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Article

Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability

1
Tarchomin Pharmaceutical Works “Polfa” S.A., A. Fleminga 2, 03-176 Warsaw, Poland
2
Department of Pharmacognosy, Poznan University of Medical Sciences, Swiecickiego 4, 60-781 Poznan, Poland
3
Institute of Materials Science and Engineering, Poznan University of Technology, M. Sklodowskiej-Curie 5, 60-965 Poznan, Poland
4
Institute of Molecular Physics, Polish Academy of Science, Smoluchowskiego 17, 60-179 Poznan, Poland
*
Author to whom correspondence should be addressed.
Academic Editor: María Ángeles Peña Fernández
Pharmaceuticals 2021, 14(5), 453; https://doi.org/10.3390/ph14050453
Received: 4 April 2021 / Revised: 6 May 2021 / Accepted: 7 May 2021 / Published: 11 May 2021
To improve physicochemical properties of vardenafil hydrochloride (VAR), its amorphous form and combinations with excipients—hydroxypropyl methylcellulose (HPMC) and β-cyclodextrin (β-CD)—were prepared. The impact of the modification on physicochemical properties was estimated by comparing amorphous mixtures of VAR to their crystalline form. The amorphous form of VAR was obtained as a result of the freeze-drying process. Confirmation of the identity of the amorphous dispersion of VAR was obtained through the use of comprehensive analysis techniques—X-ray powder diffraction (PXRD) and differential scanning calorimetry (DSC), supported by FT-IR (Fourier-transform infrared spectroscopy) coupled with density functional theory (DFT) calculations. The amorphous mixtures of VAR increased its apparent solubility compared to the crystalline form. Moreover, a nearly 1.3-fold increase of amorphous VAR permeability through membranes simulating gastrointestinal epithelium as a consequence of the changes of apparent solubility (Papp crystalline VAR = 6.83 × 10−6 cm/s vs. Papp amorphous VAR = 8.75 × 10−6 cm/s) was observed, especially for its combinations with β-CD in the ratio of 1:5—more than 1.5-fold increase (Papp amorphous VAR = 8.75 × 10−6 cm/s vs. Papp amorphous VAR:β-CD 1:5 = 13.43 × 10−6 cm/s). The stability of the amorphous VAR was confirmed for 7 months. The HPMC and β-CD are effective modifiers of its apparent solubility and permeation through membranes simulating gastrointestinal epithelium, suggesting a possibility of a stronger pharmacological effect. View Full-Text
Keywords: vardenafil hydrochloride; amorphous dispersion; apparent solubility; permeability vardenafil hydrochloride; amorphous dispersion; apparent solubility; permeability
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MDPI and ACS Style

Wiergowska, G.; Ludowicz, D.; Wdowiak, K.; Miklaszewski, A.; Lewandowska, K.; Cielecka-Piontek, J. Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability. Pharmaceuticals 2021, 14, 453. https://doi.org/10.3390/ph14050453

AMA Style

Wiergowska G, Ludowicz D, Wdowiak K, Miklaszewski A, Lewandowska K, Cielecka-Piontek J. Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability. Pharmaceuticals. 2021; 14(5):453. https://doi.org/10.3390/ph14050453

Chicago/Turabian Style

Wiergowska, Gabriela, Dominika Ludowicz, Kamil Wdowiak, Andrzej Miklaszewski, Kornelia Lewandowska, and Judyta Cielecka-Piontek. 2021. "Combinations of Freeze-Dried Amorphous Vardenafil Hydrochloride with Saccharides as a Way to Enhance Dissolution Rate and Permeability" Pharmaceuticals 14, no. 5: 453. https://doi.org/10.3390/ph14050453

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