scholarly journals Investigation of hydroxypropyl-β-cyclodextrin inclusion complexation of two poorly soluble model drugs and their taste-sensation - Effect of electrolytes, freeze-drying and incorporation into oral film formulations

2020 ◽  
pp. 102245
Author(s):  
Julia F. Alopaeus ◽  
Anja Göbel ◽  
Jörg Breitkreutz ◽  
Sverre Arne Sande ◽  
Ingunn Tho
Keyword(s):  
Freeze Drying ◽  
Inclusion Complexation ◽  
Taste Sensation ◽  
Cyclodextrin Inclusion ◽  
Soluble Model ◽  
Poorly Soluble

Photophysical Properties of Self-assembled Cyanine-dye Dimmer Formation Assisted by Cyclodextrin Inclusion Complexation

2013 ◽  
Vol 579 (1) ◽  
pp. 22-29 ◽  
Author(s):  
Shigeaki Abe ◽  
Takashi Hirota ◽  
Takayuki Kiba ◽  
Naoyuki Miyakawa ◽  
Fumio Watari ◽  
...  
Keyword(s):  
Photophysical Properties ◽  
Inclusion Complexation ◽  
Cyanine Dye ◽  
Cyclodextrin Inclusion ◽  
Self Assembled

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 Characterization of pesticide-β-cyclodextrin inclusion complexes in aqueous solution

2005 ◽  
Vol 3 (2) ◽  
pp. 151-155
Author(s):  
Goran Petrovic ◽  
Blaga Stojceva-Radovanovic ◽  
O. Jovanovic
Keyword(s):  
Aqueous Solution ◽  
Inclusion Complexes ◽  
Ultraviolet Spectrophotometry ◽  
Maximum Solubility ◽  
Complex Stability Constant ◽  
Cyclodextrin Inclusion Complexes ◽  
Cyclodextrin Inclusion ◽  
Calorimetric Measurements ◽  
Poorly Soluble

The solubility of four different pesticides, "dimethoate", "simazine" "linuron" and "thiram", poorly soluble or non-soluble in water, were measured in water and in aqueous solution of ?-cyclodextrin by ultraviolet spectrophotometry. Standard water solutions of pesticides were prepared in the range of concentrations up to the maximum solubility of each pesticide in water. Concentrations of the pesticides were determined as absorbance on the absorption maximum. The obtained results show that the aqueous solution of ?-cyclodextrin was a powerful solubilizer of investigated pesticides due to the formation of inclusion complexes. Effective solubility of some of the pesticides in aqueous ?-cyclodextrin solution was up to three orders of magnitude higher than those in water. Thermodynamic parameters and complex stability constant of the obtained inclusion complexes were determined by the calorimetric measurements.

Characteristic of Cyclodextrins: Their Role and Use in the Pharmaceutical Technology

2020 ◽  
Vol 21 (14) ◽  
pp. 1495-1510 ◽  
Author(s):  
Malwina Lachowicz ◽  
Andrzej Stańczak ◽  
Michał Kołodziejczyk
Keyword(s):  
New Drugs ◽  
Natural Form ◽  
Chemically Modified ◽  
Cyclodextrin Inclusion Complexes ◽  
Glycosidic Bonds ◽  
Cyclodextrin Inclusion ◽  
Pharmaceutical Technology ◽  
Local Toxicity ◽  
Toxicological Profile ◽  
Poorly Soluble

About 40% of newly-discovered entities are poorly soluble in water, and this may be an obstacle in the creation of new drugs. To address this problem, the present review article examines the structure and properties of cyclodextrins and the formation and potential uses of drug – cyclodextrin inclusion complexes. Cyclodextrins are cyclic oligosaccharides containing six or more D-(+)- glucopyranose units linked by α-1,4-glycosidic bonds, which are characterized by a favourable toxicological profile, low local toxicity and low mucous and eye irritability; they are virtually non-toxic when administered orally. They can be incorporated in the formulation of new drugs in their natural form (α-, β-, γ-cyclodextrin) or as chemically-modified derivatives. They may also be used as an excipient in drugs delivered by oral, ocular, dermal, nasal and rectal routes, as described in the present paper. Cyclodextrins are promising compounds with many beneficial properties, and their use may be increasingly profitable for pharmaceutical scientists.

Cyclodextrin Inclusion of Medicinal Compounds for Enhancement of their Physicochemical and Biopharmaceutical Properties

2019 ◽  
Vol 19 (25) ◽  
pp. 2357-2370 ◽  
Author(s):  
Mino R. Caira
Keyword(s):  
Drug Discovery ◽  
Inclusion Complexation ◽  
Structural Diversity ◽  
Attrition Rate ◽  
Cyclodextrin Inclusion ◽  
Biopharmaceutical Properties ◽  
Fine Tune ◽  
Early Drug ◽  
Selection Of

Owing to their wide structural diversity and unique complexing properties, cyclodextrins (CDs) find manifold applications in drug discovery and development. The focus of this mini-review is on their uses as ‘enabling excipients’ both in the context of early drug discovery and in subsequent optimisation of drug performance. Features highlighted here include descriptions of the structures of CDs, synthetic derivatisation to fine-tune their properties, the nature of inclusion complexation of drugs within the CD cavity, methodology for the study of free and complexed hosts in the solid state and in solution, the inherent pharmacological activity of several CDs and its utility, novel CD-based drug delivery systems, and the role of CDs in drug discovery and optimisation. Illustrative examples are generally based on research reported during the last two decades. Application of CDs to the optimisation of the performance of established drugs is commonplace, but there are many opportunities for the intervention of CDs during the early stages of drug discovery, which could guide the selection of suitable candidates for development, thereby contributing to reducing the attrition rate of new molecular entities.

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