Jeremy “Will” McKee is Senior Innovation Chemist at Univar Solutions.

Will McKee

Fast dissolving oral film, a solid dosage form which disintegrate and dissolve within one minute when placed in the mouth without drinking water or chewing, fast soluble films are thin and act rapidly | Image Source: ©Tamer -stock.adobe.com

As consumer expectations evolve and the demand for more patient-friendly medication formats grows, innovation in drug delivery systems has become essential. Orally dissolving films (ODFs) have emerged as a solution, particularly for individuals experiencing pill fatigue or those who struggle with swallowing such as children, the elderly, or patients with dysphagia

ODFs are ultra-thin, flexible strips that dissolve quickly when placed on the tongue, requiring no water. They are designed to deliver active ingredients, whether pharmaceutical or nutritional, directly through the oral mucosa, offering a fast and efficient route into the bloodstream. While examples of ODFs containing nutraceutical and pharmaceutical active ingredients exist in the marketplace today, most of them contain just 1 or 2 active ingredients set in a polysaccharide-based matrix film.

The aim of this study was to develop and optimize an ODF formulation containing a synergistic blend of active ingredients that support energy and mental alertness in a strategic combination of natural and synthetic excipients to achieve a balance between controlled actives release and rapid onset of action.

A series of formulations were developed using the solvent casting technique that allow the adjustment of polymer concentration, solvent type, and drying conditions and suitable for heat-sensitive vitamins as the drying temperatures are generally lower. The optimized formulation included synthetic polymer hydroxypropyl methylcellulose (HPMC) (Headcel 60HD4000) (2%), natural polymer high methoxyl rapid set pectin (10%), polyethylene glycol (PEG) (1%), lactose monohydrate (2%), and sodium starch glycolate (1%).

Active ingredients and flavors included the following:

Delivering of dosages (100% DV) based on 200mg ODF

sour cherry was used as the flavoring agent, and vitamin B2 served as the colorant, imparting a yellow hue to the final film.

The following two methods were evaluated for incorporating the active ingredients:

Formula 1: Addition of actives and PEG before being added to the polymer mix.

Formula 2: Actives dissolved in water with PEG, then mixed into the polymer mix.

In both methods, water was used as the primary solvent for blending all components. The process map given as in 

. Post drying the films were cut into 2x2cms postage stamp size strips. As though both methods gave promising results, Formula 2 was selected for further testing parameters. Characterization and testing the final formula 2 films were evaluated using the following techniques:

Thickness uniformity was measured using a Positector 6000 thickness gauge.

Mechanical properties: Puncture/penetration test Assessed via texture profile analysis (TPA).

Assay of active ingredients: absorbance using ultraviolet-visible (UV-VIS) spectrophotometer (GENESYS 10S).Films (200 mg) were compared against standard solutions of each raw material.

Fourier transform infrared (FT-IR) spectroscopy was used to analyze both raw materials and the final dry Formula 2 films to confirm chemical integrity and compatibility.

Stability testing was conducted in a temperature-controlled chamber at 45 

Figure 1: Process Map for ODF Development. Figure courtesy of the authors.

Visually, the films from both formulas appeared uniform and exhibited a smooth finish. The final films from Formula 2 maintained a consistent thickness within the target range of 80-100 microns with weight of the film less than 100mg. Mechanical testing using a texture analyzer, demonstrated that the films possessed excellent mechanical strength (

Figure 2A. Quality metrics – Thickness and Mechanical Strength. FIgure courtesy of the authors.

Figure 2b. Figure courtesy of the authors

Figure 2C. Figure courtesy of the authors.

Analytical evaluations confirmed the identity and consistency of the films:

FT-IR spectroscopy revealed that the spectral profiles of the films matched those of the individual raw materials (

UV-VIS absorbance overlays showed alignment further validating the formulations (

Figure 3A. Assay and Identity of the Ingredients. Figures courtesy of the authors.

Additionally, the films exhibited excellent disintegration performance, dissolving completely in water within 30 seconds. Stability profile showed intact actives and identical to the control.

The project delivered a patient-friendly ODF that can deliver 100% DV actives in 200mg strip. The dosage can be adjusted based on the requirement. Through systematic formulation using a combination of synthetic and natural polymers, along with carefully selected excipients, the final films achieved desirable mechanical strength, uniformity, and rapid disintegration. Both formulation methods produced films that met critical quality attributes. Analytical techniques, such as FT-IR and UV-Vis spectroscopy, confirmed the presence and stability of active ingredients, ensuring the integrity of the final product. The films’ ability to dissolve within 30 seconds, supports the purpose. This study supports the potential of ODFs as a versatile platform for delivering vitamins, nutraceuticals, and pharmaceutical actives.

Gupta MS, Kumar TP, Gowda, DV, et al. Orodispersible thin film: A new patient-centered innovation. 

Journal of Drug Delivery Science and Technology

 October 2020 59, 101843 doi:10.1016/j.jddst.2020.101843

Articles

Orally dissolving films were optimized to deliver an energy/alertness nutraceutical blend for patients with pill fatigue or dysphagia. Solvent casting with low-temperature drying enabled incorporation of heat-sensitive vitamins using a hybrid polymer matrix of HPMC and high-methoxyl pectin with PEG, lactose, and sodium starch glycolate. A water-based premix of actives (vitamins B2, B6, C, and caffeine) with PEG improved incorporation. Final 2×2 cm films showed 80–100 µm thickness uniformity, strong mechanical performance, complete disintegration within 30 seconds, and 4-week stability at 45°C.

The aim of this study was to develop and optimize an orally dissolving film formulation containing a blend of active ingredients in a strategic combination of natural and synthetic excipients to achieve a balance between controlled actives release and rapid onset of action.  