Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment
<i>Chelidonium majus</i> (also known as celandine) contains pharmacologically active compounds such as isoquinoline alkaloids (e.g., chelidonine, sanguinarine), flavonoids, saponins, carotenoids, and organic acids. Due to the presence of isoquinoline alkaloids, <i>Chelidonii herba&...
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MDPI AG
2020-04-01
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author | Magdalena Paczkowska Justyna Chanaj-Kaczmarek Aleksandra Romaniuk-Drapała Błażej Rubiś Daria Szymanowska Joanna Kobus-Cisowska Emilia Szymańska Katarzyna Winnicka Judyta Cielecka-Piontek |
author_facet | Magdalena Paczkowska Justyna Chanaj-Kaczmarek Aleksandra Romaniuk-Drapała Błażej Rubiś Daria Szymanowska Joanna Kobus-Cisowska Emilia Szymańska Katarzyna Winnicka Judyta Cielecka-Piontek |
author_sort | Magdalena Paczkowska |
collection | DOAJ |
description | <i>Chelidonium majus</i> (also known as celandine) contains pharmacologically active compounds such as isoquinoline alkaloids (e.g., chelidonine, sanguinarine), flavonoids, saponins, carotenoids, and organic acids. Due to the presence of isoquinoline alkaloids, <i>Chelidonii herba</i> extracts are widely used as an antibacterial, antifungal, antiviral (including HSV-1 and HIV-1), and anti-inflammatory agent in the treatment of various diseases, while chitosan is a biocompatible and biodegradable carrier with valuable properties for mucoadhesive formulations preparation. Our work aimed to prepare mucoadhesive vaginal drug delivery systems composed of <i>Chelidonii herba</i> lyophilized extract and chitosan as an effective way to treat vaginitis. The pharmacological safety of usage of isoquinoline alkaloids, based on MTT test, were evaluated for the maximum doses 36.34 ± 0.29 µg/mL and 0.89 ± 1.16 µg/mL for chelidonine and sanguinarine, respectively. Dissolution rate profiles and permeability through artificial membranes for chelidonine and sanguinarine after their introduction into the chitosan system were studied. The low permeability for used save doses of isoquinoline alkaloids and results of microbiological studies allow confirmation that system <i>Chelidonii herba</i> lyophilized extract chitosan 80/500 1:1 (w/w) is a promising strategy for vaginal use. Ex vivo studies of mucoadhesive properties and evaluation of tableting features demonstrated that the formulation containing <i>Chelidonii herba</i> lyophilized extract (120.0 mg) with chitosan (80/500—100.0 mg) and polymer content (HPMC—100.0 mg, microcrystalline cellulose—50.0 mg, lactose monohydrate—30.0 mg and magnesium stearate—4.0 mg) is a vaginal dosage form with prolonging dissolution profile and high mucoadhesion properties (up to 4 h). |
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issn | 2077-0383 |
language | English |
last_indexed | 2024-03-10T20:18:33Z |
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spelling | doaj.art-9eec4ad1768b4116b240bf39ec84407c2023-11-19T22:24:51ZengMDPI AGJournal of Clinical Medicine2077-03832020-04-0194120810.3390/jcm9041208Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis TreatmentMagdalena Paczkowska0Justyna Chanaj-Kaczmarek1Aleksandra Romaniuk-Drapała2Błażej Rubiś3Daria Szymanowska4Joanna Kobus-Cisowska5Emilia Szymańska6Katarzyna Winnicka7Judyta Cielecka-Piontek8Department of Pharmacognosy, Faculty of Pharmacy, Poznan University of Medical Sciences, Swiecickiego 4, 60781 Poznan, PolandDepartment of Pharmacognosy, Faculty of Pharmacy, Poznan University of Medical Sciences, Swiecickiego 4, 60781 Poznan, PolandDepartment of Clinical Chemistry and Molecular Diagnostics, Poznan University of Medical Sciences, Przybyszewskiego 49, 60355 Poznań, PolandDepartment of Clinical Chemistry and Molecular Diagnostics, Poznan University of Medical Sciences, Przybyszewskiego 49, 60355 Poznań, PolandDepartment of Biotechnology and Food Microbiology, Poznan University of Life Sciences, Wojska Polskiego 48, 60627 Poznan, PolandDepartment of Gastronomy Science and Functional Foods, Poznan University of Life Sciences, Wojska Polskiego 28, 60637 Poznan, PolandDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2c, 15222 Białystok, PolandDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2c, 15222 Białystok, PolandDepartment of Pharmacognosy, Faculty of Pharmacy, Poznan University of Medical Sciences, Swiecickiego 4, 60781 Poznan, Poland<i>Chelidonium majus</i> (also known as celandine) contains pharmacologically active compounds such as isoquinoline alkaloids (e.g., chelidonine, sanguinarine), flavonoids, saponins, carotenoids, and organic acids. Due to the presence of isoquinoline alkaloids, <i>Chelidonii herba</i> extracts are widely used as an antibacterial, antifungal, antiviral (including HSV-1 and HIV-1), and anti-inflammatory agent in the treatment of various diseases, while chitosan is a biocompatible and biodegradable carrier with valuable properties for mucoadhesive formulations preparation. Our work aimed to prepare mucoadhesive vaginal drug delivery systems composed of <i>Chelidonii herba</i> lyophilized extract and chitosan as an effective way to treat vaginitis. The pharmacological safety of usage of isoquinoline alkaloids, based on MTT test, were evaluated for the maximum doses 36.34 ± 0.29 µg/mL and 0.89 ± 1.16 µg/mL for chelidonine and sanguinarine, respectively. Dissolution rate profiles and permeability through artificial membranes for chelidonine and sanguinarine after their introduction into the chitosan system were studied. The low permeability for used save doses of isoquinoline alkaloids and results of microbiological studies allow confirmation that system <i>Chelidonii herba</i> lyophilized extract chitosan 80/500 1:1 (w/w) is a promising strategy for vaginal use. Ex vivo studies of mucoadhesive properties and evaluation of tableting features demonstrated that the formulation containing <i>Chelidonii herba</i> lyophilized extract (120.0 mg) with chitosan (80/500—100.0 mg) and polymer content (HPMC—100.0 mg, microcrystalline cellulose—50.0 mg, lactose monohydrate—30.0 mg and magnesium stearate—4.0 mg) is a vaginal dosage form with prolonging dissolution profile and high mucoadhesion properties (up to 4 h).https://www.mdpi.com/2077-0383/9/4/1208<i>Chelidonium majus</i>chelidonine and sanguinarinechitosanMTT testmicrobiological activitydissolution |
spellingShingle | Magdalena Paczkowska Justyna Chanaj-Kaczmarek Aleksandra Romaniuk-Drapała Błażej Rubiś Daria Szymanowska Joanna Kobus-Cisowska Emilia Szymańska Katarzyna Winnicka Judyta Cielecka-Piontek Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment Journal of Clinical Medicine <i>Chelidonium majus</i> chelidonine and sanguinarine chitosan MTT test microbiological activity dissolution |
title | Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment |
title_full | Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment |
title_fullStr | Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment |
title_full_unstemmed | Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment |
title_short | Mucoadhesive Chitosan Delivery System with <i>Chelidonii Herba</i> Lyophilized Extract as a Promising Strategy for Vaginitis Treatment |
title_sort | mucoadhesive chitosan delivery system with i chelidonii herba i lyophilized extract as a promising strategy for vaginitis treatment |
topic | <i>Chelidonium majus</i> chelidonine and sanguinarine chitosan MTT test microbiological activity dissolution |
url | https://www.mdpi.com/2077-0383/9/4/1208 |
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