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.
Bibliographical noteFunding Information:
I.A.T. and L.K.V. contributed equally to the work. Thanks to ViiV Healthcare for supplying CAB LA injectable formulation, the micronized cabotegravir sodium and cabotegravir free acid. Thanks to Stephen Lloyd from the Biological Services Unit at Queen's University Belfast for his help while performing the in vivo studies. The authors would also like to thank the PATH team members who contributed to the strategic direction of this work and/or provided review and copyediting support, including Abra Greene, Maggie Kilbourne‐Brook, Annie Rein‐Weston, Jill Sherman‐Konkle, and Darin Zehrung. This project was made possible by the generous support of the American people through the United States Agency for International Development (USAID) through the United States President's Emergency Plan for AIDS Relief (PEPFAR), under the terms of Cooperative Agreement #AID‐OAA‐A‐17‐00015. The contents are the responsibility of QUB and PATH and do not necessarily reflect the views of USAID, PEPFAR, or the United States government. Also, this work was supported in part by EPSRC grant EP/S028919/1 and Wellcome Trust grant WT094085MA.
© 2021 The Authors. Advanced Functional Materials published by Wiley-VCH GmbH
- Condensed Matter Physics
- Electronic, Optical and Magnetic Materials
ASJC Scopus subject areas
- Materials Science(all)
- Condensed Matter Physics