Mucoadhesive Antiviral Inserts for Sustained On-Demand PrEP
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Solution Overview
Problem
Current HIV prophylaxis methods, such as daily oral tablets and long-acting injectables, face challenges with adherence, pill burden, potential drug resistance, and irreversible effects, necessitating a need for on-demand topical pre-exposure prophylaxis products.
Innovation Solution
Development of solid dosage forms containing tenofovir alafenamide fumarate (TAF) and elvitegravir (EVG) as vaginal or rectal inserts for on-demand administration, providing sustained release and mucoadhesive properties to enhance adherence and target local sites for HIV, HSV, and HBV prevention.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If daily oral tablet regimen is used for HIV prophylaxis, then continuous drug delivery is achieved, but adherence becomes difficult due to high pill burden
Solution Approach 1:
The patent segments the continuous prophylaxis regimen into on-demand dosing units (inserts) that can be taken individually after specific exposure events, eliminating the need for daily pill-taking and reducing overall pill burden while maintaining protective coverage
Solution Approach 2:
The patent implements periodic action by designing inserts that release drugs in sustained periods (e.g., 2-7 days) after single administration, replacing continuous daily dosing with intermittent periodic dosing that maintains therapeutic levels without requiring daily adherence
2Productivity
If long-acting injectable cabotegravir is used, then dosing frequency is reduced, but drug resistance risk increases due to long PK tail
Solution Approach 1:
The patent applies dynamics by designing inserts with adjustable drug release profiles that can be tailored to match specific exposure risk periods, allowing optimization of drug concentration over time to maintain efficacy while minimizing resistance development through appropriate pharmacokinetic tail management
Solution Approach 2:
The patent changes pharmacokinetic parameters by using mucoadhesive delivery systems that provide sustained release with controlled half-life, altering the drug's temporal profile to reduce the long PK tail associated with injectables while maintaining reduced dosing frequency
3Ease of operation
If topical insert formulation is used for on-demand PrEP, then adherence and targeted delivery are improved, but chemical stability of TAF becomes challenging
Solution Approach 1:
The patent uses mucoadhesive polymers and excipients as intermediaries that protect TAF from degradation in the topical insert formulation, enabling stable storage and controlled release while maintaining drug integrity throughout the shelf life and during delivery
Solution Approach 2:
The patent employs composite material formulations combining TAF with stabilizing excipients, polymers, and protective matrices in the insert, creating a chemically stable composite system that maintains drug potency while enabling on-demand topical delivery
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 inserts offer improved adherence, targeted delivery, reduced drug resistance, and cost-effectiveness, with potential for flexible dosing and self-administration, demonstrating effective prevention of HIV, HSV, and HBV through pre- and post-exposure applications.
Implementation Method 1
the solid dosage form provides sustained release of the antiviral active pharmaceutical ingredient when administered as a vaginal or rectal insert
Implementation Method 2
the solid dosage form exhibits a mucoadhesive detachment force of at least 0.1 N when measured in accordance with test method described herein with porcine vaginal mucosa
Data Source
AI summary
A pharmaceutical composition and methods for using the pharmaceutical composition are disclosed. The pharmaceutical composition may include a therapeutically effective amount of one or more antiviral active pharmaceutical ingredients and a pharmaceutically acceptable excipient. The pharmaceutical composition may be a solid dosage form, wherein the solid dosage form provides sustained release of the antiviral active pharmaceutical ingredient when administered as a vaginal or rectal insert.