scholarly journals Inclusion complexes of pesticides in aqueous solutions of methylated-β-cyclodextrin

2013 ◽  
Vol 67 (2) ◽  
pp. 231-237 ◽  
Author(s):  
Goran Petrovic ◽  
Gordana Stojanovic ◽  
Olga Jovanovic ◽  
Aleksandra Djordjevic ◽  
Ivan Palic ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Water Solubility ◽  
Inclusion Complexation ◽  
Solubility In Water ◽  
Other Substances ◽  
Poorly Soluble ◽  
Enthalpy And Entropy ◽  
Methylated Cyclodextrin ◽  
Organic Pesticides ◽  
Hplc Data

Disadvantage of some organic pesticides is their low water solubility. Among other substances, cyclodextrins and modified cyclodextrins were considered as agents for improving pesticides water solubility. The solubility of poorly soluble pesticides, dimethoate, simazine, linuron and thiram, was determined in aqueous solution of methylated-?-cyclodextrin (mbCD) by ultraviolet spectrophotometry. Methylated-?-cyclodextrin was obtained by the modified Hawort method and characterized by 1H NMR and HPLC data. The average degree of substitution was 13.8. Methylation was done either on C-2, C-3, and C-6 atoms of glucopyranose unit therefore obtained product can be assort as randomly m?CD. Solubility of the studied pesticides in aqueous solution of m?CD increases in relation to their solubility in water for dimethoate 506, for simazine167, for thiram 44, and for linuron 20 times. Reactions of dimethoate and simazine with m?CD were entropy-driven while the inclusion complexation of m?CD with the linuron and thiram were driven by both, enthalpy and entropy, as determined by calorimetric measurements. The observed solubility increment of the investigated pesticides in aqueous solution of m?CD, suggests that it can be efficiently used in pesticide solutions formulations and increase their bioavailability, and biodegradability.

scholarly journals Review: Solid Dispersion Technique for Enhancement of Solubility of Poorly Soluble Drug

2018 ◽  
Vol 6 (02) ◽  
pp. 43-52 ◽  
Author(s):  
R. Bhaskar ◽  
Monika OLA ◽  
Ravindra M. Ghongade
Keyword(s):  
Solid Dispersion ◽  
Water Solubility ◽  
Solubility In Water ◽  
Characterization Methods ◽  
Poor Solubility ◽  
Novel Drugs ◽  
Poorly Soluble ◽  
Pharmaceutical Industries ◽  
Poorly Soluble Drug ◽  
Dispersion Technique

Nearly 40% of novel drugs comes in pharmaceutical industries are showing poor capability of solubilization in water. Therefore enhancing the solubilization of such drugs in water to enhance their bioavailability be the major challenge to formulation scientists. So the preparation of solid dispersion from the drug which shows poor solubility in water with carriers having good water solubility has decrease the occurrence of such problems and increase dissolution. Hence solid dispersion found to be attention-grabbing method for solubility enhancing of drugs which showing poor solubility in water. This review, shows an overview on the different solid dispersion types, rationale, their advantages, limitations, manufacturing processes as well as its characterization methods.

scholarly journals Enhanced Solubility and Anticancer Potential of Mansonone G By β-Cyclodextrin-Based Host-Guest Complexation: A Computational and Experimental Study

Biomolecules ◽  
2019 ◽  
Vol 9 (10) ◽  
pp. 545 ◽  
Author(s):  
Mahalapbutr ◽  
Wonganan ◽  
Charoenwongpaiboon ◽  
Prousoontorn ◽  
Chavasiri ◽  
...  
Keyword(s):  
Water Solubility ◽  
Binding Free Energy ◽  
Inclusion Complexation ◽  
Host Molecule ◽  
Inclusion Complex Formation ◽  
Practical Applications ◽  
Enhanced Solubility ◽  
Poorly Soluble ◽  
Dynamics Simulations ◽  
A549 Lung

Mansonone G (MG), a plant-derived compound isolated from the heartwood of Mansonia gagei, possesses a potent antitumor effect on several kinds of malignancy. However, its poor solubility limits the use for practical applications. Beta-cyclodextrin (βCD), a cyclic oligosaccharide composed of seven (1→4)-linked α-D-glucopyranose units, is capable of encapsulating a variety of poorly soluble compounds into its hydrophobic interior. In this work, we aimed to enhance the water solubility and the anticancer activity of MG by complexation with βCD and its derivatives (2,6-di-O-methyl-βCD (DMβCD) and hydroxypropyl-βCD). The 90-ns molecular dynamics simulations and MM/GBSA-based binding free energy results suggested that DMβCD was the most preferential host molecule for MG inclusion complexation. The inclusion complex formation between MG and βCD(s) was confirmed by DSC and SEM techniques. Notably, the MG/βCDs inclusion complexes exerted significantly higher cytotoxic effect (2–7 fold) on A549 lung cancer cells than the uncomplexed MG.

scholarly journals Inclusion complexation of .BETA.-cyclodextrin with some sulfonamides in aqueous solution.

1978 ◽  
Vol 26 (4) ◽  
pp. 1162-1167 ◽  
Author(s):  
KANETO UEKAMA ◽  
FUMITOSHI HIRAYAMA ◽  
MASAKI OTAGIRI ◽  
YOUKO OTAGIRI ◽  
KEN IKEDA
Keyword(s):  
Aqueous Solution ◽  
Inclusion Complexation ◽  
Beta Cyclodextrin

scholarly journals Molecular Dynamic Simulation Analysis on the Inclusion Complexation of Plumbagin with β-Cyclodextrin Derivatives in Aqueous Solution

Molecules ◽  
2021 ◽  
Vol 26 (22) ◽  
pp. 6784
Author(s):  
Kulpavee Jitapunkul ◽  
Pisanu Toochinda ◽  
Luckhana Lawtrakul
Keyword(s):  
Aqueous Solution ◽  
Slow Release ◽  
Storage Temperature ◽  
Simulation Analysis ◽  
Inclusion Complexation ◽  
Storage Life ◽  
Release Mechanism ◽  
Guest Binding ◽  
Binding Cavity ◽  
Dynamics Simulations

Stable encapsulation of medically active compounds can lead to longer storage life and facilitate the slow-release mechanism. In this work, the dynamic and molecular interactions between plumbagin molecule with β-cyclodextrin (BCD) and its two derivatives, which are dimethyl-β-cyclodextrin (MBCD), and 2-O-monohydroxypropyl-β-cyclodextrin (HPBCD) were investigated. Molecular dynamics simulations (MD) with GLYCAM-06 and AMBER force fields were used to simulate the inclusion complex systems under storage temperature (4 °C) in an aqueous solution. The simulation results suggested that HPBCD is the best encapsulation agent to produce stable host–guest binding with plumbagin. Moreover, the observation of the plumbagin dynamic inside the binding cavity revealed that it tends to orient the methyl group toward the wider rim of HPBCD. Therefore, HPBCD is a decent candidate for the preservation of plumbagin with a promising longer storage life and presents the opportunity to facilitate the slow-release mechanism.

scholarly journals Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

2019 ◽  
Vol 28 (2) ◽  
pp. 105-114
Author(s):  
Samer K. Ali ◽  
Eman B. H. Al-Khedairy
Keyword(s):  
Polyethylene Glycol ◽  
Solid Dispersion ◽  
Water Solubility ◽  
Drug Carrier ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Drug Solubility ◽  
Scanning Calorimetry ◽  
Poorly Soluble

            Atorvastatin (ATR) is poorly soluble anti-hyperlipidemic drug; it belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs.           The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorption technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers and Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents.            All solid dispersion adsorbate (SDA) formulas  were prepared in ratios of 1:1:1  (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content,  , dissolution, crystal structure using  X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC)  studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction.                The prepared (SDA) showed significant improvement of drug solubility in all prepared formula. Best result was obtained with formula SDA12(ATR :Poloxamer407 : MAS 1:1:1) that showed 8.07 and 5.38  fold increase in solubility compared to  solubility of pure ATR and  solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improve drug solubility  and  dissolution .

Cellular membrane-anchored fluorescent probe with aggregation-induced emission characteristics for selective detection of Cu2+ ions

2017 ◽  
Vol 196 ◽  
pp. 377-393 ◽  
Author(s):  
Danni Liu ◽  
Shenglu Ji ◽  
Heran Li ◽  
Liang Hong ◽  
Deling Kong ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Cell Membrane ◽  
Water Solubility ◽  
Live Cells ◽  
Probe Design ◽  
Specific Cell ◽  
Selective Detection ◽  
High Concentration ◽  
Aggregation Induced Emission ◽  
Emissive Probes

The exploration of advanced fluorescent probes that can detect divalent copper (Cu2+) in aqueous environments and even in live organisms is particularly valuable for understanding the occurrence and development of Cu2+-related diseases. In this work, we report the design and synthesis of an aggregation-induced emission luminogen (AIEgen)-based probe (TPE-Py-EEGTIGYG) by integrating an AIEgen, TPE-Py, with a peptide, EEGTIGYG, which can selectively detect Cu2+ in both aqueous solution and live cells. Peptide EEGTIGYG has dual functionality in the probe design, namely improving water solubility and providing specific cell membrane-binding ability. TPE-Py-EEGTIGYG can self-assemble into nanoaggregates at high concentration in aqueous solution (e.g., 25 μM), which possess large fluorescence output due to the restriction of intramolecular rotation of the phenyl rings on TPE-Py. The fluorescence of the TPE-Py-EEGTIGYG nanoaggregates can be significantly quenched by Cu2+ but not by other metal ions, achieving the selective detection of Cu2+ in aqueous media. Furthermore, TPE-Py-EEGTIGYG can exist as a molecular species and is very weakly fluorescent in dilute aqueous solution (e.g., 5 μM), but can however largely switch on its fluorescence upon specifically anchoring onto the cell membrane. The emissive probes on the cell membrane can be used for the detection of Cu2+ ions that move in and out of cells with a fluorescence “turn-off” mode.

scholarly journals New Active Pharmaceutical Ingredient-Ionic Liquids (API-ILs) Derived from Indomethacin and Mebendazole

Proceedings ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 48 ◽  
Author(s):  
◽  
Emilia Tojo
Keyword(s):  
Ionic Liquids ◽  
Water Solubility ◽  
Methanesulfonic Acid ◽  
Active Pharmaceutical Ingredient ◽  
High Water ◽  
Solubility In Water ◽  
Pharmaceutical Ingredients ◽  
Low Toxicity ◽  
Low Solubility ◽  
High Water Solubility

The transformation of two solid Active Pharmaceutical Ingredients (APIs) into new ionic liquids (IL)s that incorporate APIs (API-ILs) is reported. The structures of the APIs (indomethacin and mebendazole) were selected by their susceptibility to being transformed into API-ILs (either to form the cation or the anion) and their limited bioavailability due to their low solubility in water. The counterions, such as those derived from 2-dimethylaminoethanol (DMEA), tetramethylguanidine (TMG), 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), 1,4-diazabicyclo[2.2.2] (TED), <i>p</i>-toluensulfonic acid, glycolic acid, methanesulfonic acid, and saccharin, were carefully chosen, aiming for high biocompatibility, low toxicity, and high water solubility. The synthesis was carried out by direct treatment of the API with the corresponding selected acid or base. Finally, the solubility in water of all the synthesized salts was determined.

scholarly journals The Development of Novel Organotin Anti-Tumor Drugs: Structure and Activity

1998 ◽  
Vol 5 (4) ◽  
pp. 179-188 ◽  
Author(s):  
Dick de Vos ◽  
Rudolph Willem ◽  
Marcel Gielen ◽  
Kyra E. van Wingerden ◽  
Kees Nooter
Keyword(s):  
Water Solubility ◽  
Solubility In Water ◽  
In Vivo Testing ◽  
Polar Substituents ◽  
Tumor Drugs ◽  
Separate Class ◽  
Structure And Activity ◽  
Very High

An overview of the development of anti-tumor organotin derivatives in selected classes of compounds is presented and discussed. High to very high in vitro activity has been found, sometimes equaling that of doxorubicin. Solubility in water is an important issue, dominating the in vivo testing of compounds with promising in vitro properties. The cytotoxicity of the compounds was increased by the presence of a bulky group, an active substituent or one or more polar substituents. Polar substituents may also improve the water solubility. Although organotin derivatives constitute a separate class of compounds, the comparison with cisplatin is inevitable. Among the observed toxicities, neurotoxicity, known from platinum cytostatics, and gastrointestinal toxicity, typical for many oncology drugs, have been detected. Further research to develop novel, useful organotin anti-tumor compounds should be carried out.

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