Paczkowska-Walendowska Magdalena, Dvořák Jakub, Rosiak Natalia, Tykarska Ewa, Szymańska Emilia, Winnicka Katarzyna, Ruchała Marek A, Cielecka-Piontek Judyta
Department of Pharmacognosy, Poznan University of Medical Sciences, Święcickiego 4, 60-781 Poznań, Poland.
Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 3, 166 28 Prague, Czech Republic.
Pharmaceutics. 2021 Mar 20;13(3):417. doi: 10.3390/pharmaceutics13030417.
The health benefits of resveratrol have been proven to inhibit the development of numerous diseases. A frequent limitation in its use is a low bioavailability stemming from a poor solubility and fast enterohepatic metabolism. Thus, the aim of the research was to investigate the possibility to formulate mucoadhesive cyclodextrin- and xanthan gum-based buccal tablets in order to increase the solubility of resveratrol and to eliminate bypass enterohepatic metabolism. Systems of resveratrol with α-cyclodextrin (α-CD), β-cyclodextrin (β-CD), γ-cyclodextrin (γ-CD) and 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) prepared by the dry mixing method (ratio 1:1) were selected for the of tablets where xanthan gum was used as a mucoadhesive agent. They were identified on the basis of PXRD, FT-IR analysis. Tablets F1 (with α-CD), F2 (with β-CD) and F3 (with γ-CD) were characterized by the highest compactibility as well as by favorable mucoadhesive properties. Resveratrol release from these tablets was delayed and controlled by diffusion. The tablets prepared in the course of this study appear to constitute promising resveratrol delivery systems and are recommended to increase the effectiveness of the treatment in many diseases, particularly periodontitis.
白藜芦醇的健康益处已被证明可抑制多种疾病的发展。其使用中常见的一个限制是生物利用度低,这源于溶解度差和快速的肠肝循环代谢。因此,该研究的目的是研究制备基于环糊精和黄原胶的粘膜粘附口腔片的可能性,以提高白藜芦醇的溶解度并消除肠肝循环旁路代谢。通过干混法(比例1:1)制备的白藜芦醇与α-环糊精(α-CD)、β-环糊精(β-CD)、γ-环糊精(γ-CD)和2-羟丙基-β-环糊精(HP-β-CD)的体系被选用于制备口腔片,其中黄原胶用作粘膜粘附剂。通过粉末X射线衍射(PXRD)、傅里叶变换红外光谱(FT-IR)分析对它们进行了鉴定。片剂F1(含α-CD)、F2(含β-CD)和F3(含γ-CD)具有最高的可压性以及良好的粘膜粘附性能。这些片剂中白藜芦醇的释放被延迟并受扩散控制。在本研究过程中制备的片剂似乎构成了有前景的白藜芦醇递送系统,并且被推荐用于提高许多疾病,特别是牙周炎的治疗效果。