Chitosan as a Functional Carrier for the Local Delivery Anti-Inflammatory Systems Containing Scutellariae baicalensis radix Extract

Abstract

The aim of the study was to establish the influence of chitosan on the preparation of systems containing Scutellariae baicalensis radix extract and to demonstrate the potential of anti-inflammatory action for the treatment of periodontitis. In the first stage, the impact of the variables (extraction mixture composition, temperature, and the number of extraction cycles) on the extracted samples’ biological characteristics was analyzed using the Design of Experiments (DoE) approach. The best conditions for baicalin, baicalein, and wogonin extraction from Scutellariae baicalensis radix were 80% methanol in the extraction mixture, 70 °C, and 4 cycles per 60 min. The DoE approach can be used to choose the best chitosan system parameters with equal success. An increase in the deacetylation degree of chitosan used in the system improved the potential for reducing free radicals and inhibiting the hyaluronidase enzyme. Also, increasing the degree of chitosan deacetylation results in increased resistance of the carrier to biodegradation and an extended baicalin release profile, which is also associated with an increase in the viscosity of the chitosan-based system. In total, the system of a freeze-dried extract with chitosan 90/500 in the ratio of 2:1 (system S9) turns out to be the one with the best physicochemical (high percentage of baicalin release and the highest viscosity conditioning the prolonged stay at the site of administration) and biological properties (the highest antioxidant and anti-inflammatory activities), resulting in the highest potential for use in the treatment of oral inflammatory diseases.

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

“…The X-ray diffractograms ( Figure 2 ) of the lyophilized extract and its system with chitosan show a large broadening of the diffraction peaks, which at low intensity indicates their amorphous structure, which was described previously [ 14 ]. HPMC is also amorphous in nature.…”

“…In the first stage, a lyophilized extract of Scutellariae baicalensis radix was obtained according to the procedure described previously [ 14 ]. In an earlier study, the phytochemical and biological properties (including antioxidant and anti-inflammatory activity) of the obtained extract were confirmed.…”

“…Bands of S. baicalensis lyophilized extract at 3330 cm −1 , 1720 cm −1 , and 1660 cm −1 are characteristic for vibration of the O–H, –COOH, and C=O groups, while signals at 1600 cm −1 and 1580 cm −1 for the C=C vibration of the aromatic rings in the structure of flavones. The broad bands in the range 1200–900 cm −1 are characteristic of vibrations of C–O bonds of saccharides [ 14 ]. For the HPMC spectrum, a wide band was observed at 3300 cm −1 , associated with the presence of -OH groups.…”

“…In this regard, baicalin release is preferred from an extrudate-based tablet (formulations F1, F3, and F5). For these formulations, as the most probable, the Higuchi model was shown, which best describes the release from the matrix system and suggests that the baicalin was primarily released by diffusion and that its release was from a homogeneous flat matrix that did not degrade [ 14 ]. Additionally, a good fit to Korsmeyer-Peppas with ‘n’ values in the range 0.45–0.89 indicated the release approximated the non-Fickian diffusion release mechanism [ 23 ].…”

“…The temperature on the freeze dryer shelf was heated and ranged from +15 °C to +20 °C; the temperature inside the product was estimated −4 °C; and the condensation temperature was set at −48 °C. The freeze-drying was conducted at reduced pressure (1.030 mbar) for 48 h. So obtained lyophilized extract was combined with chitosan 90:500 in a weight ratio of 2:1 and named as ‘system’ for further tests [ 14 ].…”