Synthesis of a Disulfuram Inclusion Complex with Hydroxypropyl-β-Cyclodextrin and Its Effect on Cataract Development in Rats

Tyukova, V. S.; Кедик, С. А.; Панов, А. В.; Жаворонок, Е. С.; Mendeleev, D. I.; Senchikhin, I. N.; Фурсова, А. Ж.; Rumyantseva, Yu. V.; Колосова, Н.Г.

doi:10.1007/s11094-020-02140-y

Cited by 8 publications

(12 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…As shown in Figure 4 a,b, DS powder has two sharp endothermic peaks at 74.2 °C and 208.9 °C, whilst no endothermic sharp peaks were detected in any of the pure CDs nor inclusion complexes, proving an efficient inclusion of the drug. Moreover, the peak detected at about 74.2 °C might correspond to the melting point indicating its crystalline state, whereas the peak detected at about 208.9 °C corresponds to its thermal degradation [ 24 , 28 ]. It was also observed in Figure 4 that the freeze-dried formulations (HP20 and SBE20) demonstrated similar profiles to that of raw CDs.…”

Section: Resultsmentioning

confidence: 99%

See 1 more Smart Citation

Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization

et al. 2022

View full text Add to dashboard Cite

Disulfiram (DS), known as an anti-alcoholism drug, has shown a potent antiviral activity. Still, the potential clinical application of DS is limited by its low water solubility and rapid metabolism. Cyclodextrins (CDs) have been widely used to improve the solubility of drugs in water. In this study, five concentrations of hydroxypropyl β-cyclodextrin (HP) and sulfobutyl ether β-cyclodextrin (SBE) were used to form inclusion complexes of DS for enhanced solubility. Solutions were freeze-dried, and the interaction between DS and CD was characterized using differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and Fourier transform infrared spectroscopy (FTIR). In addition, the nebulization properties of the DS–CD solutions were studied. The aqueous solubility of DS increased significantly when loaded to either of both CDs. The phase solubility of both complexes was a linear function of the CD concentration (AL type). Furthermore, physicochemical characterization studies showed a potent inclusion of the drug in the CD–DS complexes. Aerosolization studies demonstrated that these formulations are suitable for inhalation. Overall, the CD inclusion complexes have great potential for the enhancement of DS solubility. However, further studies are needed to assess the efficacy of DS–CD inclusion complexes against SARS-CoV-2 via nebulization.

show abstract

Section: Resultsmentioning

confidence: 99%

“…The use of CD inclusion complexes to enhance the solubility of DS is reported in the literature for the treatment of other diseases such as cancer [ 23 , 24 ]. However, only one type of β-cyclodextrin was used at high concentrations, and no phase solubility studies were performed.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization

et al. 2022

View full text Add to dashboard Cite

show abstract

“…The thermogram for disulfiram show characteristic endotherms at 74 °C and 190–250 °C corresponding to melting and degradation events, respectively [ 46 ]. The thermograms for blank and loaded nanoparticles prepared by both methods were almost identical ( Figure 4 ), with a characteristic endotherm for the glass transition temperature for PLGA nanoparticles shown at 55 °C [ 47 ].…”

Section: Resultsmentioning

confidence: 99%

Comparative Nanofabrication of PLGA-Chitosan-PEG Systems Employing Microfluidics and Emulsification Solvent Evaporation Techniques

et al. 2020

View full text Add to dashboard Cite

Poor circulation stability and inadequate cell membrane penetration are significant impediments in the implementation of nanocarriers as delivery systems for therapeutic agents with low bioavailability. This research discusses the fabrication of a biocompatible poly(lactide-co-glycolide) (PLGA) based nanocarrier with cationic and hydrophilic surface properties provided by natural polymer chitosan and coating polymer polyethylene glycol (PEG) for the entrapment of the hydrophobic drug disulfiram. The traditional emulsification solvent evaporation method was compared to a microfluidics-based method of fabrication, with the optimisation of the parameters for each method, and the PEGylation densities on the experimental nanoparticle formulations were varied. The size and surface properties of the intermediates and products were characterised and compared by dynamic light scattering, scanning electron microscopy and X-ray diffraction, while the thermal properties were investigated using thermogravimetric analysis and differential scanning calorimetry. Results showed optimal particle properties with an intermediate PEG density and a positive surface charge for greater biocompatibility, with nanoparticle surface characteristics shielding physical interaction of the entrapped drug with the exterior. The formulations prepared using the microfluidic method displayed superior surface charge, entrapment and drug release properties. The final system shows potential as a component of a biocompatible nanocarrier for poorly soluble drugs.

show abstract

“…The sample was placed in an aluminum sample holder and scanned over the range between 4 to 80 • and position 2 Theta (θ) with increments of 0.008 • at a rate of 3 • /min at an ambient temperature. The raw data is converted into the graphical form using Origin Pro ® 2021 software (OriginLab Corporation, Northampton, MA, USA) [50]. The percentage crystallinity index (% CI) was determined using Equation (4).…”

Section: Crystallinity Of Powdermentioning

confidence: 99%

“…An average of 16 scans per sample was recorded. Spectra were plotted and analyzed using Origin Pro ® 2021 software (OriginLab Corporation, Northampton, MA, USA) [50].…”

Section: Ftir Analysismentioning

confidence: 99%

Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

et al. 2022

View full text Add to dashboard Cite

Rifampicin, a potent broad-spectrum antibiotic, remains the backbone of anti-tubercular therapy. However, it can cause severe hepatotoxicity when given orally. To overcome the limitations of the current oral therapy, this study designed inhalable spray-dried, rifampicin-loaded microparticles using aloe vera powder as an immune modulator, with varying concentrations of alginate and L-leucine. The microparticles were assessed for their physicochemical properties, in vitro drug release and aerodynamic behavior. The spray-dried powders were 2 to 4 µm in size with a percentage yield of 45 to 65%. The particles were nearly spherical with the tendency of agglomeration as depicted from Carr’s index (37 to 65) and Hausner’s ratios (>1.50). The drug content ranged from 0.24 to 0.39 mg/mg, with an association efficiency of 39.28 to 96.15%. The dissolution data depicts that the in vitro release of rifampicin from microparticles was significantly retarded with a higher L-leucine concentration in comparison to those formulations containing a higher sodium alginate concentration due to its hydrophobic nature. The aerodynamic data depicts that 60 to 70% of the aerosol mass was emitted from an inhaler with MMAD values of 1.44 to 1.60 µm and FPF of 43.22 to 55.70%. The higher FPF values with retarded in vitro release could allow sufficient time for the phagocytosis of synthesized microparticles by alveolar macrophages, thereby leading to the eradication of M. tuberculosis from these cells.

show abstract

Synthesis of a Disulfuram Inclusion Complex with Hydroxypropyl-β-Cyclodextrin and Its Effect on Cataract Development in Rats

Cited by 8 publications

References 8 publications

Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization

Preparation and Characterization of Disulfiram and Beta Cyclodextrin Inclusion Complexes for Potential Application in the Treatment of SARS-CoV-2 via Nebulization

Comparative Nanofabrication of PLGA-Chitosan-PEG Systems Employing Microfluidics and Emulsification Solvent Evaporation Techniques

Polymeric Microparticles: Synthesis, Characterization and In Vitro Evaluation for Pulmonary Delivery of Rifampicin

Contact Info

Product

Resources

About