Abstract
Colchicine is the first-line option for both the treatment and prophylaxis of gout flares. However, due to potentially severe side effects, the clinical use of colchicine is limited. A well-tolerated and safe delivery system for colchicine is widely desired. For this purpose, colchicine-loaded inseparable microneedles were fabricated using silk fibroin. Additionally, separable microneedles made of silk fibroin as the needle tips and PVP K30 as the base material were developed. Both types of microneedles were evaluated for their mechanical strength, swelling and dissolution characteristics, insertion abilities, degradation properties, in vitro penetration, skin irritation, and in vivo anti-gout effects. The results demonstrated that separable microneedles had greater mechanical strength and insertion ability. Moreover, the separable microneedles separated quickly and caused little skin irritation. In the pharmacodynamic test, mice with acute gouty arthritis responded significantly to treatment with separable microneedles. In conclusion, the separable silk fibroin-based microneedles provide a promising route for colchicine delivery.
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Data Availability
The authors confirm that the data supporting the findings of this study are available within the article [and/or its supplementary materials].
Change history
22 March 2024
A Correction to this paper has been published: https://doi.org/10.1208/s12249-024-02779-w
Abbreviations
- COL:
-
Colchicine
- MNs:
-
Microneedles
- SF:
-
Silk fibroin
- SF-MNs:
-
Silk fibroin–based microneedles
- SF-SMNs:
-
Silk fibroin–based separable microneedles
- SF-IMNs:
-
Silk fibroin–based inseparable microneedles
- PVP-MNs:
-
PVP-based microneedles
- PF:
-
Parafilm
- SF-SMNs-COL:
-
Silk fibroin–based separable microneedles loaded with colchicine
- SF-IMNs-COL:
-
Silk fibroin–based inseparable microneedles loaded with colchicine
- SF-SMNs-blank:
-
Silk fibroin–based separable microneedles without drug
- SF-IMNs-blank:
-
Silk fibroin–based inseparable microneedles without drug
- i.g.:
-
Intragastric administration
- AGA:
-
Acute gout arthritis
- MSU:
-
Monosodium urate
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Funding
This work was supported by the Startup Fund for Distinguished Scholars of Guangdong Pharmaceutical University, and the Provincial university Students’ innovation and entrepreneurship training programs in 2021 (Grant No. S202110573031).
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Yuqin Qiu: conceptualization; writing—review and editing; supervision; project administration. Shiji Liao: investigation, formal analysis, writing—original draft.
Guirong Qiu: methodology, acquisition of data. Yanping Hu: methodology. Bohong Guo: resources.
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Liao, S., Qiu, G., Hu, Y. et al. Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons. AAPS PharmSciTech 25, 3 (2024). https://doi.org/10.1208/s12249-023-02716-3
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DOI: https://doi.org/10.1208/s12249-023-02716-3