Drug Delivery Through Oral Mucoadhesive Films

Meir Haber, Biota Ltd, Or Akiva, Israel
Irina Lir, Biota Ltd, Or Akiva, Israel

Transmucosal administration of drugs to the bloodstream via the highly permeable and readily accessible oral cavity mucosa is a non-invasive alternative to injections that prevents the metabolism and increase the bio-availability of poorly absorbed drugs.

Oral mucoadhesive films (OMF) are a convenient vehicle for oral transmucosal drug delivery that are advantageous over gels and sprays due to their ability to provide adherence and long residence time, exact dose and large contact area, thus enhancing drug absorption.
Effects of viscosity grade of alginate-based OMF prepared by aqueous solvent-evaporation technique on the properties of OMF have been studied.

Viscosity of alginate solutions was measured using Brookfield viscometer.

Films' swelling and dissolution as well as effects of plasticizers on the films properties and release kinetics were evaluated in saline solution at 370C.

Mechanical properties were evaluated by tensile test using INSTRON universal testing machine at a cross-head speed of 0.1mm/sec. Human volunteers tested in–vivo mucoadhesion and oral palate residence time.

It was found that viscosity of alginate 5% (w/v) solutions ranges was from 50cP to over 20,000cP (semi-gel).

Heating was required for hydration and casting high viscosity grades.

All films possess strong adherence to the oral palate, non-slimy swelling and tailored residence time. Oral palate residence time was significantly affected by both film thickness and alginate viscosity.

Addition of plasticizers increased elasticity of the films, decreased their strength and residence time, but only slightly affected swelling.
The results indicate that alginate viscosity significantly influence film swelling and oral mucosa residence time, but have little effect on mechanical properties of the films.

Alginates 5% (w/v) solutions possessing viscosity range of 1000-5000cP have been found optimal for OMF formulation. Properties of nicotine incorporated smoking cessation aid OMF, in particular nicotine stabilization and acrid taste masking will be described.