ◽  
Ogochukwu Jennifer Ikeh ◽  
Michael Aimiesomon Erhayimwen ◽  
Blessing James
Keyword(s):  
Organic Matter ◽  
Acidic Medium ◽  
Soil Depth ◽  
Chemical Properties ◽  
Water Soluble ◽  
Sequential Fractionation ◽  
Soil Redox ◽  
Parent Materials ◽  
Physico Chemical ◽  
Negative Effect

The effectiveness of three different extractants soil mixtures—HCl, HCl + H2S04, and DTPA-TEA, in order to determine Si from soil and the forms of Silicon as influenced by different parent materials under acidic medium. Seven forms of Silicon; namely water soluble, specifically adsorbed, oxides bound, organic matter bound, exchangeable, residual, total viz sequential fractionation. Extractable Si value established in this study was (50.0 mg kg-1), indicating negative effect on plant physiology. The physico-chemical properties decreased significantly with increase in soil depth vs soil parent materials. In addition, the forms of Si in the parent materials decreased in the pattern RES, bound residual fractions > EXC, soluble & exchangeable fractions > OM, organic matter fraction. Among the properties the silt fraction, pH & OM significantly and positively correlated with the forms of silicon, with negative correlation vs clay which maybe due to silicon adsorption by clayey fraction of the soil (redox). Therefore the soil maybe be maintained and conserved for farming activities.

scholarly journals Physico-chemical properties of the water-soluble C70-tris-malonic solutions

2015 ◽  
Vol 211 ◽  
pp. 487-493 ◽  
Author(s):  
Olga S. Manyakina ◽  
Konstantin N. Semenov ◽  
Nikolay A. Charykov ◽  
Natalia M. Ivanova ◽  
Viktor A. Keskinov ◽  
...  
Keyword(s):  
Chemical Properties ◽  
Water Soluble ◽  
Physico Chemical

scholarly journals Physico-chemical Standardization of NPCF (Non-Pharmacopoeial Compound Formulation) Use in Diabetes mellitus

2019 ◽  
Vol 9 (1) ◽  
pp. 154-158
Author(s):  
Reesha Ahmed ◽  
Naeem Ahmad Khan
Keyword(s):  
Diabetes Mellitus ◽  
Petroleum Ether ◽  
Chemical Study ◽  
Quality Parameters ◽  
Water Soluble ◽  
Biologically Active ◽  
Herbal Drugs ◽  
Physico Chemical ◽  
Tap Density ◽  
Quality Material

Background: Variety of reasons has been cited for the need for scientific evaluation and standardization of herbal drugs. Three methods, viz., activity-based standardization, determination of biologically active compound and standardization of herbal drugs on various physical, chemical and other parameters were found to be suitable and practically applicable. Phytochemical investigations along with biological screening to understand the therapeutic dynamics of medicinal plants etc. will help in developing quality parameters and help in the standardization and establish for authenticity and quality. Material and methods: Standardization was made on the basis of physicochemical and analytical parameters laid down by National Unani Pharmacopoeia Committee (Anonymous, 2007). Results: The parameters studied includes alcohol soluble content 15.34±0.48    water soluble content  18.27±0.38,  successive extractive values viz. petroleum ether 7.60±0.05 , diethyl ether 1.24±0.02, chloroform 2.24± 0.04 , acetone 4.74±0.02, alcohol 8.51±0.06  , and aqueous 4.20±0.05, non- successive extractive values viz. petroleum ether 6.70±0.06, chloroform  7.70±0.06, alcohol16.15± 0.03 and aqueous 10.65±0.03, total ash  5.50±0.28   , acid   insoluble   ash  2.33±0.33, water soluble ash 1.16±0.16    , moisture   content 7.30±0.12 , Bulk density 0.419±0.005 (pour density) and 0.74±0.01 (Tap density), pH values of 1% solution 4.89±0.01 and 10% solution  4.69±0.005. The qualitative analysis of various phytochemicals was estimated that revealed the presence of alkaloid, carbohydrate, flavonoids, protein, starch, phenols, tannin, sterols, amino acid and resin. The TLC profile of the extracts of non-pharmacopoeial Compound Formulation was also performed which confirms various biomolecules in it.. Conclusion: This study helps in determining the quality and purity of NPCF which is use in Diabetes mellitus. Keywords: Standardization, Non-Pharmacopoeial Compound formulation, Physico-chemical study

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 Gelatin: sources, preparation and application in food and biomedicine

2020 ◽  
pp. 28-46
Author(s):  
Elvira Shatabayeva ◽  
Grigoriy Mun ◽  
Yerengaip Shaikhutdinov ◽  
Vitaliy Khutoryanskiy
Keyword(s):  
Pharmaceutical Industry ◽  
Food Packaging ◽  
Chemical Properties ◽  
Essential Amino Acids ◽  
Biologically Active ◽  
Wound Dressings ◽  
Human Gastrointestinal Tract ◽  
Physico Chemical ◽  
Anti Cancer ◽  
Cell Adhesion And Proliferation

Gelatin is a proteinaceous substance composed of all the essential amino acids (except tryptophan) and derived from collagen using a hydrolysis technique. Hydrogels and modified composites based on gelatin are widely used in the food industry, biomedicine, pharmaceutical industry and food packaging materials due to their biocompatibility, biodegradability, nonimmunogenicity and ability to stimulate cell adhesion and proliferation. Gelatin can absorb 5-10 times its weight of water and is the main ingredient of hard and soft capsules in pharmaceutical industry. It melts above 30°C and easily releases biologically active compounds, nutrients and drugs in human gastrointestinal tract. In addition, gelatin contains arginine-glycine-asparagine RGD-sequences in the polymer structure and contributes to various functions such as antioxidant, anti-hypertensive, anti-microbial, tissue regeneration, wound healing, enhances bone formation and anti-cancer therapy. This article reports a brief overview of gelatin sources, gelatin preparation processes and its physico-chemical properties, as well as advances in the preparation of gelatin-based composite materials and hydrogels for tissue engineering, drug delivery, wound dressings, active packaging using various cross-linking techniques.

scholarly journals Impact of Resistant Maltodextrin Addition on the Physico-Chemical Properties in Pasteurised Orange Juice

Foods ◽  
2020 ◽  
Vol 9 (12) ◽  
pp. 1832
Author(s):  
Elías Arilla ◽  
Marta Igual ◽  
Javier Martínez-Monzó ◽  
Pilar Codoñer-Franch ◽  
Purificación García-Segovia
Keyword(s):  
Particle Size ◽  
Particle Size Distribution ◽  
Size Distribution ◽  
Orange Juice ◽  
Chemical Properties ◽  
Water Soluble ◽  
Soluble Solids ◽  
Soluble Fibre ◽  
Physico Chemical ◽  
Resistant Maltodextrin

Resistant maltodextrin (RMD) is a water-soluble fibre that can be fermented in the colon and exert prebiotic effects. Therefore, its addition to food and beverage products could be beneficial from both technological and nutritional viewpoints. However, to date, most studies have focused on the stability of the prebiotic fibre rather than its impact in the original food matrices. Therefore, this work aimed to evaluate the addition of RMD on the physico-chemical properties of pasteurised orange juice (with and without pulp). °Brix, pH, acidity, particle size distribution, density, turbidity, rheology, and colour were measured in orange juices with increasing RMD concentrations (2.5, 5, and 7.5%). Control samples without RMD were also prepared. RMD added soluble solids to the orange juice, affecting the °Brix, density, turbidity, and rheology. Slight colour differences were observed, and lower citric acid content was achieved because of orange juice replacement with RMD. Differences in particle size distribution were exclusively because of pulp content. Further studies are needed to elucidate if potential consumers will appreciate such physico-chemical changes in organoleptic terms.

scholarly journals Reconstitution properties of biologically active polymersomes after cryogenic freezing and a freeze-drying process

RSC Advances ◽  
2018 ◽  
Vol 8 (45) ◽  
pp. 25436-25443 ◽  
Author(s):  
Robert Ccorahua ◽  
Silvia Moreno ◽  
Hannes Gumz ◽  
Karin Sahre ◽  
Brigitte Voit ◽  
...  
Keyword(s):  
Membrane Permeability ◽  
Freeze Drying ◽  
Chemical Properties ◽  
Biologically Active ◽  
Enzymatic Reactions ◽  
Drying Process ◽  
Physico Chemical ◽  
And Storage

Polymersomes can retain their physico-chemical properties and membrane permeability for enzymatic reactions after lyophilization or cryogenic freezing and storage.

scholarly journals Natural Sesquiterpene Lactones as Renewable Chemical Materials for New Medicinal Products

2013 ◽  
Vol 15 (3) ◽  
pp. 163 ◽  
Author(s):  
S.M. Adekenov
Keyword(s):  
Chemical Modification ◽  
Sesquiterpene Lactones ◽  
Physiological Activity ◽  
Chemical Properties ◽  
Water Soluble ◽  
Biologically Active ◽  
Isolation And Purification ◽  
Environmentally Safe ◽  
Renewable Material ◽  
Derivatives Of

<p>Literature data and own research results on the technology for isolating natural sesquiterpene lactones such as arglabin, alantolactone, artemisinin, grosheimin, isoalantolactone, parthenolide, santonin and potential possibilities of their use as renewable material for obtaining new compounds as well as biologically active derivatives are generalized in this review. Sesquiterpene lactones from plants are promising sources for the development and practical application of new original medical products possessing antitumor, anti-inflammatory, antimalarial, antiulcer, antiviral and immune-stimulating action. The technology for isolating sesquiterpene lactones is based on the extraction of raw plant material by different organic solvents with the subsequent chromatographic purification. The effective and environmentally safe technology for isolation and purification of sesquiterpene lactone arglabin from <em>Artemisia glabella</em> Kar. et Kir. by the СО<sub>2</sub>-extraction method is developed. Thereat, it was experimentally determined that the method for isolating arglabin from CO<sub>2</sub> extract of <em>Artemisia glabella</em> Kar. et Kir. using centrifugal partition chromatography is effective for preparative isolation of the active substance and its manufacturing application. It is practically important to obtain water-soluble derivatives of biologically active sesquiterpene lactones and also to use the nanotechnology achievements for directed transportation of a molecule of the medicine in the human body thereby reducing toxicity of an active component. Promising direction is chemical modification of molecules in sesquiterpene lactones which are renewable material for obtaining new derivatives, thanks to which it becomes possible to solve two problems at the same time. Firstly, these researches help to obtain derivatives with higher biological activity or improved physical and chemical properties. Secondly, these researches enable us to disclose the mechanism of action of different medicines within the framework of “structure-activity” correlation. The article presents the literature data and own results on chemical modification of sesquiterpene lactones of alantolactone, arglabin, artemisinin, grosheimin, isoalantolactone, parthenolide and santonin. Various reactions on functional groups of these molecules were used to obtain a number of new derivatives of sesquiterpene lactones containing haloid-, pyrazole-, triazole-, amino-, dialkylamino-, hydroxy-, dialkyl phosphonate- and cyclopropane groups, which have shown high physiological activity.</p>

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