Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Rubim, Alexandre Machado; Rubenick, Jaqueline Bandeira; Maurer, Marcela; Laporta, Lorenzo; Rolim, Clarice Madalena Bueno

doi:10.1590/s2175-97902017000216083

Cited by 13 publications

(15 citation statements)

References 36 publications

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“…Rubim et al prepared an amiodarone hydrochloride– β -CD (HP β CD) inclusion complex by a spray drying method. Compared with the pure drug and physical mixture, the water solubility and drug dissolution rate of the inclusion complex were increased significantly [7]. β -CD, as a new drug inclusion material, could not only improve the water solubility and controlled release rate of the drug, but also enhanced the cytotoxicity of the drug in vitro.…”

Section: Introductionmentioning

confidence: 99%

Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

et al. 2019

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The herbicide diuron is hardly soluble in water and most organic solvents and is usually made into a wettable powder or mixed with soil when used, which causes environmental risk and a reduction in herbicidal efficacy. In this study, the physicochemical properties were changed by using β-cyclodextrin (β-CD) to encapsulate diuron to form an inclusion complex. Some key technologies, including X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and nuclear magnetic resonance (1H NMR), were used to characterize the inclusion complex. The stoichiometry of the inclusion complex was determined by recording the 1H NMR spectrum or by using a diagram of inclusion ratios. A phase solubility study proved that the formed inclusion complex exhibited higher water solubility. Thermogravimetric analysis (TGA) demonstrated that the formed inclusion complex exhibited better thermal stability. Biological activity studies indicated that the herbicidal activity, in terms of herbicide removal, of the formed inclusion complex was higher than that of the original diuron. In general, the formation of the inclusion complex could reduce the environmental damage caused by diuron and enhance its herbicidal activity, providing an environmentally friendly method for using diuron.

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Section: Introductionmentioning

confidence: 99%

Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

et al. 2019

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“…Inclusion complexes of HP-β-CD are of great interest in pharmaceutical application, and they have been used to increase the solubility of a great number of various drugs [16,[21][22][23][24][25][26]. Rubim et al [27] followed the effect of the CD type as β-cyclodextrin, methyl-β-cyclodextrin, and 2-hydroxypropyl-β-cyclodextrin on the complexation with AMD and release ability. The enhanced solubility and dissolution may help to improve in vivo performance.…”

Section: Introductionmentioning

confidence: 99%

“…The enhanced solubility and dissolution may help to improve in vivo performance. Only a few studies are reported on the formation and characterization of inclusion complexes of HP-β-CD with amiodarone [27], but no detailed studies on loading and release of the drug have been found, and there are no pharmacokinetic data available about these systems.…”

Section: Introductionmentioning

confidence: 99%

Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

Crețeanu

Pamfil²,

Vasile³

et al. 2019

International Journal of Polymer Science

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The aim of this study was to improve the solubility of amiodarone hydrochloride (AMD) and the drug release using its inclusion complexes with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD). The inclusion complexes were prepared by coprecipitation and freeze-drying. The solubility enhancement of AMD/HP-β-CD inclusion complexes by 4–22 times was evaluated by the phase solubility method. The inclusion complexes were studied both in solution and in solid state by spectroscopic methods, dynamic light scattering (DLS) and zeta potential analysis, SEM, and DSC. The formulations of AMD/HP-β-CD inclusion complexes both as powdered form and as matrix tablets showed superior pharmacokinetic performance in improving loading and release properties in respect of those of the insoluble AMD drug. In vitro kinetic study reveals a complex mechanism of release occurring in three steps: the first one being attributed to a burst effect and the other two to different bonding existing in inclusion complexes. An in vivo test on matrix tablets containing Kollidon® and chitosan also reveals a multiple (at least two) peaks release diagram because of both structures of the inclusion complexes and also of different sites of absorption in biological media (digestive tract).

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“…Thus, enhanced solubility and dissolution rate was obtained in vitro in the case of amiodarone complexation with β-cyclodextrin ( Riekes et al, 2010 ). A recent in vitro study ( Rubim et al, 2017 ) evaluated the influence of the CD type (β-cyclodextrin, methyl-β-cyclodextrin, and 2-hydroxypropyl-β-cyclodextrin) on the complexation with AMD and on dissolution rate and found enhanced solubility and dissolution rates for inclusion complexes ( Rubim et al, 2017 ). Only a few studies reported in vitro characterization of inclusion complexes of HP-β-CD with amiodarone ( Rubim et al, 2017 ; Creteanu et al, 2019 ), but there are no data available about the acute toxicity of these systems.…”

Section: Introductionmentioning

confidence: 99%

Study on Acute Toxicity of Amiodarone New Complexes With Cyclodextrin

Ghiciuc¹,

Shleghm²,

Vasile³

et al. 2021

Front. Pharmacol.

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Amiodarone low solubility and high permeability is the limiting step for its bioavailability, therefore new formulations are needed to improve the solubility of amiodarone either to increase its oral bioavailability or to reduce its toxic effects. Complexation of amiodarone with cyclodextrin results in improved dissolution rate, solubility, and allows for a more controlled drug release. We characterized the acute toxicity of a new amiodarone 2-hydroxypropyl-β-cyclodextrin complex (AMD/HP-β-CD) as powdered form and as a matrix based on Kollidon® and chitosan, administered intraperitoneally in laboratory animals. There were developed two formulations of matrix: one containing only pure AMD as a control sample (Fc) and one containing the inclusion complex with the optimal solubility (F). AMD was equitoxic with HP-β-CD after intraperitoneal administration (289.4 mg/kg for AMD and 298.3 mg/kg for AMD/HP-β-CD), with corresponding histopathological changes. The matrix based formulations presented higher LD50 values for acute toxicity, of 347.5 mg/kg for Fc and 455.6 mg/kg for F10, conducting to the idea of a safer administration because KOL and CHT matrix modified the solubility and controlled the AMD release. The LD50 is 1.5 higher for AMD/HP-β-CD included in a KOL and CHT based matrix compared to the pure AMD, administered intraperitoneally.

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Inclusion complex of amiodarone hydrochloride with cyclodextrins: preparation, characterization and dissolution rate evaluation

Cited by 13 publications

References 36 publications

Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

Enhanced Solubility, Stability, and Herbicidal Activity of the Herbicide Diuron by Complex Formation with β-Cyclodextrin

Study on the Role of the Inclusion Complexes with 2-Hydroxypropyl-β-cyclodextrin for Oral Administration of Amiodarone

Study on Acute Toxicity of Amiodarone New Complexes With Cyclodextrin

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