LAPSE:2021.0721
Published Article
LAPSE:2021.0721
Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms
Teodora Balaci, Bruno Velescu, Oana Karampelas, Adina Magdalena Musuc, George Mihai Nițulescu, Emma Adriana Ozon, Georgiana Nițulescu, Cerasela Elena Gîrd, Catalina Fița, Dumitru Lupuliasa
September 21, 2021
The aim of our study was to obtain rutoside (RUT) inclusion complexes in β-cyclodextrin (β-CD) and in hydroxypropyl-β-cyclodextrin (HP-β-CD), in a 1:1 molar ratio, using the lyophilization method of complexation in solution. The complexes were confirmed and characterized, in comparison with the raw materials and their simple physical mixtures, by SEM, DSC, and FT-IR analyses. The antioxidant activity of the compounds was assessed by using the 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and 2’-azino-bis(3-ethylbenzothiazolin-6-sulfonic) acid (ABTS) radicals, determining the radical scavenging activity, and by ferric reducing antioxidant power (FRAP) assay. The results revealed superior antioxidant ability for the inclusion complexes towards rutoside alone. The inclusion complexes were used as active ingredients in formulations of immediate-release tablets. The preformulation studies were performed on the powders for direct compression obtained after mixing the active ingredients with the excipients (Avicel PH 102, Polyplasdone XL-10, magnesium stearate, and talc). The materials were assessed for particle size, flowability, compressibility, and moisture content, establishing they are suitable for a direct compression process. The tablets were characterized regarding their pharmaco-technical properties and the results proved that the formulations lead to high-quality delivery systems, showing a good mechanical resistance with a low friability, excellent disintegration times, and satisfying dissolution rate. The performances were very similar for both formulations and the physico-mechanical properties of the tablets are not influenced by type of the used cyclodextrin, but the RUT- HP-β-CD tablets presented a higher dissolution rate.
Keywords
antioxidant activity, hydroxypropyl-β-cyclodextrin, inclusion complexes, rutoside, β-cyclodextrin
Subject
Suggested Citation
Balaci T, Velescu B, Karampelas O, Musuc AM, Nițulescu GM, Ozon EA, Nițulescu G, Gîrd CE, Fița C, Lupuliasa D. Physico-Chemical and Pharmaco-Technical Characterization of Inclusion Complexes Formed by Rutoside with β-Cyclodextrin and Hydroxypropyl-β-Cyclodextrin Used to Develop Solid Dosage Forms. (2021). LAPSE:2021.0721
Author Affiliations
Balaci T: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Velescu B: Department of Pharmacology and Clinical Pharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Karampelas O: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Musuc AM: Romanian Academy, “Ilie Murgulescu” Institute of Physical Chemistry, 202 Spl. Independentei, 060021 Bucharest, Romania [ORCID]
Nițulescu GM: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania [ORCID]
Ozon EA: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Nițulescu G: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Gîrd CE: Department of Pharmacognosy, Phytochemistry, Phytotherapy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania [ORCID]
Fița C: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania [ORCID]
Lupuliasa D: Department of Pharmaceutical Technology and Biopharmacy, Faculty of Pharmacy, “Carol Davila” University of Medicine and Pharmacy, 020956 Bucharest, Romania
Journal Name
Processes
Volume
9
Issue
1
First Page
pr9010026
Year
2020
Publication Date
2020-12-24
Published Version
ISSN
2227-9717
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Original Submission
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PII: pr9010026, Publication Type: Journal Article
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LAPSE:2021.0721
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doi:10.3390/pr9010026
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Sep 21, 2021
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Calvin Tsay
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