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Updated: Sep 11, 2025

Author Spotlight: Innovative Microneedle-Based Strategies for Enhanced Exosome Delivery and Stability
Published on: July 12, 2024
Enzyme-Responsive Peptide-Prodrug Integrated Biphasic Microneedle Patch for Enhanced Transdermal Delivery and
Shibo Zhang1, Bing Dong2, Yao Shuai3
1School of Life Science and Technology, China Pharmaceutical University, Nanjing 211198, China.
None:
Hypertension is a major risk factor for cardiovascular diseases and needs effective blood pressure reduction. Current antihypertensive drugs, such as captopril, face challenges, including the enzymatic degradation and the liver first-pass effect. Here, we developed a dissolving microneedle (MN) loaded with a peptide-based enzyme-responsive prodrug peptide-captopril (PC) to enhance the stability of captopril and enable efficient transdermal delivery. Kinetic studies revealed that PC exhibited a lower Km value (1.1 × 10-5 M) for esterase-mediated hydrolysis compared to free captopril (2.1 × 10-5 M), indicating improved enzymatic stability. Meanwhile, PC was encapsulated stably in microneedle tips to form the PC MN, achieving approximately 90% transdermal drug delivery. In spontaneously hypertensive rat models, PC MN elicited a rapid and potent blood-pressure-lowering effect, outperforming oral captopril administration. This study presents a promising self-administering strategy to enhance hypertension treatment through efficient transdermal drug delivery.
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