Development and evaluation of microneedle systems for sustained transdermal delivery of entecavir

While entecavir (ETV) is a potent first-line agent for Hepatitis B treatment, its clinical effectiveness is often compromised by strict fasting requirements and the burden of daily adherence. Thus, there is a clear clinical need for alternative delivery strategies that offer sustained release and reduce dosing frequency.

This study explored microneedle (MN)-based transdermal systems as alternative platforms for sustained ETV delivery. Both dissolving microneedles (DMNs) incorporating the lipidic prodrug entecavir-3-palmitate (EV-P) and hydrogel-forming microneedles (HFMNs) loaded with ETV were evaluated. EV-P-loaded DMNs achieved sustained systemic exposure for up to 28 days following a single administration in vivo.