Studies on spectral characterization and solubility of hydroxypropyl β-cyclodextrin/iloperidone binary and ternary complexes using different auxiliary agents

Ziprasidone (ZPR) is an antipsychotic agent having less solubility. It is used for the treatment of schizophrenia. Complexation of hydrophobic drugs with cyclodextrins leads to enhanced solubility and dissolution. In this study, inclusion complexes were prepared by different methods, using ZPR, β-cyclodextrin (β-CD), and different auxiliary agents like hydrophilic polymer and hydroxy acid (1:1:0.5) to improve the aqueous solubility. The characterization of the ternary complexes was carried out using solubility study, Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Fourier transformation infrared spectroscopy (FT-IR) and in vitro dissolution studies. DSC, XRD, and FT-IR studies showed interaction in drug, cyclodextrin, and auxiliary agents which are confirmed by enhancement of solubility and dissolution. Spray-dried dispersion showed less crystallinity and higher solubility as compared to the kneading method for both citric acid and Lutrol® F-68. Thus, the investigation concludes that the presence of the auxiliary agent has a synergistic action on complexation with cyclodextrin, which helps to modify the physicochemical properties of the drug.

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“…PMs for both AAs showed slower dissolution as compared to KN and SD. These results are in tune with those reported in literature [31,34].…”

Section: In Vitro Dissolution Studysupporting

confidence: 93%

Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies

Londhe

Krishnan

2020

Eur J Chem

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“…The oxalate characteristic absorption bands of the C−C stretching is around 1300 cm −1 . There is no strong peak around 3300 cm −1 , which convincingly excluded the presence of hydroxyl groups in the crystal structure of KSb 2 C 2 O 4 F 5 [18] …”

Section: Figurementioning

confidence: 80%

An Antimony(III) Fluoride Oxalate with Large Birefringence

Chen

Yang

et al. 2021

Chemistry A European J

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Birefringent materials play a key role in modulating the polarization of light and thus in optical communication as well as in laser techniques and science. Designing new, excellent birefringent materials remains a challenge. In this work, we designed and synthesized the first antimony(III) fluoride oxalate birefringent material, KSb2C2O4F5, by a combination of delocalized π‐conjugated [C2O4]2− groups, stereochemical active Sb3+ cations, and the most electronegative element, fluorine. The [C2O4]2− groups are not in an optimal arrangement in the crystal structure of KSb2C2O4F5; nonetheless, KSb2C2O4F5 exhibits a large birefringence (Δn=0.170 at 546 nm) that is even better than that of the well‐known commercial birefringent material α‐BaB2O4, even though the latter features an optimal arrangement of π‐conjugated [B3O6]3− groups. Based on first‐principles calculations, this prominent birefringence should be attributed to the alliance of planar π‐conjugated [C2O4]2− anions, highly distorted SbO2F2 and SbOF3 polyhedra with a stereochemically active lone pair. The combination of lone‐pair electrons and π‐conjugated systems boosts the birefringence to a large extent and will help the development of high‐performance birefringent materials.

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“…In phosphate buffer (pH 6.8), no significant difference was observed between the drug Figure 5c. In multimedia, the inclusion complex showed no significant difference when compared with the HPβCD-based inclusion complex [16]. The multimedia dissolution data show that as the buffer's pH decreased from 6.8 to 4.5 and 1.2, the dissolution rate was significantly enhanced.…”

Section: Multimedia Dissolution Studymentioning

confidence: 86%

Inclusion Complex of Iloperidone with Sulfobutyl Ether Beta-Cyclodextrin: Characterization and Dissolution Studies

Bhadale

Londhe

2020

The 1st International Electronic Conference on Pharmaceutics

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Iloperidone (ILO) is a second-generation antipsychotic drug and a first-line treatment approved by USFDA in May 2009. Iloperidone belongs to Biopharmaceutical Classification Systems (BCS) class II; thus, it is poorly water-soluble, highly permeable, and has pH-dependent solubility. Cyclodextrins and their derivatives have a wide range of applications in different formulations due to their complexation ability, which improves the solubility, stability, safety, and bioavailability of a drug. We have tried the complexation of iloperidone with sulfobutyl ether-β-cyclodextrin (SEβCD) to improve its solubility and dissolution. Complexation was done by the kneading method. The characterization of the SEβCD complexes with Iloperidone was done by FTIR, differential scanning calorimetry (DSC), saturation solubility, etc. A multimedia dissolution of the complex was carried out and compared with the plain drug. A significant improvement in drug release was found from SEβCD complexes in all media when compared with the drug alone.

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Studies on spectral characterization and solubility of hydroxypropyl β-cyclodextrin/iloperidone binary and ternary complexes using different auxiliary agents

Cited by 15 publications

References 41 publications

Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies

Effect of inclusion of citric acid and Lutrol® F-68 on ziprasidone and β-cyclodextrin complexation: Characterization, solubility and dissolution studies

An Antimony(III) Fluoride Oxalate with Large Birefringence

Inclusion Complex of Iloperidone with Sulfobutyl Ether Beta-Cyclodextrin: Characterization and Dissolution Studies

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