Mucoadhesive Buccal Tablet for Prolonged Acyclovir Release
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Solution Overview
Problem
Current treatments for orofacial herpes, such as acyclovir tablets and creams, have poor bioavailability and require frequent administration, leading to incomplete efficacy and patient compliance issues, as they do not effectively target the latent HSV reservoir and fail to prevent recurrence or alleviate symptoms like pain and discomfort.
Innovation Solution
A prolonged release mucoadhesive buccal tablet containing acyclovir, designed to adhere to the oral mucosa for at least 5 hours and provide sustained release for 20 hours, achieving high salivary concentrations to target the viral reservoir and reduce recurrence and symptom severity with a single dose.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional acyclovir tablets or creams are used for treatment, then the drug can be administered, but bioavailability is poor and frequent administration is required leading to incomplete efficacy
Solution Approach 1:
The buccal tablet is segmented into functional layers including a mucoadhesive layer for attachment and a drug release layer containing acyclovir. This segmentation allows the tablet to adhere to the buccal mucosa and provide sustained drug release over multiple days, eliminating the need for frequent administration while maintaining efficacy.
Solution Approach 2:
The buccal mucosa serves as an intermediary site between the administered tablet and the systemic circulation. The tablet adheres to the buccal mucosa, allowing direct absorption of acyclovir into the bloodstream, bypassing the gastrointestinal tract and first-pass metabolism, thereby improving bioavailability and enabling less frequent dosing.
2Reliability
If conventional treatments are used, then administration is simple, but they do not effectively target the latent HSV reservoir and fail to prevent recurrence
Solution Approach 1:
The buccal tablet is applied at the prodromal stage, before visible lesions appear, when viral replication is active but lesions are not yet formed. This preliminary action allows the drug to intercept viral replication early, preventing lesion development and reducing recurrence frequency.
Solution Approach 2:
The mucoadhesive buccal tablet provides continuous drug release over 2-3 days, maintaining therapeutic acyclovir levels at the application site and in saliva. This continuous action ensures sustained antiviral pressure on the latent reservoir, preventing recurrence more effectively than intermittent conventional dosing.
3Quantity of substance
If conventional creams are applied, then local treatment is possible, but they require frequent application and do not achieve sufficient drug concentrations in saliva
Solution Approach 1:
The buccal tablet is applied once and remains adhered to the buccal mucosa for 2-3 days, automatically providing sustained drug release into saliva without requiring repeated patient applications. The tablet self-maintains therapeutic drug levels in saliva through its prolonged release mechanism, eliminating the need for frequent reapplication.
4Ease of operation
If a single dose is used, then patient compliance improves, but achieving sufficient drug levels and duration of action is challenging
Solution Approach 1:
The tablet formulation incorporates specific polymers and excipients that control drug release kinetics, maintaining acyclovir concentrations above the minimum inhibitory level for 2-3 days from a single application. This parameter optimization allows a single dose to provide sufficient duration of action while improving patient compliance.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The mucoadhesive buccal tablet significantly reduces the duration and severity of orofacial herpes episodes, increases the number of aborted lesions, improves patient compliance, and maintains effective acyclovir concentrations in saliva and mucosa, thereby reducing viral load and transmission.
Implementation Method 1
a mucoadhesive buccal tablet (e.g., by applying the mucoadhesive buccal tablet to the oral mucosa), said mucoadhesive buccal tablet adheres to said oral mucosa for a period of at least 5 hours following administration
Implementation Method 2
the mucoadhesive buccal tablet provides sustained release of said acyclic guanosine antiviral agent for a period of at least 20 hours following administration
Data Source
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AI summary
The present invention relates to the treatment and/or prevention of muco-cutaneous herpes simplex virus diseases using prolonged release mucoadhesive buccal tablets comprising an acyclic guanosine antiviral agent. These tablets are particularly suitable for the treatment and/or prevention of orofacial herpes.