DataVXACS Applied Materials & InterfacesPaper
journal article·2025-08-27

Enzyme-Responsive Peptide-Prodrug Integrated Biphasic Microneedle Patch for Enhanced Transdermal Delivery and Hypertension Therapy

Shibo Zhang, Bing Dong, Yao Shuai, Shuyue Deng, Jun Luo, Caixia Sun, Xing Ge, Lilin Chen, Hai Qian, Jianjun Dai, Yanmin Ju

ACS Applied Materials & Interfaces· Volume 17· Issue 34
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Source abstract

Abstract

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 K m 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.
Source: openalex_inverted_index · Quality: baseline

Research context

OpenAlex topics: Advancements in Transdermal Drug Delivery · Lipid Membrane Structure and Behavior · Advanced Drug Delivery Systems

SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.

Affiliations

School of Life Science and Technology

China Pharmaceutical University

Department of Environmental Engineering

Hebei University of Environmental Engineering

College of Pharmacy

Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China

Jiangsu Key Laboratory of Drug Discovery for Metabolic Disease, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, Jiangsu, China

MOE Joint International Research Laboratory of Animal Health and Food Safety, Key Laboratory of Animal Bacteriology, Ministry of Agriculture, College of Veterinary Medicine

Nanjing Agricultural University

Funding

Natural Science Foundation of Hebei Province · State Key Laboratory of Natural Medicines · Jiangsu Provincial Department of Science and Technology · Fundamental Research Funds for the Central Universities · National Natural Science Foundation of China

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