Introduction

The administration of food supplements and drugs through the oral mucosa represents an innovative and highly efficient absorption modality .

This approach allows direct absorption of active substances through the oral mucosa, bypassing the gastrointestinal tract and first-pass hepatic metabolism.

It is particularly advantageous for improving bioavailability and ensuring a rapid onset of therapeutic action.

In this article, we will review the benefits , challenges , and innovations related to the delivery of supplements and drugs through the oral mucosa, providing a comprehensive review to better understand this mode of administration .

Advantages of Oral Mucosal Transport

One of the main advantages of oral mucosal delivery is rapid and effective absorption.

In fact, the absorption of active substances administered orally occurs rapidly , allowing the active ingredients to enter directly into the bloodstream through the capillaries present in various areas of the mouth, not just under the tongue.

This leads to a faster therapeutic effect than traditional oral administration.

In other words, patients may experience faster relief from their symptoms, which is crucial in situations where time is of the essence.

Another significant benefit is the increased bioavailability .

By avoiding first-pass hepatic metabolism, orally administered active substances show a significant increase in bioavailability .

This is especially useful for supplements and medications that are highly metabolized in the liver.

As a result, lower doses can be used to achieve the same therapeutic effect , thus reducing the risk of side effects.

Additionally, oral administration offers convenience and ease of use .

This modality is a preferred choice for patients who have difficulty swallowing tablets or capsules.

It is also a discreet and easy-to-use modality, requiring no water or special conditions for administration.

Therefore, it is particularly advantageous for elderly or pediatric populations, as well as for patients with swallowing difficulties .

Considerations on the Formulation

To maximize the benefits of oral mucosal delivery, it is essential to develop specific formulations that can dissolve rapidly and be absorbed efficiently through the oral mucosa.

Some of the key factors to consider include:

• Rapid Dissolution : Formulations must provide rapid dissolution in the oral cavity to allow timely absorption . This is crucial for products intended to treat acute conditions, such as severe pain or cardiovascular emergencies.
• Product Stability : The active substance must remain stable in the oral cavity environment, without degrading before being absorbed. This requires the use of excipients that can protect the active substance from the variable humidity and pH conditions of the mouth.
• Palatability : The taste of the product is a critical factor, as an unpleasant taste can affect patient compliance. It is essential to mask any bitter or unpleasant tastes by using appropriate flavorings and sweeteners.
• Bioadhesiveness : Oral formulations may benefit from bioadhesive features that help hold the product in place in the mouth for a sufficient period of time for absorption to occur.

Mechanism of Absorption Through Oral Mucosa

The mechanism of absorption through the oral mucosa involves the passage of active substances through the highly vascularized mucous membrane present in various areas of the mouth.

This membrane is thin and permeable , allowing substances to pass directly into the bloodstream.

Small, lipophilic molecules tend to be absorbed more easily, while hydrophilic and larger molecules may require specialized formulations to improve their permeability .

The absorption process can be influenced by various factors, including the solubility of the substance, the pH of saliva, the presence of enzymes in the mouth, and the amount of saliva produced.

To optimize absorption, oral formulations often include permeabilizing agents that increase the permeability of the oral mucosa.

Innovations in Oral Formulation Technology

Recent innovations in formulation technology have led to the development of new ways to improve the efficacy and stability of oral formulations .

Some of these advances include:

• Nanotechnology : The use of nanoparticles can improve the solubility and permeability of substances, facilitating absorption through the oral mucosa. Nanoparticles can also protect the active substance from degradation and improve its stability.
• Bioadhesive Polymers : Incorporating bioadhesive polymers into oral formulations can help keep the substance in place in the mouth for a longer period of time, improving absorption. These polymers can also provide a controlled release of the active substance.
• Oral Films : Oral films are thin strips that dissolve rapidly in the mouth, releasing the active substance . These films are easy to administer and can be formulated to improve the stability and palatability of the substance.

LifeLion® recognizes the multiple benefits of oral administration and has developed a complete line of food supplements using this innovative formulation technology.

All of our orodispersible supplements are designed to ensure rapid dissolution and efficient absorption, thus providing rapid relief and greater bioavailability.

We use high-quality ingredients and advanced technologies to ensure the stability and effectiveness of our products, making them an ideal choice for our users.

Conclusions

The delivery of supplements and drugs through the oral mucosa represents a promising option to improve the bioavailability and therapeutic efficacy of numerous products.

With the continuous advancement of research and technology , oral formulations will be able to offer increasingly effective and safe solutions for patients.

The implementation of new technologies and materials , together with a deeper understanding of the absorption mechanisms, will help to maximize the benefits of this delivery modality.

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FAQ

1. Which products are suitable for administration through the oral mucosa?

Products suitable for administration through the oral mucosa include food supplements , analgesics, nitroglycerin for angina, and some anxiolytics.

However, the formulation must be optimised to ensure stability and effective absorption of the active substance.

2. What are the main advantages of administration through the oral mucosa?

The main advantages include rapid absorption, increased bioavailability by avoiding first-pass hepatic metabolism, and ease of use for patients who have difficulty swallowing.

3. How does administration through the oral mucosa compare with other routes of administration?

Administration through the oral mucosa offers faster absorption and greater bioavailability than traditional oral administration.

However, it is important to consider the specific characteristics of the active substance to determine the most appropriate route of administration.

4. What technological innovations are improving oral mucosal delivery?

Innovations include the use of nanotechnologies to improve the solubility and permeability of substances, bioadhesive polymers to improve product retention in the mouth, and oral films for rapid and controlled release of the active substance.