Assessment of Binary Agarose–Carbopol Buccal Gels for Mucoadhesive Drug Delivery: Ex Vivo and In Vivo Characterization

Abstract

Agarose (AG) is a naturally occurring biocompatible marine seaweed extract that is converted to hydrocolloid gel in hot water with notable gel strength. Currently, its mucoadhesion properties have not been fully explored. Therefore, the main aim of this study was to evaluate the mucoadhesive potential of AG binary dispersions in combination with Carbopol 934P (CP) as mucoadhesive gel preparations. The gels fabricated via homogenization were evaluated for ex vivo mucoadhesion, swelling index (SI), dissolution and stability studies. The mucoadhesive properties of AG were concentration dependent and it was improved by the addition of CP. Maximum mucoadhesive strength (MS) (27.03 g), mucoadhesive flow time (FT) (192.2 min), mucoadhesive time in volunteers (MT) (203.2 min) and SI (23.6% at 4 h) were observed with formulation F9. The mucoadhesive time investigated in volunteers (MT) was influenced by AG concentration and was greater than corresponding FT values. Formulations containing 0.3%, w/v AG (F3 and F9) were able to sustain the release (~99%) for both drugs till 3 h. The optimized formulation (F9) did not evoke any inflammation, irritation or pain in the buccal cavity of healthy volunteers and was also stable up to 6 months. Therefore, AG could be considered a natural and potential polymer with profound mucoadhesive properties to deliver drugs through the mucosal route.

Formulation and Evaluation of Prednisolone Sodium Metazoate-Loaded Mucoadhesive Quatsomal Gel for Local Treatment of Recurrent Aphthous Ulcers: Optimization, In Vitro, Ex Vivo, and In Vivo Studies

“…When the whole system was motionless, the weight on the left pan was increased by adding water drops to create tension on the wire. The MF value was estimated based on the strength that made the gel detach from either mucosa surface [ 41 ]. The MF values of different quatsomal gels were estimated from the following equation MF.…”

Recent Advances in Nanotechnology Formulations to Treat Diseases of the Oral Cavity

“…The rate of drug release depends on both the viscosity of the gel and the nature and quality of the polymers [90]. The dose can be adjusted in gels and, moreover, the dose can be administered over a unit area for better contact, swelling, and effective drug release [101,102]. A scaffold or cross-linked gel structure increases the drug loading capacity.…”

“…Recently, a study evaluated salivary drug concentrations of the antiseptic and anesthetic agents tibezonium iodide and benzocaine, respectively, achieved through application of scaffold gels. The initial formulation (Figure 7) was prepared through homogenization of ingredients in aqueous solution and stored at room temperature [102]. Furthermore, in a study of the mucoadhesive role of agarose gel and Carbopol 934P, the concentration of agarose was responsible for sustained drug release.…”

Intranasal Administration of Dolutegravir-Loaded Nanoemulsion-Based In Situ Gel for Enhanced Bioavailability and Direct Brain Targeting

“…This would increase the retention of formulations at the nostrils and thereby prolong the duration of the drug release and subsequent therapeutic effect [28]. The most popular mucoadhesive ingredient for making in situ gel formulations is carbopol (polymer), because of its exceptional mucoadhesive characteristics [29]. This study aimed to formulate a Dolutegravir-loaded nanoemulsion and assess its achievability for nose-to-brain delivery.…”