Date of Award

2022

Document Type

Thesis

Degree Name

Master of Science (MS)

Department

Pharmaceutics

First Advisor

Rutesh Dave

Committee Chair and Members

Rutesh Dave, Chair

Grazia Stagni

Devang Patel

Harsh Shah

Keywords

Ascorbic acid, Design of experiments, Oral dissolving films, Oral dissolving strips, Vitamin C

Abstract

People are becoming increasingly health conscious and the popularity of dietary supplements is growing. More specifically, consumers have become focused on improving the beauty of their hair, skin and nails and improving the health of their immune systems. Vitamin C or ascorbic acid provides many health and beauty benefits. Because humans are unable to synthesize vitamin C endogenously, it is an essential dietary component that one must consume either through foods or through supplements. For beauty, ascorbic acid supports the biosynthesis of collagen which is important for maintaining skin’s elasticity as well as for wound healing. Ongoing research studies are evaluating the role of ascorbic acid in immune function and its antioxidant activity that limits the damaging effects of free radicals or reactive oxygen species. Ascorbic acid is a water-soluble vitamin and its Biopharmaceutics Classification System (BCS) assignment is Class 3: high solubility, low permeability. The oral dissolving film (ODF) is a potential dosage form for dietary supplementation because it acts by dissolving rapidly on the oral mucosa, an area that has high permeability and blood supply. This is advantageous because tablet supplements that need to be swallowed are subject to the effects of first pass metabolism, enzymatic degradation and lower solubility in the gastrointestinal tract. ODFs are also a more accessible option for any consumer who has difficulty swallowing pills or who simply wants to consume something on the go, without the need for water. The current research project endeavors to identify and validate the optimal oral dissolving film formulation with ascorbic acid as the active pharmaceutical ingredient (API). To develop a well-functioning oral dissolving film, it is crucial to choose the ingredients that will maximize efficient drug delivery through the oral mucosa. The key formulation components of an oral dissolving film include the API, film forming polymer and plasticizer and other components may include: flavor agents, colorants, penetration enhancers, surfactants and saliva stimulating agents. The ingredients used besides ascorbic acid were HPMC E-5 as the film forming polymer, PEG-400 as the plasticizer, orange food coloring for the colorant and grapefruit oil as the flavoring agent. First, oral dissolving films that are on the market were evaluated as a benchmark for the current study. Then, a design of experiments software was used to generate a Box-Behnken study design with three key variables and 13 total trials. Each film was evaluated in triplicate through physical characterization (film length, width, thickness, weight, cross sectional area) and through their tensile strength, disintegration time and drug load. Through statistical analysis, the main effects and interactions between the variables on the resulting film characteristics were investigated. Then, the resulting optimal formula composition was created again as a confirmatory batch to validate the ideal composition. In summary, design of experiments methodology was successfully implemented to develop an optimal formulation for an oral dissolving film with ascorbic acid. The resulting film satisfactorily met the ideal ODF criteria by demonstrating a higher tensile strength, a lower disintegration time and a higher drug load.

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