Evaluation and Optimization of Prolonged Release Mucoadhesive Tablets of Dexamethasone for Wound Healing: In Vitro–In Vivo Profiling in Healthy Volunteers

Abstract

The aim of the projected study was to design and develop a novel strategy for evaluating the mucoadhesive potential of polymeric tablets of dexamethasone (DXM) for local delivery against wounds. Therefore, formulations (Q1–Q7) were synthesized via direct compression method by varying the concentrations of polymers, i.e., ethyl cellulose (EC) and agar extract (AG). Moreover, the mucoadhesive polymeric tablets were characterized via physicochemical, in vitro, ex vivo and in vivo experiments. However, physicochemical characteristics such as FTIR showed no interaction with different polymeric combination. Surface pH of all formulations was normal to slightly alkaline. Highest hydration of up to 6.22% and swelling index was comprehended with maximum concentration of AG (50% of total tablet weight). Whereas, ex vivo and in vivo residence time and mucoadhesion were attributed to the increased concentrations of polymers. Moreover, Q7, (optimized formulation), containing 10% of EC and 40% of AG, exhibited maximum release of DXM (100%) over 8 h, along with sufficient mucoadhesive strength up to 11.73 g, following first-order kinetics having r2 value of 0.9778. Hemostatic effects and epithelialization for triggering and promoting wound healing were highly pronounced in cases of Q7. Furthermore, in vivo residence time was 7.84 h followed by salivary drug concentration (4.2 µg/mL). However, mucoadhesive buccal tablets showed stability for 6 months, thus following the standardization (ICH-Iva) stability zone. In summary, DXM mucoadhesive tablets seem to be an ideal candidate for eradication of wound infections via local targeted delivery.

Release Kinetics of Dexamethasone Phosphate from Porous Chitosan: Comparison of Aerogels and Cryogels

“…These dressings were effective in preventing wound fibrosis. In another study, it was shown that a much lower concentration (0.5–3.5 μg/mL), obtained with Dex-P releasing from cellulose/agar tablets, is effective to trigger buccal wound healing . The concentrations of Dex-P in aerogels and cryogels obtained in our work (some tens of μg/mL, see Figure S3) are in between the values presented in the publications cited above; by modulating the type of material (cryogel or aerogel), its density, and the drug concentration in the loading bath, drug concentration in our porous chitosans can be adjusted to the desired therapeutic response.…”

Exorbitant Drug Loading of Metformin and Sitagliptin in Mucoadhesive Buccal Tablet: In Vitro and In Vivo Characterization in Healthy Volunteers

“…However, the cell viability for all the formulations with a modified polymeric system was also higher than 70% as compared to the control, i.e., 45%, with a statistical significance of (p < 0.05), as shown in Figure 8. The peaks of MET and SIT were separated according to the devised conditions with the respective values of 1.96 and 3.70 min, as reported in the preliminary findings associated with the current study [41].…”

“…Surface pH For the measurement of surface pH, the tablets were allowed to swell in 10 mL of distilled water adjusted to pH 6.8 for 2 h, at 37.5 • C on a hot plate. The surface pH was then measured by touching the electrode of the pH meter on the surface of the tablet and allowing it to equilibrate approximately for 1 min [26,41].…”

“…High Performance Liquid Chromatographic (HPLC) method was adopted with instrumental conditions as reported by Aqeela et al [41] for the simultaneous estimation of metformin hydrochloride and sitagliptin phosphate monohydrate in the mucoadhesive tablet. Briefly, the mobile phase was composed of acidified water: methanol (6:4) volumetrically and adjusted to pH 3.0.…”

Mechanochemical Properties of Mucoadhesive Tablets Based on PVP/HPβCD Electrospun Nanofibers as Local Delivery of Polygoni cuspidati Extract for Treating Oral Infections

“…To better understand the mechanism of release, it is worth looking at the diffusional exponent n for Korsmeyer-Peppas kinetics, which describes the release as anomalous (for values 0.43 < n < 0.89), suggesting that the combination of diffusion and erosion contributes to the control of drug release [26]. This release mechanism is characteristic of many PVP-based mucoadhesive formulations [27,28]. To better illustrate the differences in the release profiles, in the absence of statistically significant differences between the profiles for different compression forces, the profiles for TP and TN were averaged, and are presented in Figure 4.…”