Cyclodextrin as Functional Carrier in Development of Mucoadhesive Tablets Containing Polygoni cuspidati Extract with Potential for Dental Applications

Polygoni cuspidati root is a resveratrol-rich source with anti-inflammatory, angiogenic and neuroprotective effects. The raw material was standardized for the content of resveratrol, for which there is a special justification for administration within the oral mucosa. To improve the solubility of resveratrol and to assure its high content in plant material, an ultrasound-assisted extraction method was applied.

The addition of cyclodextrin was found to increase the extraction efficiency of resveratrol (from 13 to 297 µg per 1 g of plant material in case of 50% ethanol extracts) and enhanced its antioxidant activity as compared to pure Polygoni cuspidati extract/resveratrol. Cyclodextrin plays the role of a functional extract regarding technological properties (increasing the extraction of resveratrol from the extract, improving mucoadhesive properties). Therefore, the aim of this study was to develop mucoadhesive tablets containing combinations of the Polygoni cuspidati extract with a cyclodextrin carrier for buccal delivery.

The tests sequentially included extract preparation and characterization of its physical and biological properties and then formulation studies with a broad description of the prototype properties. The test results indicate that cyclodextrin increases the efficiency of resveratrol extraction from Polygoni cuspidati rhizome, which is a rich source of resveratrol, and its extract enclosed in a mucoadhesive tablet guarantees prolonged action at the site of administration.

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Materials: Plant raw material, Polygonum cuspidatum rhizome and root, was purchased from Herbapol Cracow (Krakow, Poland). Resveratrol (98%) (RSV) isolated from giant knotweed powder extract was supplied by PK Components (Warsaw, Poland). Emodin was obtained by Sigma-Aldrich (Poznań, Poland). Prisma™ HT buffer, Acceptor Sink Buffer, and GIT lipid solution were supplied by Pion Inc. (Billerica, MA, USA) Carbopol® 974 NF polymer was obtained by Lubrizol (Wickliffe, OH, USA), whereas β-cyclodextrin, hydroxypropyl-β-cyclodextrin average Mw ~ 1460 (0.8–1.0 MS Molar Substitution) and (hydroxypropyl)methyl cellulose (HPMC) with average Mn ~ 90,000 (~15,000 cP) and magnesium stearate were supplied by Sigma-Aldrich (Poznań, Poland). The following chemicals from Sigma-Aldrich (Poznań, Poland) were used: DMSO D4540, AChE C3389, BChE C7512, ATChI A5751, BTCh B3128, DTNB D8130, donepezil D6821, neostigmine N2001, magniflorine SMB00377, rivastigmine SML0881, eserine E8375, neocuproin N1501, CuCl2 307483, TPTZ 93285, Trolox 238813, fluorescein 46955, CoF2 236128, linoleic acid L1376, Tween 20 P1379, β-carotene C9750, Tween 80 P1754, ascorbic acid A92902, glutathione reductase G3664, glutathione (GSH) G4251, glutathione peroxidase G6137, nicotinamide adenine dinucleotide phosphate (NADPH) N5130, ethylenediaminetetraacetic acid (EDTA) E9884, glutathione disulfide (GSSG) G4626, superoxide dismutase (SOD) S5395, nitrobluetrazolium N6639, xanthine X0626, xanthine oxidase X4875. 2,2′-Azobis(2-amidinopropane) dihydrochloride (AAPH) was from Acros Organics (401560250), cyclooxygenase-2 (COX-2, human recombinant, 60122) and COX-2 activity assay kit (760151) were from Cayman Chemicals (Ann Arbor, MI, USA). Buffer salts, solvents and other reagents were from Sigma Aldrich (Poznań, Poland) and were at least of analytical grade. HPLC grade acetonitrile was obtained by Merck (Warsaw, Poland). High-quality pure water and ultra-high-quality pure water were prepared by using a Direct-Q 3 UV Merck Millipore purification system. Buccal mucosa from the porcine cheek was obtained from Bost slaughterhouse (Turosn Koscielna, Poland). Samples excised immediately after animal death were washed and frozen at −20 °C in isotonic saline solution. Prior to experiments, tissue was defrosted at ambient temperature and cut into pieces.

Article information: Paczkowska-Walendowska, M.; Szymańska, E.; Winnicka, K.; Szwajgier, D.; Baranowska-Wójcik, E.; Ruchała, M.A.; Simon, M.; Cielecka-Piontek, J. Cyclodextrin as Functional Carrier in Development of Mucoadhesive Tablets Containing Polygoni cuspidati Extract with Potential for Dental Applications. Pharmaceutics 2021, 13, 1916. https://doi.org/10.3390/pharmaceutics13111916