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Monday, 16 February 2015 13:48

Technical Report: Assessment of the Mucoadhesive Properties of MucoLox™ Using a 3D Model of the Human Oral Mucosa

Introduction:

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Delivery of medication via the oral mucosa has been continuously evolving since the mid-1980s due to the development of novel delivery systems, allowing for increased efficacy upon delivery. Since then, the oral mucosa has been an ideal target for drug delivery due to the ability of the medication to bypass first-pass metabolism, avoid gastrointestinal degradation, and achieve more rapid onset of action. Within the oral mucosa lies the buccal mucosa, which is composed of non-keratinized epithelial cells that line the inner cheeks. Buccal delivery is advantageous in that the buccal mucosa is highly vascularized, has low levels of enzymatic activity, and is fairly immobile, making it a suitable site for both local and systemic delivery of medication. However, one of the greatest disadvantages of buccal delivery is the low residence time (time at site of action) of the medication. This can be due to various factors such as continuous secretion of saliva triggering involuntary swallowing, intake of food, and movement of the tongue. All these factors can influence the efficacy of the compounded medication. Recognition of the drawback has led to the development of mucoadhesive polymers, a delivery system that adheres to the mucosal lining of the cheeks and prolongs residence time. The primary purpose of this study is to assess the mucoadhesive properties of MucoLox, a polymer gel, in comparison to a mucoadhesive commercial reference product, using the EpiOral model (MatTek Corporation), a highly differentiated three-dimensional (3D) model of the human oral mucosa. MucoLox is a proprietary polymer gel designed to improve mucoadhesion and prolong retention of medications at application sites within the oral mucosa.

 

Abstract:

The buccal mucosa is a common site for delivery of medication in the treatment of disease and conditions of the oral mucosa. However, low residence time at the site of action is a drawback for buccal delivery, increasing the need for mucoadhesive polymers. This study examines the mucoadhesive properties of MucoLox, a polymer gel, in comparison to a reference product, when applied on an EpiOral™ tissue model, a three-dimensional (3D) model of the human oral mucosa. Results show that sample retention for MucoLox was 24 times longer than for the reference product. The ability of MucoLox to prolong contact between the medication and the site of action has the potential to increase the efficacy of the compounded medication and to reduce the need for frequent dosing.

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Conclusions:

Optimal mucoadhesive properties exhibited by MucoLox are ideal features sought after by many compounding pharmacists searching for bases to be used in the treatment of diseases and conditions of the oral mucosa. These conditions include, but are not limited to, mucositis (ulceration and inflammation of mucous membranes), candidiasis (fungal infection), recurrent ulcers (herpes virus), bacterial infections, and trauma of the oral mucosa. For instance, in the case of mucositis in cancer patients, the ulceration and inflammation of the mucous membranes as a result of radiation and chemotherapy can be very painful and uncomfortable for patients. For this reason, pharmacists often want to compound medications that will not add additional burden to a patient’s medication regimen. It is then beneficial to use a base with high mucoadhesive strength and long mucosal retention to prolong the contact between the medication and the site of action. This reduces the need for frequent dosing as the effectiveness of each dose is optimized. The active ingredients are not washed away with the base by saliva and can remain at the affected site, facilitating the treatment process. The concept of increased efficacy with less frequent dosing potentially achieved with MucoLox can be appealing to patients who are already in pain and discomfort from the underlying condition, overall, improving their compliance with the medication regimen.

Download the complete PDF detailing the results of this study.

Click to learn more about MucoLox.