Dissolvable polymeric microneedles loaded with aspirin for antiplatelet aggregation

Baorui Wang; Suohui Zhang; Guozhong Yang; Zequan Zhou; Mengzhen Xing; Han Liu; Aguo Cheng; Yunhua Gao

doi:10.1016/j.ajps.2023.100776

Dissolvable polymeric microneedles loaded with aspirin for antiplatelet aggregation

Asian J Pharm Sci. 2023 Jan;18(1):100776. doi: 10.1016/j.ajps.2023.100776. Epub 2023 Jan 17.

Authors

Baorui Wang^{1

2}, Suohui Zhang^{1

3}, Guozhong Yang³, Zequan Zhou¹, Mengzhen Xing¹, Han Liu¹, Aguo Cheng¹, Yunhua Gao^{1

2

3}

Affiliations

¹ Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry of Chinese Academy of Sciences, Beijing 100190, China.
² School of Future Technology, University of Chinese Academy of Sciences, Beijing 101408, China.
³ Beijing CAS Microneedle Technology Ltd, Beijing 102609, China.

Abstract

To reduce mucosal damage in the gastrointestinal tract caused by aspirin, we developed a dissolvable polymeric microneedle (MN) patch loaded with aspirin. Biodegradable polymers provide mechanical strength to the MNs. The MN tips punctured the cuticle of the skin and dissolved when in contact with the subcutaneous tissue. The aspirin in the MN patch is delivered continuously through an array of micropores created by the punctures, providing a stable plasma concentration of aspirin. The factors affecting the stability of aspirin during MNs fabrication were comprehensively analyzed, and the hydrolysis rate of aspirin in the MNs was less than 2%. Compared to oral administration, MN administration not only had a smoother plasma concentration curve but also resulted in a lower effective dose of antiplatelet aggregation. Aspirin-loaded MNs were mildly irritating to the skin, causing only slight erythema on the skin and recovery within 24 h. In summary, aspirin-loaded MNs provide a new method to reduce gastrointestinal adverse effects in patients requiring aspirin regularly.

Keywords: Antiplatelet aggregation; Aspirin; Hydrolysis; Polymeric microneedles; Transdermal drug delivery.