A high-dosage microneedle for programmable lidocaine delivery and enhanced local long-lasting analgesia
Source abstract
Abstract
Considering the staggering global prevalence of local pain affecting hundreds of million individuals, it is of great significance to develop advanced dosage forms or delivery systems for analgesic therapy to fulfill clinical applicability. In this study, a hydrogel microneedles (MNs) system made out of gelatin-methacryloyl (GelMA) was designed to deliver lidocaine hydrochloride (LiH) in a sustained manner, and the drug loading capacity of the GelMA MNs was increased considerably by using the backing layer reservoir. The in vitro and in vivo tests showed that the fabricated GelMA MNs are strong enough for reliable skin application, and achieve high drug delivery efficiency as compared with the commercial lidocaine patches. The Spared-nerve injury (SNI) model of rats was also prepared to test behavioral pain sensitivity in response to mechanical stimuli, which proved that the LiH/GelMA MNs can enhance and prolong the anesthetic effect of LiH. In addition, with biosafety evaluation in rats, the MNs treated site restored to normal appearance within several hours of application and no dermatosis-related side effects or behavior disorders were observed during the experiment. Together these results indicated that the use of GelMA MNs for transdermal delivery of LiH is an effective, safe and simple treatment method to provide a better choice for local long-lasting analgesia.
Source: europepmc · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Advancements in Transdermal Drug Delivery · Pain Mechanisms and Treatments · Dermatology and Skin Diseases
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (41)
Show source-provided references
1. Crisis: what crisis?10.1007/s005860050018 ↗
2. Incidence rates and treatment of neuropathic pain conditions in the general population10.1016/j.pain.2008.03.002 ↗
3. Pathophysiology of pain10.1007/s00423-004-0468-9 ↗
4. Mechanisms of disease: neuropathic pain—a clinical perspective10.1038/ncpneuro0113 ↗
5. Pain: pathways and physiology10.1016/j.cps.2019.11.001 ↗
6. Analgésicos tópicos10.1590/S0034-70942012000200010 ↗
7. Current status and future prospects of transdermal drug delivery10.1023/A:1016060403438 ↗
8. Molecular mechanisms of action of systemic lidocaine in acute and chronic pain: a narrative review10.1016/j.bja.2019.06.014 ↗
9. Subcutaneous lidocaine for treatment of neuropathic cancer pain10.1016/0304-3959(91)90180-6 ↗
10. Subcutaneous injection of drugs: literature review of factors influencing pain sensation at the injection site10.1007/s12325-019-01101-6 ↗
11. Recent advances in topical anesthesia10.17245/jdapm.2016.16.4.237 ↗
12. A basal-bolus insulin regimen integrated microneedle patch for intraday postprandial glucose control10.1126/sciadv.aba7260 ↗
13. Rai, microneedle array: applications, recent advances, and clinical pertinence in transdermal drug delivery
14. Fabrication of coated polymer microneedles for transdermal drug delivery10.1016/j.jconrel.2017.03.383 ↗
15. Insulin delivery systems combined with microneedle technology10.1016/j.addr.2018.03.011 ↗
16. Microneedles: a smart approach and increasing potential for transdermal drug delivery system10.1016/j.biopha.2018.10.078 ↗
17. Transdermal delivery of lidocaine-loaded elastic nano-liposomes with microneedle array pretreatment10.3390/biomedicines9060592 ↗
18. Lidocaine carboxymethylcellulose with gelatine co-polymer hydrogel delivery by combined microneedle and ultrasound10.3109/10717544.2014.935985 ↗
19. Lidocaine permeation from a lidocaine NaCMC/gel microgel formulation in microneedle-pierced skin: vertical (depth averaged) and horizontal permeation profiles10.1007/s13346-015-0229-z ↗
20. The effects of chemical and physical penetration enhancers on the percutaneous permeation of lidocaine through equine skin10.1186/1746-6148-10-138 ↗
21. Microneedle-assisted permeation of lidocaine carboxymethylcellulose with gelatine co-polymer hydrogel10.1007/s11095-013-1240-z ↗
22. Coating solid dispersions on microneedles via a molten dip-coating method: development and in vitro evaluation for transdermal delivery of a water-insoluble drug10.1002/jps.24159 ↗
23. Drug-coated microneedles for rapid and painless local anesthesia10.1007/s10544-016-0144-1 ↗
24. Development of lidocaine-coated microneedle product for rapid, safe, and prolonged local analgesic action10.1007/s11095-011-0524-4 ↗
25. Development of lidocaine-loaded dissolving microneedle for rapid and efficient local anesthesia10.3390/pharmaceutics12111067 ↗
26. Dissolving microneedles for rapid and painless local anesthesia10.3390/pharmaceutics12040366 ↗
27. Lidocaine-loaded fish scale-nanocellulose biopolymer composite microneedles10.1208/s12249-017-0758-5 ↗
28. Implantable polymeric microneedles with phototriggerable properties as a patient-controlled transdermal analgesia system10.1039/C6TB02718K ↗
29. Synthesis and properties of gelatin methacryloyl (GelMA) hydrogels and their recent applications in load-bearing tissue10.3390/polym10111290 ↗
30. Synthesis, properties, and biomedical applications of gelatin methacryloyl (GelMA) hydrogels10.1016/j.biomaterials.2015.08.045 ↗
31. Fabrication and in vitro evaluation of a sponge-like bioactive-glass/gelatin composite scaffold for bone tissue engineering10.1016/j.msec.2013.02.021 ↗
32. A fabrication method of microneedle molds with controlled microstructures10.1016/j.msec.2016.03.097 ↗
33. Preparation and characterization of novel carbopol based bigels for topical delivery of metronidazole for the treatment of bacterial vaginosis10.1016/j.msec.2014.08.026 ↗
34. Assessment and analysis of mechanical allodynia-like behavior induced by spared nerve injury (SNI) in the mouse10.1016/j.pain.2005.10.036 ↗
35. Spared nerve injury: an animal model of persistent peripheral neuropathic pain10.1016/S0304-3959(00)00276-1 ↗
36. Paw withdrawal threshold in the von frey hair test is influenced by the surface on which the rat stands10.1016/S0165-0270(99)00004-7 ↗
37. Carboxyl-modified poly (vinyl alcohol)-crosslinked chitosan hydrogel films for potential wound dressing10.1016/j.carbpol.2015.02.034 ↗
38. An update on the routes for the delivery of donepezil10.1021/acs.molpharmaceut.1c00290 ↗
39. Osteoconductive hybrid hyaluronic acid hydrogel patch for effective bone formation10.1016/j.jconrel.2020.09.006 ↗
40. Cell mediated cytotoxicity against U 937 cells by human monocytes and macrophages in a modified colorimetric MTT assay: a methodological study10.1016/0022-1759(91)90205-T ↗
41. Hemolysis and cytotoxicity mechanisms of biodegradable magnesium and its alloys10.1016/j.msec.2014.08.038 ↗