Separable and Inseparable Silk Fibroin Microneedles for the Transdermal Delivery of Colchicine: Development, Characterization, and Comparisons

Overview

Journal AAPS PharmSciTech

Publisher Springer

Specialty Pharmacology

Date 2023 Dec 19

PMID 38114734

Authors

Shiji Liao

Guirong Qiu

Yanping Hu

Bohong Guo

Yuqin Qiu

Affiliations

Soon will be listed here.

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.

Citing Articles

Ultrasonication-Induced Preparation of High-Mechanical-Strength Microneedles Using Stable Silk Fibroin.

Liang H, Chen J, Qiu G, Guo B, Qiu Y Polymers (Basel). 2024; 16(22).

PMID: 39599274 PMC: 11598507. DOI: 10.3390/polym16223183.

Microneedles as an Emerging Platform for Transdermal Delivery of Phytochemicals.

Gowda B, Ahmed M, Thakur R, Donnelly R, Vora L Mol Pharm. 2024; 21(12):6007-6033.

PMID: 39470172 PMC: 11615954. DOI: 10.1021/acs.molpharmaceut.4c00894.

Preparing a novel baicalin-loaded microemulsion-based gel for transdermal delivery and testing its anti-gout effect.

Wang Y, Liu M, Li J, Jiang P, Han D, Zhang H Saudi Pharm J. 2024; 32(6):102100.

PMID: 38812945 PMC: 11135029. DOI: 10.1016/j.jsps.2024.102100.

References

AlKadi H, Khubeiz M, Jbeily R . Colchicine: A Review on Chemical Structure and Clinical Usage. Infect Disord Drug Targets. 2017; 18(2):105-121. DOI: 10.2174/1871526517666171017114901. View

Burns C, Wortmann R . Latest evidence on gout management: what the clinician needs to know. Ther Adv Chronic Dis. 2013; 3(6):271-86. PMC: 3539261. DOI: 10.1177/2040622312462056. View

Caraco Y, Putterman C, Rahamimov R, Ben-Chetrit E . Acute colchicine intoxication--possible role of erythromycin administration. J Rheumatol. 1992; 19(3):494-6. View

Niel E, Scherrmann J . Colchicine today. Joint Bone Spine. 2006; 73(6):672-8. DOI: 10.1016/j.jbspin.2006.03.006. View

Luciani I . Fatal i.v. colchicine injection in a 60-year-old woman. J Emerg Nurs. 1989; 15(2( Pt 1)):80-2. View

STEMMERMANN G, Hayashi T . Colchicine intoxication. A reappraisal of its pathology based on a study of three fatal cases. Hum Pathol. 1971; 2(2):321-32. DOI: 10.1016/s0046-8177(71)80040-0. View

Ferron G, Rochdi M, Jusko W, Scherrmann J . Oral absorption characteristics and pharmacokinetics of colchicine in healthy volunteers after single and multiple doses. J Clin Pharmacol. 1996; 36(10):874-83. DOI: 10.1002/j.1552-4604.1996.tb04753.x. View

Rochdi M, Sabouraud A, Girre C, Venet R, Scherrmann J . Pharmacokinetics and absolute bioavailability of colchicine after i.v. and oral administration in healthy human volunteers and elderly subjects. Eur J Clin Pharmacol. 1994; 46(4):351-4. DOI: 10.1007/BF00194404. View

Marwah H, Garg T, Goyal A, Rath G . Permeation enhancer strategies in transdermal drug delivery. Drug Deliv. 2014; 23(2):564-78. DOI: 10.3109/10717544.2014.935532. View

10.

Matadh A, Jakka D, Pragathi S, Rangappa S, Shivakumar H, Maibach H . Polymer-Coated Polymeric (PCP) Microneedles for Controlled Dermal Delivery of 5-Fluorouracil. AAPS PharmSciTech. 2022; 24(1):9. DOI: 10.1208/s12249-022-02471-x. View

11.

Dabholkar N, Gorantla S, Waghule T, Rapalli V, Kothuru A, Goel S . Biodegradable microneedles fabricated with carbohydrates and proteins: Revolutionary approach for transdermal drug delivery. Int J Biol Macromol. 2021; 170:602-621. DOI: 10.1016/j.ijbiomac.2020.12.177. View

12.

Ahmad Z, Khan M, Siddique M, Sarwar H, Shahnaz G, Hussain S . Fabrication and Characterization of Thiolated Chitosan Microneedle Patch for Transdermal Delivery of Tacrolimus. AAPS PharmSciTech. 2020; 21(2):68. DOI: 10.1208/s12249-019-1611-9. View

13.

Yang Y, Song W, Wang N, Ren Y, Liu H . Tip-concentrated microneedle patch delivering everolimus for therapy of multiple sclerosis. Biomater Adv. 2022; 135:212729. DOI: 10.1016/j.bioadv.2022.212729. View

14.

Chen G, Hao B, Ju D, Liu M, Zhao H, Du Z . Pharmacokinetic and pharmacodynamic study of triptolide-loaded liposome hydrogel patch under microneedles on rats with collagen-induced arthritis. Acta Pharm Sin B. 2015; 5(6):569-76. PMC: 4675819. DOI: 10.1016/j.apsb.2015.09.006. View

15.

Raja W, Maccorkle S, Diwan I, Abdurrob A, Lu J, Omenetto F . Transdermal delivery devices: fabrication, mechanics and drug release from silk. Small. 2013; 9(21):3704-13. PMC: 3883884. DOI: 10.1002/smll.201202075. View

16.

Yucel T, Lovett M, Kaplan D . Silk-based biomaterials for sustained drug delivery. J Control Release. 2014; 190:381-97. PMC: 4142080. DOI: 10.1016/j.jconrel.2014.05.059. View

17.

Zhang L, Liu X, Li G, Wang P, Yang Y . Tailoring degradation rates of silk fibroin scaffolds for tissue engineering. J Biomed Mater Res A. 2018; 107(1):104-113. DOI: 10.1002/jbm.a.36537. View

18.

Lu Q, Zhang B, Li M, Zuo B, Kaplan D, Huang Y . Degradation mechanism and control of silk fibroin. Biomacromolecules. 2011; 12(4):1080-6. PMC: 3404841. DOI: 10.1021/bm101422j. View

19.

Yin Z, Kuang D, Wang S, Zheng Z, Yadavalli V, Lu S . Swellable silk fibroin microneedles for transdermal drug delivery. Int J Biol Macromol. 2017; 106:48-56. DOI: 10.1016/j.ijbiomac.2017.07.178. View

20.

Rnjak-Kovacina J, DesRochers T, Burke K, Kaplan D . The effect of sterilization on silk fibroin biomaterial properties. Macromol Biosci. 2015; 15(6):861-74. PMC: 4456215. DOI: 10.1002/mabi.201500013. View