Physicochemical Properties and Dissolution Studies of Dexamethasone Acetate-β-Cyclodextrin Inclusion Complexes Produced by Different Methods

Doile, Mayara M.; Fortunato, Keila A.; Schmücker, Iára C.; Schucko, Sacha K.; Silva, Marcos A. S.; Rodrigues, Patrik Oening

doi:10.1208/s12249-008-9042-z

Cited by 57 publications

(37 citation statements)

References 20 publications

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“…The endothermic process was followed by thermal degradation -a process that was confirmed by the TG curve (Fig. 25 Similar results were also reported for the inclusion process of other substances. The broad endothermic HF peak also indicated HPBCD dehydration within the same temperature interval; the melting point of HPBCD had a higher value than that of ZOF (336 °C), proven by both the HF and DTG curves, which is consistent with the previously reported value.…”

Section: Thermal Analysissupporting

confidence: 82%

Physicochemical characterization of zofenopril inclusion complex with hydroxypropyl-β-cyclodextrin

Udrescu

Sbârcea

Fuliaş

et al. 2015

JSCS

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Zofenopril calcium (ZOF) is one of the newest angiotensin-converting enzyme (ACE) inhibitors, highly lipophilic and with low water solubility. This research investigates the interaction between ZOF and a chemically modified derivative of β-cyclodextrin, 2-hydroxypropyl-β-cyclodextrin (HPBCD), in order to prove the formation of an inclusion complex with an enhanced water solubility profile of ZOF. In this research, for the first time, the physicochemical characterization and the solubility profile of an inclusion complex between ZOF and HPBCD are reported. Different spectroscopic techniques (UV absorption spectrometry, powder X-ray diffraction, attenuated total reflectance Fourier transform IR spectroscopy) were applied in order to prove the formation of the ZOF/HPBCD inclusion complex, both in water and in the solid state, backed by thermal analysis (TGA/DTG/HF). The obtained results confirmed that the physicochemical properties of the ZOF/HPBCD binary system, prepared using the kneading method, are different in comparison to both with the parent substances and the corresponding physical mixture, thus suggesting that an inclusion complex was formed. After the formation of the inclusion complex with HPBCD, the solubility test indicated that the water solubility of ZOF was increased 5-fold.

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Section: Thermal Analysissupporting

confidence: 82%

Physicochemical characterization of zofenopril inclusion complex with hydroxypropyl-β-cyclodextrin

Udrescu

Sbârcea

Fuliaş

et al. 2015

JSCS

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“…Optical microscopy analysis is a fast and relatively inexpensive technique to confirm the formation of drug/CD complex by comparing the shape and particle size of β-CD, IBU and their binary systems [23,31] . The photomicrographs of samples are shown in fig.…”

Section: Resultsmentioning

confidence: 99%

Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes

Ai¹,

Ma²,

Li³

et al. 2017

ijps

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Ai, et al.: Effect of Drug Particle Size on Cyclodextrin Inclusion ComplexesThe main purpose of this study was to investigate the role of drug particle size on the complexation, physicochemical properties and dissolution of β-cyclodextrin inclusion complexes. In this work, ibuprofen in size of 3 μm and 45 μm (ibuprofen 3 and ibuprofen 45) were employed as the poorly water-soluble drug model. Complexation kinetics and complexation efficiency studies were conducted to investigate the complexation of ibuprofen with β-cyclodextrin in water. The solid cyclodextrins inclusion complexes were prepared with kneading method and characterized by Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry, optical microscopy analyses and dissolution test. Ibuprofen with smaller particle size showed higher complexation rate with β-cyclodextrin in complexation kinetics study. By comparing the apparent stability constant, K c and complexation efficiency of complexes, it also indicated that smaller drug particles are more efficient to interact with β-cyclodextrin than larger particles. The phase solubility diagram could be classified as Bs type, which denotes complexes with limited solubility. The Fourier transform-infrared spectroscopy, differential scanning calorimetry, X-ray powder difractometry and optical microscopy analyses confirmed the formation of β-cyclodextrin inclusion complexes with ibuprofen 3 or ibuprofen 45. In the dissolution study, the inclusion complexes presented faster dissolution rate on contrast with the physical mixtures and pure drugs. What is more, the inclusion complexes prepared with ibuprofen in small particle size showed improving dissolution rate than in large particle size.

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“…Then the mixture was stirred for 1 h and was evaporated to dryness at 45 °C. The dried mass was crushed and sieved through 100 micron mesh [29].…”

Section: Complex Formation By Co-evaporation Methods (Coe)mentioning

confidence: 99%

ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DERIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH Β-Cyclodextrin

Hossain

Nanda²

2018

Int J Pharm Pharm Sci

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Objective: To synthesis a novel methodology of bioactive quinazoline derivatives under greener process to an excellent yields and increases their solubility via inclusion with β-cyclodextrin (CD). Methods: Derivatives of quinazoline compounds were prepared by the mixture of 3-amino-2-phenylquinazolin-4(3H)-one, derived from 2-phenyl-4H-benzo[1,3]oxazin-4-one by refluxing with hydrazine, substituted aromatic aldehyde and alumina intimately in an agate mortar and pestle under solvent-free condition. Using various techniques for preparing inclusion complexes, kneaded method is the best method for encapsulation in host-guest complex chemistry. All compounds including inclusion complexes were characterised by spectral methods. Results: Synthesized a series of novel quinazoline compounds under a very easier greener process with a commercially available reagent. However, their low bioavailability, due to low absorption and solubility, can limit their potential applications. CD was used to resolve this solubility problem. CD can easily accommodated the guest molecules to encapsulate inside its cavity due to interior the hydrophobic nature with a hydrophilic exterior part to form thermodynamically more stable molecular microcapsules, commonly name as host-guest complexes or inclusion complexes. In this sense, CD was utilized to enhance not only the solubility and bioavailability of these quinazoline compounds but also their antibacterial capacity. The formation of inclusion complex was thus confirmed by ultraviolet-visible spectroscopy (UV-VIS), Fourier Transform Infrared Spectrometry (FT-IR), differential scanning calorimetry (DSC) and solubility study technique. Conclusion: Here we have successfully unfolded an eco-friendly methodology for the synthesis of derivatives of quinazoline and increased their solubility via host-guest inclusion technique. From the spectral analysis, it was concluded that the quinazoline compound is fully encapsulated inside the cavity of the CD.

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Physicochemical Properties and Dissolution Studies of Dexamethasone Acetate-β-Cyclodextrin Inclusion Complexes Produced by Different Methods

Cited by 57 publications

References 20 publications

Physicochemical characterization of zofenopril inclusion complex with hydroxypropyl-β-cyclodextrin

Physicochemical characterization of zofenopril inclusion complex with hydroxypropyl-β-cyclodextrin

Effect of Drug Particle Size on Complexation, Physicochemical Properties and Dissolution of Cyclodextrin Inclusion Complexes

ALUMINA CATALYST: SYNTHESIS OF NOVEL QUINAZOLINE DERIVATIVES AND THEIR SOLUBILITY INCREASES THROUGH INCLUSION WITH Β-Cyclodextrin

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