Novel Bilayer Microarray Patch‐Assisted Long‐Acting Micro‐Depot Cabotegravir Intradermal Delivery for HIV Pre‐Exposure Prophylaxis

• Published in: Advanced functional materials Vol. 32; no. 9
• Main Authors: Tekko, Ismaiel A., Vora, Lalitkumar K., Volpe‐Zanutto, Fabiana, Moffatt, Kurtis, Jarrahian, Courtney, McCarthy, Helen O., Donnelly, Ryan F.
• Format: Journal Article
• Language: English
• Published: Hoboken Wiley Subscription Services, Inc 01.02.2022
• Subjects: cabotegravir; Disease prevention; dissolving microarray patch; HIV; Human immunodeficiency virus; In vivo methods and tests; long‐acting drugs; Materials science; Mechanical properties; pre‐exposure prophylaxis; Prophylaxis; Sodium salts; Tips
• ISSN: 1616-301X; 1616-3028
• DOI: 10.1002/adfm.202106999

Injectable long‐acting cabotegravir (CAB LA) is effective and safe for pre‐exposure HIV prophylaxis. It is recently approved for clinical use in those at high risk of contracting HIV. However, injections are invasive and access to trained healthcare personnel to administer CAB LA can be limited, especially in low‐income countries (LICs). Herein, for the first time, the development of a bilayer microarray patch (MAP) with unique design and novel formulation as a potential alternative self‐administrated intradermal delivery system for CAB is reported. The novel MAP has a high drug load (≈3 mg/0.5 cm2 of CAB LA or its micronized sodium salt) and fast‐dissolving tips (<30 min) and shows good mechanical properties and skin insertion capabilities. Importantly, in preclinical in vivo studies using Sprague Dawley rats, this MAP is able to implant the drug‐loaded tips in the skin, forming micro‐depots. Both drug forms are then released in a sustained manner, maintaining human therapeutic levels in the rats for one month after a single application. Weekly repeated MAP dosing in the rats showed the MAPs to be reproducible and well‐tolerated. This bilayer MAP presents a promising minimally‐invasive, self‐administered, alternative delivery system for CAB for enhanced HIV prevention, especially in LICs. A novel bilayer polymeric microarray patch (MAP) with highly drug‐loaded tips is developed for intradermal long‐acting delivery of cabotegravir for HIV pre‐exposure prophylaxis. This MAP is able to deliver substantial amounts of the drug into the skin as implanted micro‐depots, which are shown to maintain human therapeutic levels in rats for 1 month after a single application.