Antiviral prodrugs and nanoformulations thereof

Nanoformulations of cabotegravir prodrugs with aliphatic modifications provide sustained drug release and improved biodistribution, addressing limitations of current LAPs by maintaining effective plasma concentrations and reducing injection site reactions, thus enhancing HIV treatment adherence and efficacy.

AU2024213169B2Pending Publication Date: 2026-07-16BOARD OF RGT UNIV OF NEBRASKA

Patent Information

Authority / Receiving Office
AU · AU
Patent Type
Applications
Current Assignee / Owner
BOARD OF RGT UNIV OF NEBRASKA
Filing Date
2024-08-22
Publication Date
2026-07-16

AI Technical Summary

Technical Problem

Current long-acting antiretroviral (LAP) formulations of cabotegravir (CAB) face challenges such as intolerable injection site reactions, limited dosing intervals, and variable drug absorption, necessitating improvements in formulation to enhance regimen adherence and maintain effective plasma concentrations.

Method used

Development of prodrugs of integrase inhibitors, such as cabotegravir, modified with aliphatic or alkyl groups, encapsulated in nanoparticles with amphiphilic block copolymers, to create stable nanoformulations that provide sustained drug release and improved biodistribution.

Benefits of technology

The nanoformulations achieve prolonged plasma half-life and tissue retention of cabotegravir, maintaining therapeutic levels for up to a year with reduced injection volumes and adverse reactions, enhancing treatment adherence and efficacy against HIV.

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Abstract

The present invention provides prodrugs and methods of use thereof. 64 20 24 21 31 69 22 A ug 2 02 4 A B S T R A C T 2 0 2 4 2 1 3 1 6 9 2 2 A u g 2 0 2 4 6 4
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