Assisted Extraction with Cyclodextrins as a Way of Improving the Antidiabetic Activity of Actinidia Leaves

Sip, Szymon; Gościniak, Anna; Szulc, Piotr; Walkowiak, Jarosław; Cielecka‐Piontek, Judyta

doi:10.3390/pharmaceutics14112473

Cited by 5 publications

(5 citation statements)

References 68 publications

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“…The inhibition of α-glucosidase activity was studied on the basis of the method of Sip et al [ 44 ] with minor modifications. A total of 50 μL of 0.1 M phosphate buffer (pH 6.8), 50 μL of the sample, prepared similarly to the solubility test, and 30 μL of α-glucosidase solution (0.5 U·mL −1 ) were added to wells of a 96-well microplate.…”

Section: Methodsmentioning

confidence: 99%

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Garbiec,

Rosiak,

Zalewski

et al. 2023

Pharmaceutics

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Genistein, an isoflavone known for its antioxidant and antidiabetic effects, suffers from the drawback of low solubility. To overcome this limitation, co-amorphous systems were synthesized by incorporating amino acids that were chosen through computational methods. The confirmation of the amorphous state of lysine and arginine-containing systems was ascertained by X-ray powder diffraction. Subsequently, the characterization of these systems was extended by employing thermo-gravimetry, differential scanning calorimetry, Fourier-transform infrared spectroscopy, and scanning electron microscopy. The investigation also included an assessment of the physical stability of the samples during storage. The apparent solubility of the systems was studied in an aqueous medium. To evaluate the in vitro permeability through the gastrointestinal tract, the parallel artificial membrane permeability assay was employed. The biological properties of the systems were assessed with regard to their antioxidant activity using 2,2-diphenyl-1-picrylhydrazyl and cupric ion-reducing antioxidant capacity assays, as well as their ability to inhibit α-glucosidase. The systems’ glass transition temperatures were determined, and their homogeneity confirmed via differential scanning calorimetry analysis, while Fourier-transform infrared spectroscopy analysis provided data on molecular interactions. Stability was maintained for the entire 6-month storage duration. The co-amorphous system containing lysine displayed the most pronounced apparent solubility improvement, as well as a significant enhancement in antioxidant activity. Notably, both systems demonstrated superior α-glucosidase inhibition relative to acarbose, a standard drug for managing type 2 diabetes. The results indicate that co-amorphous systems with lysine and arginine have the potential to significantly enhance the solubility and biological activity of genistein.

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Section: Methodsmentioning

confidence: 99%

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Garbiec,

Rosiak,

Zalewski

et al. 2023

Pharmaceutics

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“…The stability constant ( K st ) equals 994.2 M -1 . It was reported that K s value between 50 and 5000 M −1 was considered the most suitable for the improvement of solubility and stability of poorly soluble drugs [ 23 ]. In conclusion, HPβCD increased the solubility of AP significantly with good stability of the complex in a ratio 1:1 host-guest molecules.…”

Section: Resultsmentioning

confidence: 99%

Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclo¬dextrin) and computational calculation of their inclusion complexes

Salman,

Al-Ani,

Al Azzam

et al. 2023

ADMET DMPK

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Background and Purpose: Apixaban (AP) is a factor X inhibitor, an orally active drug that inhibits blood coagulation for better prevention of venous thromboembolism. It has poor solubility, dissolution rate and low bioavailability. The aim of this study was to improve the aqueous solubility and dissolution rate of oral AP as a step to enhance its bioavailability by preparing it as an inclusion complex with beta- and hydroxy propyl beta-cyclodextrin. Experimental Approach: A simple, rapid method of analysis of AP was developed using ultraviolet spectrophotometry (UV) and partially validated in terms of linearity, precision and accuracy, recovery, and robustness. AP was prepared as a complex with beta cyclodextrin (βCD) and hydroxy propyl beta cyclodextrin (HPβCD) in weight ratios 1:1, 1:2, and 1:3 by kneading, solvent evaporation and spray drying methods and characterized by Fourier transfer infra-red (FTIR), differential scanning calorimetry (DSC), and percent drug content in each of the prepared complex. Using the computer simulation, the interactions of AP with βCD and HPβCD were investigated. Key Results: The phase solubility study showed that the solubility of AP was greatly enhanced from 54×10-3 mmol /L to 66 mmol/L using HPβCD with acceptable stability constant. Computer docking supports the formation of a stable 1:1 complex between AP and CD’s. The dissolution test results showed that the complex gave a significantly higher percentage of drug release (95%) over one hour compared to the free AP (60%) (p<0.05). Conclusion: AP- HPβCD complex in the ratio of 1:2 (w/w) can significantly improve the solubility and in vitro dissolution rate of AP.

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“…For the CUPRAC assay, following the Gościniak et al method [ 123 ], an amount of 50.0 µL of each sample solution and 150.0 µL of the CUPRAC reagent was pipetted onto the plate and incubated for 30 min at room temperature in darkness. For the FRAP assay, following the Sip et al method [ 124 ], the mixture of 25.0 µL of each sample solution and 175.0 µL of FRAP mixture was incubated for 30 min at 37 °C in dark conditions. Then, the absorbance was measured at 450 nm (CUPRAC assay) and 593 nm (FRAP assay) using a plate reader (Multiskan GO, Thermo Fisher Scientific, Waltham, MA, USA).…”

Section: Methodsmentioning

confidence: 99%

Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions

Rosiak,

Tykarska,

Cielecka-Piontek

2024

IJMS

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In this study, amorphous solid dispersions (ASDs) of pterostilbene (PTR) with polyvinylpyrrolidone polymers (PVP K30 and VA64) were prepared through milling, affirming the amorphous dispersion of PTR via X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). Subsequent analysis of DSC thermograms, augmented using mathematical equations such as the Gordon–Taylor and Couchman–Karasz equations, facilitated the determination of predicted values for glass transition (Tg), PTR’s miscibility with PVP, and the strength of PTR’s interaction with the polymers. Fourier-transform infrared (FTIR) analysis validated interactions maintaining PTR’s amorphous state and identified involved functional groups, namely, the 4′–OH and/or –CH groups of PTR and the C=O group of PVP. The study culminated in evaluating the impact of amorphization on water solubility, the release profile in pH 6.8, and in vitro permeability (PAMPA-GIT and BBB methods). In addition, it was determined how improving water solubility affects the increase in antioxidant (ABTS, DPPH, CUPRAC, and FRAP assays) and neuroprotective (inhibition of cholinesterases: AChE and BChE) properties. The apparent solubility of the pure PTR was ~4.0 µg·mL−1 and showed no activity in the considered assays. For obtained ASDs (PTR-PVP30/PTR-PVPVA64, respectively) improvements in apparent solubility (410.8 and 383.2 µg·mL−1), release profile, permeability, antioxidant properties (ABTS: IC50 = 52.37/52.99 μg·mL−1, DPPH: IC50 = 163.43/173.96 μg·mL−1, CUPRAC: IC0.5 = 122.27/129.59 μg·mL−1, FRAP: IC0.5 = 95.69/98.57 μg·mL−1), and neuroprotective effects (AChE: 39.1%/36.2%, BChE: 76.9%/73.2%) were confirmed.

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Assisted Extraction with Cyclodextrins as a Way of Improving the Antidiabetic Activity of Actinidia Leaves

Cited by 5 publications

References 68 publications

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Genistein Co-Amorphous Systems with Amino Acids: An Investigation into Enhanced Solubility and Biological Activity

Enhancement of apixaban's solubility and dissolution rate by inclusion complex (β-cyclodextrin and hydroxypropyl β-cyclo¬dextrin) and computational calculation of their inclusion complexes

Enhanced Antioxidant and Neuroprotective Properties of Pterostilbene (Resveratrol Derivative) in Amorphous Solid Dispersions

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