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

Wiergowska, Gabriela; Ludowicz, Dominika; Wdowiak, Kamil; Miklaszewski, Andrzej; Lewandowska, Kornelia; Cielecka-Piontek, Judyta

doi:10.3390/ph14050453

Submit to this Journal Review for this Journal Edit a Special Issue

Article Menu

...

Open AccessArticle

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

¹,

⁴

and

Judyta Cielecka-Piontek

^2,*

Tarchomin Pharmaceutical Works “Polfa” S.A., A. Fleminga 2, 03-176 Warsaw, Poland

Department of Pharmacognosy, Poznan University of Medical Sciences, Swiecickiego 4, 60-781 Poznan, Poland

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

(This article belongs to the Special Issue Solubilization and Controlled Release Strategy of Poorly Water-Soluble Drugs)

View Full-Text Download PDF

Browse Figures

Citation Export

Abstract

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 (P_{app crystalline VAR} = 6.83 × 10⁻⁶ cm/s vs. P_{app 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 (P_{app amorphous VAR} = 8.75 × 10⁻⁶ cm/s vs. P_{app 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

▼ Show Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited

Supplementary Material

Supplementary File 1:
ZIP-Document (ZIP, 517 KiB)

Share and Cite

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

Find Other Styles

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Metrics

Abstract views Pdf views Html views

Article Menu

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

Abstract

Supplementary Material

Share and Cite

Article Metrics

Article Access Statistics

Article Access Map by Country/Region

Further Information

Guidelines

MDPI Initiatives

Follow MDPI