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Article

Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A

1
Department of Pharmaceutical Technology and Biopharmaceutics, University of Bonn, 53121 Bonn, Germany
2
Institute for Medical Microbiology, Immunology and Parasitology, University Hospital Bonn, 53127 Bonn, Germany
3
German Center for Infection Research (DZIF), Partner Site Bonn-Cologne, 53127 Bonn, Germany
4
Institute for Pharmaceutical Biology, University of Bonn, 53115 Bonn, Germany
5
Pharmaceutical & Medicinal Chemistry, University of Bonn, 53121 Bonn, Germany
6
Department of Microbial Drugs, Helmholtz Centre for Infection Research, 38124 Braunschweig, Germany
7
German Center for Infection Research (DZIF), Partner Site Hannover-Braunschweig, 38124 Braunschweig, Germany
8
Translational Project Management Office (TPMO), German Center for Infection Research (DZIF), 38124 Braunschweig, Germany
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(11), 1105; https://doi.org/10.3390/pharmaceutics12111105
Received: 29 October 2020 / Revised: 13 November 2020 / Accepted: 16 November 2020 / Published: 18 November 2020
(This article belongs to the Special Issue Natural Products in Drug Delivery Systems)
Novel-antibiotics are urgently needed to combat an increase in morbidity and mortality due to resistant bacteria. The preclinical candidate corallopyronin A (CorA) is a potent antibiotic against Gram-positive and some Gram-negative pathogens for which a solid oral formulation was needed for further preclinical testing of the active pharmaceutical ingredient (API). The neat API CorA is poorly water-soluble and instable at room temperature, both crucial characteristics to be addressed and overcome for use as an oral antibiotic. Therefore, amorphous solid dispersion (ASD) was chosen as formulation principle. The formulations were prepared by spray-drying, comprising the water-soluble polymers povidone and copovidone. Stability (high-performance liquid chromatography, Fourier-transform-infrared spectroscopy, differential scanning calorimetry), dissolution (biphasic dissolution), and solubility (biphasic dissolution, Pion’s T3 apparatus) properties were analyzed. Pharmacokinetic evaluations after intravenous and oral administration were conducted in BALB/c mice. The results demonstrated that the ASD formulation principle is a suitable stability- and solubility-enhancing oral formulation strategy for the API CorA to be used in preclinical and clinical trials and as a potential market product. View Full-Text
Keywords: corallopyronin A (CorA); antibiotic; anthelmintic; povidone (PVP); copovidone (PVP/VA); solubility enhanced formulation; stability enhanced formulation; spray-dried amorphous solid dispersion (ASD); biphasic dissolution (BiPHa+); pharmacokinetic analysis corallopyronin A (CorA); antibiotic; anthelmintic; povidone (PVP); copovidone (PVP/VA); solubility enhanced formulation; stability enhanced formulation; spray-dried amorphous solid dispersion (ASD); biphasic dissolution (BiPHa+); pharmacokinetic analysis
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MDPI and ACS Style

Krome, A.K.; Becker, T.; Kehraus, S.; Schiefer, A.; Steinebach, C.; Aden, T.; Frohberger, S.J.; López Mármol, Á.; Kapote, D.; Jansen, R.; Chaverra-Muñoz, L.; Hübner, M.P.; Pfarr, K.; Hesterkamp, T.; Stadler, M.; Gütschow, M.; König, G.M.; Hoerauf, A.; Wagner, K.G. Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A. Pharmaceutics 2020, 12, 1105. https://doi.org/10.3390/pharmaceutics12111105

AMA Style

Krome AK, Becker T, Kehraus S, Schiefer A, Steinebach C, Aden T, Frohberger SJ, López Mármol Á, Kapote D, Jansen R, Chaverra-Muñoz L, Hübner MP, Pfarr K, Hesterkamp T, Stadler M, Gütschow M, König GM, Hoerauf A, Wagner KG. Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A. Pharmaceutics. 2020; 12(11):1105. https://doi.org/10.3390/pharmaceutics12111105

Chicago/Turabian Style

Krome, Anna K., Tim Becker, Stefan Kehraus, Andrea Schiefer, Christian Steinebach, Tilman Aden, Stefan J. Frohberger, Álvaro López Mármol, Dnyaneshwar Kapote, Rolf Jansen, Lillibeth Chaverra-Muñoz, Marc P. Hübner, Kenneth Pfarr, Thomas Hesterkamp, Marc Stadler, Michael Gütschow, Gabriele M. König, Achim Hoerauf, and Karl G. Wagner. 2020. "Solubility and Stability Enhanced Oral Formulations for the Anti-Infective Corallopyronin A" Pharmaceutics 12, no. 11: 1105. https://doi.org/10.3390/pharmaceutics12111105

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