Hot Melt Extrusion as an Effective Process in the Development of Mucoadhesive Tablets Containing Scutellariae baicalensis radix Extract and Chitosan Dedicated to the Treatment of Oral Infections

Hot Melt Extrusion (HME) technology was developed to obtain blends containing lyophilized Scutellariae baicalensis root extract and chitosan in order to improve the rheological properties of the obtained blends, including tableting and compressibility properties. (Hydroxypropyl)methyl cellulose (HPMC) in 3 different ratios was used as amorphous matrix formers. The systems were characterized using X-ray powder diffraction (PXRD), Fourier Transform Infrared Spectroscopy with Attenuated Total Reflectance (FTIR-ATR), and in vitro release, permeability, and microbiological activity studies.

Then, the extrudates were used to prepare tablets in order to give them the appropriate pharmaceutical form. HPMC-based systems released baicalin more slowly, resulting in delayed peaks in the acceptor fluid. This behavior can be explained by the fact that HPMC swells significantly, and the dissolved substance must have diffused through the polymer network before being released. The best tabletability properties are provided by the formulation containing the extrudate with lyophilized extract HPMC 50:50 w/w. These tablets offer a valuable baicalin release profile while maintaining good mucoadhesive properties that condition the tablet’s retention in the application site and the effectiveness of therapy.

Download the full article as PDF here Hot Melt Extrusion as an Effective Process in the Development of Mucoadhesive Tablets Containing Scutellariae baicalensis radix Extract and Chitosan Dedicated to the Treatment of Oral Infections

or read it here

Materials

Baicalin (≥95%, HPLC) was obtained from Sigma-Aldrich (Poznan, Poland). Excipients, such as chitosan with a degree of acetylation of 90% with a viscosity range of 500 mPas (marked as 90/500), was supplied from Heppe Medical Chitosan GmbH (Halle, Germany), (hydroxypropyl)methyl cellulose (HPMC) with an average Mn~90.000 (~15.000 cP), and magnesium stearate, were supplied by Sigma-Aldrich (Poznan, Poland). Microcrystalline cellulose (MCC) VIVAPUR 102 was supplied by JRS PHARMA (Rosenberg, Germany). Reagent for mucoadhesive tests: mucin from porcine stomach was obtained from Sigma-Aldrich (Poznan, Poland). HPLC grade acetonitrile and water were obtained from Merck. High-quality pure water and ultra-high-quality pure water were prepared using an Direct-Q 3 UV Merck Millipore purification system.

Paczkowska-Walendowska, M.; Miklaszewski, A.; Szymanowska, D.; Skalicka-Woźniak, K.; Cielecka-Piontek, J. Hot Melt Extrusion as an Effective Process in the Development of Mucoadhesive Tablets Containing Scutellariae baicalensis radix Extract and Chitosan Dedicated to the Treatment of Oral Infections. Int. J. Mol. Sci. 2023, 24, 5834. https://doi.org/10.3390/ijms24065834