Academic Journal
Physicochemical Profiling of Baicalin Along with the Development and Characterization of Cyclodextrin Inclusion Complexes
| العنوان: | Physicochemical Profiling of Baicalin Along with the Development and Characterization of Cyclodextrin Inclusion Complexes |
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| المؤلفون: | Jakab, Géza, Bogdán, Dóra, Mazák, Károly, Deme, Ruth, Mucsi, Zoltán, Mándity, István M., Noszál, Béla, Kállai-Szabó, Nikolett, Antal, István |
| المساهمون: | Semmelweis University |
| المصدر: | AAPS PharmSciTech ; volume 20, issue 8 ; ISSN 1530-9932 |
| بيانات النشر: | Springer Science and Business Media LLC |
| سنة النشر: | 2019 |
| الوصف: | Baicalin is a flavone glycoside extracted from Scutellaria baicalensis , a traditional Chinese herbal medicine. Numerous pharmacological effects of baicalin were reported ( e.g. antioxidant, anxiolytic); nevertheless, the most important physicochemical properties influencing the pharmacokinetic behaviour and the concomitant oral bioavailability have not yet been described in a comprehensive study. The aim of this project was to characterize the acid-base, lipophilicity, biorelevant solubility and permeability properties of the drug substance and providing scientific data to support the dosage form design. Another important objective was the comparative evaluation of six various baicalin-cyclodextrin (CD) inclusion complexes along with the creation of a suitable Drug Delivery System (DDS) for this BCS IV drug. Biorelevant profiling was carried out by NMR-pH titrations, saturation shake-flask and distribution coefficients (log P ) measurements, while CD inclusion studies were fulfilled by experimental methods (phase solubility, 1 H/ 13 C NMR, 2D ROESY) and computational approaches. Due to low aqueous solubility (67.03 ± 1.60 μg/ml) and low permeability ( P app = 0.037 × 10 −6 cm/s), baicalin is classified as BCS IV. The γ-CD complexation significantly increased the solubility of baicalin (~ 5 times). The most promoted chemical shift change occurred in baicalin-γ-CD complex. Computational studies showed disparate binding pattern for baicalin in case of β- and γ-CD; furthermore, the calculated complexation energy was − 162.4 kJ mol −1 for β-CD, while it was significantly stronger for γ-CD (− 181.5 kJ mol −1 ). The physicochemical and structural information of baicalin and its CD complexes introduced herein can create molecular basis for a promising DDS with enhanced bioavailability containing a bioactive phytopharmacon. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| DOI: | 10.1208/s12249-019-1525-6 |
| DOI: | 10.1208/s12249-019-1525-6.pdf |
| DOI: | 10.1208/s12249-019-1525-6/fulltext.html |
| الاتاحة: | http://dx.doi.org/10.1208/s12249-019-1525-6 http://link.springer.com/content/pdf/10.1208/s12249-019-1525-6.pdf http://link.springer.com/article/10.1208/s12249-019-1525-6/fulltext.html |
| Rights: | https://creativecommons.org/licenses/by/4.0 ; https://creativecommons.org/licenses/by/4.0 |
| رقم الانضمام: | edsbas.1E3B5DF8 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1208/s12249-019-1525-6 |
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