Journal
ADVANCED HEALTHCARE MATERIALS
Volume 8, Issue 22, Pages -Publisher
WILEY
DOI: 10.1002/adhm.201900896
Keywords
5-aminolevulinic acid; dissolving microneedles; long-term stability; photodynamic therapy; superficial tumors
Funding
- National Natural Science Foundation of China [51703074, 51525302]
- China Postdoctoral Science Foundation [2017M612454]
- Program for HUST Academic Frontier Youth Team [2015-01]
- Scientific Research Training Program for Young Talents
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5-Aminolevulinic acid (5-ALA) is one of the most widely used prodrug in clinical photodynamic therapy of dermatological diseases and cancers; yet, its clinical application is still limited by the shallow skin penetration and unsatisfied stability in any existed formulations. Here, 5-ALA-loaded hyaluronic acid dissolving microneedles (5-ALA@HAMNs) are prepared for photodynamic therapy of superficial tumors. The HAMNs can not only assist the loaded 5-ALA to effectively penetrate the stratum corneum but also provide 5-ALA with an acidic and oxygen-free environment to reduce the dimerization of 5-ALA molecules via Schiff-base bonds and formation of inactive pyrazine derivatives, thus maintaining its chemical structure and biological activity. The chemical stability of 5-ALA in HAMNs is confirmed by UV-vis spectra and mass spectra measurements. The 5-ALA@HAMNs display remarkable tumor elimination both in vitro and in vivo, even after storage at room temperature for nine months, making it a highly potential device for effective delivery of 5-ALA in cancer photodynamic therapy.
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