scholarly journals Synthesis and characterization of a hyper-branched water-soluble β-cyclodextrin polymer

2014 ◽  
Vol 10 ◽  
pp. 2586-2593 ◽  
Author(s):  
Francesco Trotta ◽  
Fabrizio Caldera ◽  
Roberta Cavalli ◽  
Andrea Mele ◽  
Carlo Punta ◽  
...  

A new hyper-branched water-soluble polymer was synthesized by reacting β-cyclodextrin with pyromellitic dianhydride beyond the critical conditions that allow the phenomenon of gelation to occur. The molar ratio between the monomers is a crucial parameter that rules the gelation process. Nevertheless, the concentration of monomers in the solvent phase plays a key role as well. Hyper-branched β-cyclodextrin-based polymers were obtained performing the syntheses with excess of solvent and cross-linking agent, and the conditions for critical dilution were determined experimentally. A hyper-branched polymer with very high water solubility was obtained and fully characterized both as for its chemical structure and for its capability to encapsulate substances. Fluorescein was used as probe molecule to test the complexation properties of the new material.

Polymers ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 1140
Author(s):  
Silvana Alfei ◽  
Gabriella Piatti ◽  
Debora Caviglia ◽  
Anna Maria Schito

The growing resistance of bacteria to current chemotherapy is a global concern that urgently requires new and effective antimicrobial agents, aimed at curing untreatable infection, reducing unacceptable healthcare costs and human mortality. Cationic polymers, that mimic antimicrobial cationic peptides, represent promising broad-spectrum agents, being less susceptible to develop resistance than low molecular weight antibiotics. We, thus, designed, and herein report, the synthesis and physicochemical characterization of a water-soluble cationic copolymer (P5), obtained by copolymerizing the laboratory-made monomer 4-ammoniumbuthylstyrene hydrochloride with di-methyl-acrylamide as uncharged diluent. The antibacterial activity of P5 was assessed against several multi-drug-resistant clinical isolates of both Gram-positive and Gram-negative species. Except for strains characterized by modifications of the membrane charge, most of the tested isolates were sensible to the new molecule. P5 showed remarkable antibacterial activity against several isolates of genera Enterococcus, Staphylococcus, Pseudomonas, Klebsiella, and against Escherichia coli, Acinetobacter baumannii and Stenotrophomonas maltophilia, displaying a minimum MIC value of 3.15 µM. In time-killing and turbidimetric studies, P5 displayed a rapid non-lytic bactericidal activity. Due to its water-solubility and wide bactericidal spectrum, P5 could represent a promising novel agent capable of overcoming severe infections sustained by bacteria resistant the presently available antibiotics.


2019 ◽  
Vol 9 (5) ◽  
pp. 419-428
Author(s):  
Li Li ◽  
Chunjiao Pan ◽  
Zhongqiu Guo ◽  
Bingmi Liu ◽  
Hao Pan ◽  
...  

In this study, graphene oxide was synthesized using the Hummers method, and stable and homogeneous graphene oxide aqueous solutions were obtained through mechanical stirring and ultrasonic stripping. In conjunction with our previous studies, graphene oxide-loaded insoluble compound delivery systems were prepared to verify the in vivo release profiles of the graphene oxide delivery system. Several insoluble compounds including imatinib, nilotinib, erlotinib, gefitinib, and afatinib were selected for loading and in vitro graphene oxide release assays to study the non-covalent adsorption mechanisms. Computer simulations were employed for validation processes. For in vivo release assays, the T1/2 values of the poorly water soluble groups were 1.104 ± 0.18 h and the Cmax was 2.600 ± 2.06 mg/L. In previous assays, compounds with high water solubility supported by graphene oxide were released and detected in vivo. The solubility of the compound and its binding force with the carrier played a crucial role in release. The results of graphene oxide loading experiments showed that the maximum loading and entrapment efficiencies of the insoluble model compounds with similar aromatic rings were comparable. Under basic conditions, the in vitro release rates and maximum release levels of amino pyrimidine were elevated. In contrast, quinazoline release declined. Combined with computer simulations, π–π stacking was identified as the dominant mechanism for adsorption onto graphene oxide. Both hydrogen bonding and cation-π bonds played an auxiliary reinforcing role, and the two were regarded as antagonistic.


2013 ◽  
Vol 781-784 ◽  
pp. 526-530 ◽  
Author(s):  
Shao Ying Li ◽  
Chun Mei Niu ◽  
Hua Yu Zhong

Series of cationic cassia tora gum (CCTG) were synthesized using 3-chloro-2-hydroxypropyl trimethyl ammonium chloride (CHPTAC) as cationic etherifying agent, isopropanol-water solution as dispersing agent, in presence of sodium hydroxide under different reaction conditions. The optimum ratio for preparing the cationic cassia tora gum are that CHPTAC-CTG molar ratio is 0.6:1; NaOH-CHPTAC molar ratio is 1.3:1.The optimum conditions are that reaction temperature is 55°Cand reaction time is 3.5 h. The cold water solubility was improved apparently. The solution transmittance has corresponding relationship with the nitrogen content (N%) in the certain range, and the maximum transmittance is up to 87.2%. N% increased with the increase of reaction time and stable N% can be obtained in shorter reaction time at higher reaction temperature. The products were characterized by 13C-NMR. The heat resistance of CTG and CCTG were analyzed.


RSC Advances ◽  
2020 ◽  
Vol 10 (13) ◽  
pp. 7643-7653 ◽  
Author(s):  
Eunsoo Kim ◽  
Rajeev K. K. ◽  
Jaebin Nam ◽  
Junyoung Mun ◽  
Tae-Hyun Kim

We develop a polymeric binder with outstanding cell properties, and high water solubility for Si anodes by grafting a conductive PAAA onto chitosan.


2019 ◽  
Vol 70 (3) ◽  
pp. 848-852
Author(s):  
Monica Iliuta Stamate ◽  
Lacramioara Ochiuz ◽  
Daniel Timofte ◽  
Bogdan Ciuntu ◽  
Cristina Ghiciuc ◽  
...  

Polyvinyl alcohol is a biocompatible polymer used very commonly both in pharmaceutical and medical fields. Being a water-soluble polymer, it is suitable for the manufacture of hydrogels as well as cryogels used for various medical applications. The present work describes the preparation, structural and physico-mechanical characterization of polyvinyl alcohol cryogels loaded with ketoprofen. By cryogenic technique the polymeric solutions are transformed under certain conditions into porous, elastic and very compressible structures. They are able to absorb a large amount of liquids that they give off by gentle compression. The prepared cryogels were evaluated for different physical, chemical and structural properties, as following: internal morphology, equilibrium swelling ratio and mechanical testing. The cryogel structures show good elasticity and optimal swelling at different temperatures. Due to these properties the studied cryogels are suitable for use in various medical applications involving liquid absorption, mechanical resistance and anti-inflammatory effect.


2021 ◽  
Vol 14 (12) ◽  
pp. 1327
Author(s):  
Moritz Rosch ◽  
Kurt Lucas ◽  
Jozef Al-Gousous ◽  
Ulrich Pöschl ◽  
Peter Langguth

Hydrogen, as a medical gas, is a promising emerging treatment for many diseases related to inflammation and oxidative stress. Molecular hydrogen can be generated through hydrogen ion reduction by a metal, and magnesium-containing effervescent tablets constitute an attractive formulation strategy for oral delivery. In this regard, saccharide-based excipients represent an important class of potential fillers with high water solubility and sweet taste. In this study, we investigated the effect of different saccharides on the morphological and mechanical properties and the disintegration of hydrogen-generating effervescent tablets prepared by dry granulation. Mannitol was found to be superior to other investigated saccharides and promoted far more rapid hydrogen generation combined with acceptable mechanical properties. In further product optimization involving investigation of lubricant effects, adipic acid was selected for the optimized tablet, due to regulatory considerations.


2017 ◽  
Vol 2017 ◽  
pp. 1-9 ◽  
Author(s):  
Long Chen ◽  
Xichun Peng ◽  
Jiaying Lv ◽  
Siyin Liao ◽  
Shiyi Ou ◽  
...  

Polysaccharide is one of the important active ingredients of Cantharellus cibarius. The aims of this work were to analyze preliminary characterization and to investigate immunostimulating activity of a novel water-soluble neutral polysaccharide named JP1, which was purified from the fruiting body of Cantharellus cibarius using DEAE-FF chromatography and Sephadex G-100 chromatography. The characteristics of JP1 were determined by HPGPC, FT-IR spectra, gas chromatography, and Congo Red Method. Immunostimulating activity of JP1 was investigated in RAW264.7 cells. Results indicated that JP1 consisted of L-Arabinose, D-Mannose, D-Glucose, and D-Galactose in a molar ratio of 1 : 1.06 : 1.95 : 1.17 with a molecular weight of 336 kDa. JP1 is nontoxic to RAW264.7 cells at this concentration range (62.5–1000 μg/mL). Furthermore, JP1 can promote mouse peritoneal macrophages to secrete NO and enhance the secretion of macrophages’ cytokines IL-6 in RAW264.7 cells. These results suggested that JP1 could have potential immunostimulating activity applications as medicine or functional food.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (9) ◽  
pp. 465 ◽  
Author(s):  
Griffin Pauli ◽  
Wei-Lun Tang ◽  
Shyh-Dar Li

A large proportion of pharmaceutical compounds exhibit poor water solubility, impacting their delivery. These compounds can be passively encapsulated in the lipid bilayer of liposomes to improve their water solubility, but the loading capacity and stability are poor, leading to burst drug leakage. The solvent-assisted active loading technology (SALT) was developed to promote active loading of poorly soluble drugs in the liposomal core to improve the encapsulation efficiency and formulation stability. By adding a small volume (~5 vol%) of a water miscible solvent to the liposomal loading mixture, we achieved complete, rapid loading of a range of poorly soluble compounds and attained a high drug-to-lipid ratio with stable drug retention. This led to improvements in the circulation half-life, tolerability, and efficacy profiles. In this mini-review, we summarize our results from three studies demonstrating that SALT is a robust and versatile platform to improve active loading of poorly water-soluble compounds. We have validated SALT as a tool for improving drug solubility, liposomal loading efficiency and retention, stability, palatability, and pharmacokinetics (PK), while retaining the ability of the compounds to exert pharmacological effects.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 772 ◽  
Author(s):  
Songbai Zhang ◽  
Vega Lloveras ◽  
Daniel Pulido ◽  
Flonja Liko ◽  
Luiz F. Pinto ◽  
...  

Finding alternatives to gadolinium (Gd)-based contrast agents (CA) with the same or even better paramagnetic properties is crucial to overcome their established toxicity. Herein we describe the synthesis and characterization of entirely organic metal-free paramagnetic macromolecules based on biocompatible oligoethylene glycol dendrimers fully functionalized with 5 and 20 organic radicals (OEG Gn-PROXYL (n = 0, 1) radical dendrimers) with the aim to be used as magnetic resonance imaging (MRI) contrast agents. Conferring high water solubility on such systems is often a concern, especially in large generation dendrimers. Our approach to overcome such an issue in this study is by synthesizing dendrimers with highly water-soluble branches themselves. In this work, we show that the highly water-soluble OEG Gn-PROXYL (n = 0, 1) radical dendrimers obtained showed properties that convert them in good candidates to be studied as contrast agents for MRI applications like diagnosis and follow-up of infectious diseases, among others. Importantly, with the first generation radical dendrimer, a similar r1 relaxivity value (3.4 mM−1s−1) in comparison to gadolinium-diethylenetriamine pentaacetic acid (Gd-DTPA) used in clinics (3.2 mM−1s−1, r.t. 7T) has been obtained, and it has been shown to not be cytotoxic, avoiding the toxicity risks associated with the unwanted accumulation of Gd in the body.


2021 ◽  
Vol 58 (2) ◽  
pp. 88-96
Author(s):  
Dominic Byrne ◽  
Geert Boeije ◽  
Ian Croft ◽  
Gerd Hüttmann ◽  
Gerard Luijkx ◽  
...  

Abstract Questions and potential misperceptions have arisen about the potential contribution of liquid detergent capsules to the environmental microplastics issue. The film of these detergents is highly water soluble, also in cold water, as it must fully dissolve during every type of washing process. Water-soluble grades of polyvinyl alcohol, the most commonly used detergent capsule film material, are recognised to be biodegradable. In the current paper, adequate biodegradability is confirmed by means of ready biodegradation screening tests, across a range of polyvinyl alcohol detergent grade films. The high water solubility in itself implies that detergent capsule films are not within the microplastic scope. Furthermore, their biodegradability ensures there is no concern for persistence or accumulation in the environment.


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