Citation: Xuebing Jiang, Siyi Wang, Li Zhang, Xian Jiang, Maling Gou. Lidocaine hydrochloride loaded isomaltulose microneedles for efficient local anesthesia of the skin[J]. Chinese Chemical Letters, ;2024, 35(4): 108686. doi: 10.1016/j.cclet.2023.108686 shu

Lidocaine hydrochloride loaded isomaltulose microneedles for efficient local anesthesia of the skin

Xuebing Jiang ^{a, 1} ,
Siyi Wang ^{a, b, 1} ,
Li Zhang ^a ,
Xian Jiang ^c ,
Maling Gou ^{a, *,}

a.
State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu 610041, China
b.
Huahang Microcreate Technology Co., Ltd., Chengdu 610042, China
c.
Department of Dermatology, West China Hospital, Sichuan University, Chengdu 610041, China

goumaling@scu.edu.cn

Received Date: 10 April 2023
Revised Date: 8 June 2023
Accepted Date: 11 June 2023
Available Online: 16 June 2023

Figures(3)

Lidocaine hydrochloride (LIDH) as an anesthetic is widely used in local anesthesia. Dissolving microneedles (MNs) have great application value in the field of skin anesthesia. However, the limited drug-loading of dissolving MNs is an existing challenge that affects clinical use. In this study, we have screened isomaltulose (ISO) as the proper matrix material for the MNs by using molecular dynamics (MD) simulation. Our findings indicate that ISO has good compatibility with LIDH, and the LIDH-loaded ISO MNs (LI-MNs) have high drug-loading capacity. The drug-loading capacity of LI-MNs could reach 80%, and it could effectively puncture the skin. In addition, the preparation method of customized LI-MNs was established based on three-dimensional (3D) printing technology. It was shown that the administration time of LI-MNs could be controlled within 3 min. Also, the LI-MNs were able to provide the local anesthetic efficacy within 2 min and sustained for more than 2 h. Significantly, LI-MNs had more efficient drug efficacy compared to the topical creams and the majority of existing LIDH-loaded dissolving MNs. They even provided a longer duration of action than the injections. Overall, the LI-MNs with high drug-loading have a promising application prospect.
- Microneedles,
- Local anesthesia,
- Lidocaine hydrochloride,
- Isomaltulose,
- Transdermal delivery
1. [1]
  H. Yang, G. Kang, M. Jang, et al., Pharmaceutics 12 (2020) 1067. doi: 10.3390/pharmaceutics12111067
2. [2]
  M. Horikiri, K. Ueda, T. Sakaba, J. Plast. Surg. Hand Surg. 52 (2018) 94–96. doi: 10.1080/2000656x.2017.1342092
3. [3]
  K. Kabashima, T. Honda, F. Ginhoux, G. Egawa, Nat. Rev. Immunol. 19 (2019) 19–30. doi: 10.1038/s41577-018-0084-5
4. [4]
  M. Kumar, R. Chawla, M. Goyal, J. Anaesthesiol. Clin. Pharmacol. 31 (2015) 450–456. doi: 10.4103/0970-9185.169049
5. [5]
  M. Ali, S. Namjoshi, H.E. Benson, Y. Mohammed, T. Kumeria, J. Control. Release 347 (2022) 561–589. doi: 10.1016/j.jconrel.2022.04.043
6. [6]
  Z. Zeng, G. Jiang, T. Liu, et al., Biodes. Manuf. 4 (2021) 902–911. doi: 10.1007/s42242-021-00140-9
7. [7]
  P. Das, S. Manna, S. Roy, S.K. Nandi, P. Basak, Burns Trauma 11 (2023) tkac058. doi: 10.1093/burnst/tkac058
8. [8]
  M.R. Prausnitz, J. Adv. Drug Deliv. Rev. 56 (2004) 581–587. doi: 10.1016/j.addr.2003.10.023
9. [9]
  M. Sheng, Y. Chen, H. Li, Y. Zhang, Z. Zhang, Burns Trauma 11 (2023) tkad009. doi: 10.1093/burnst/tkad009
10. [10]
  Y. Wang, A.A. Sheng, X. Jiang, et al., Bio-Des. Manuf. 6 (2023) 255–267. doi: 10.1007/s42242-022-00221-3
11. [11]
  Y. Liu, T. Huang, Z. Qian, W. Chen, Chin. Chem. Lett. 34 (2023) 108103. doi: 10.1016/j.cclet.2022.108103
12. [12]
  S. Mdanda, P. Ubanako, P.P.D. Kondiah, P. Kumar, Y.E. Choonara, Polymers 13 (2021) 2405. doi: 10.3390/polym13152405
13. [13]
  J. Yu, Y. Xia, H. Zhang, et al., J. Drug Deliv. Sci. Technol. 78 (2022) 103984. doi: 10.1016/j.jddst.2022.103984
14. [14]
  H. Zhan, F. Ma, Y. Huang, et al., Eur. J. Pharm. Sci. 121 (2018) 330–337. doi: 10.1016/j.ejps.2018.06.014
15. [15]
  Y. Wang, Y. Guo, S. Qiang, et al., Front. Pharmacol. 12 (2021) 764351. doi: 10.3389/fphar.2021.764351
16. [16]
  W.L. Jorgensen, Science 303 (2004) 1813–1818. doi: 10.1126/science.1096361
17. [17]
  Q. Gao, C. Lu, X.W. Wang, et al., J. Mol. Model. 24 (2018) 95. doi: 10.1007/s00894-018-3609-8
18. [18]
  T.K. Min, T.L. Yoon, T.L. Lim, Mater. Res. Express 5 (2018) 065054. doi: 10.1088/2053-1591/aacdb7
19. [19]
  X. Liu, R. Li, X. Yuan, et al., ACS Appl. Mater. Interfaces 13 (2021) 60522–60530. doi: 10.1021/acsami.1c21489
20. [20]
  J. Cui, J. Huang, Y. Yan, et al., J. Colloid Interface Sci. 617 (2022) 718–729. doi: 10.1016/j.jcis.2022.03.046
21. [21]
  S.P. Davis, B.J. Landis, Z.H. Adams, M.G. Allen, M.R. Prausnitz, J. Biomech. 37 (2004) 1155–1163. doi: 10.1016/j.jbiomech.2003.12.010
22. [22]
  N. Roxhed, T.C. Gasser, P. Griss, G.A. Holzapfel, G. Stemme, J. Microelectromech. Syst. 16 (2007) 1429–1440. doi: 10.1109/JMEMS.2007.907461
23. [23]
  L. Peebles, B. Norris, Appl. Ergon. 34 (2003) 73–88. doi: 10.1016/S0003-6870(02)00073-X
24. [24]
  J. Cho, G.H. Kang, E.C. Kim, et al., Emerg. Med. J. 25 (2008) 732–734. doi: 10.1136/emj.2008.059014
25. [25]
  X. Zhang, X. Fu, G. Chen, Y. Wang, Y. Zhao, Adv. Sci. 8 (2021) 202101210.
26. [26]
  D. Zhang, D.B. Das, C.D. Rielly, J. Pharm. Sci. 103 (2014) 613–627. doi: 10.1002/jps.23835
27. [27]
  A. Rzhevskiy, A. Popov, C. Pavlov, et al., PLoS One 17 (2022) e0261641. doi: 10.1371/journal.pone.0261641
28. [28]
  P.J. Austin, A. Wu, G. Moalem-Taylor, J. Vis. Exp. (2012) 3393.
29. [29]
  X. Wu, L.Y. Xu, E.M. Li, G. Dong, Chem. Biol. Drug Des. 99 (2022) 789–800. doi: 10.1111/cbdd.14038
30. [30]
  B.M. Lee, C. Lee, S.F. Lahiji, et al., Pharmaceutics 12 (2020) 366. doi: 10.3390/pharmaceutics12040366
31. [31]
  H. Kathuria, H. Li, J. Pan, et al., Pharm. Res. 33 (2016) 2653–2667. doi: 10.1007/s11095-016-1991-4
1. [1]
  Qin Yu , Haisheng He , Jianping Qi , Yi Lu , Wei Wu . Oral delivery of insulin by barbed microneedles actuated by intestinal peristalsis. Chinese Chemical Letters, 2024, 35(9): 109888-. doi: 10.1016/j.cclet.2024.109888
2. [2]
  Dexuan Xiao , Tianyu Chen , Tianxu Zhang , Sirong Shi , Mei Zhang , Xin Qin , Yunkun Liu , Longjiang Li , Yunfeng Lin . Transdermal treatment for malignant melanoma by aptamer-modified tetrahedral framework nucleic acid delivery of vemurafenib. Chinese Chemical Letters, 2024, 35(4): 108602-. doi: 10.1016/j.cclet.2023.108602
3. [3]
  Haijun Shen , Yi Qiao , Chun Zhang , Yane Ma , Jialing Chen , Yingying Cao , Wenna Zheng . A matrix metalloproteinase-sensitive hydrogel combined with photothermal therapy for transdermal delivery of deferoxamine to accelerate diabetic pressure ulcer healing. Chinese Chemical Letters, 2024, 35(12): 110283-. doi: 10.1016/j.cclet.2024.110283
4. [4]
  Makhloufi Zoulikha , Zhongjian Chen , Jun Wu , Wei He . Approved delivery strategies for biopharmaceuticals. Chinese Chemical Letters, 2025, 36(2): 110225-. doi: 10.1016/j.cclet.2024.110225
5. [5]
  Ruru Li , Qian Liu , Hui Li , Fengbin Sun , Zhurui Shen . Rational design of dual sites induced local electron rearrangement for enhanced photocatalytic oxygen activation. Chinese Chemical Letters, 2024, 35(11): 109679-. doi: 10.1016/j.cclet.2024.109679
6. [6]
  Linghui Zou , Meng Cheng , Kaili Hu , Jianfang Feng , Liangxing Tu . Vesicular drug delivery systems for oral absorption enhancement. Chinese Chemical Letters, 2024, 35(7): 109129-. doi: 10.1016/j.cclet.2023.109129
7. [7]
  Fengjie Liu , Fansu Meng , Zhenjiang Yang , Huan Wang , Yuehong Ren , Yu Cai , Xingwang Zhang . Exosome-biomimetic nanocarriers for oral drug delivery. Chinese Chemical Letters, 2024, 35(9): 109335-. doi: 10.1016/j.cclet.2023.109335
8. [8]
  Quanyou Guo , Yue Yang , Tingting Hu , Hongqi Chu , Lijun Liao , Xuepeng Wang , Zhenzi Li , Liping Guo , Wei Zhou . Regulating local electron transfer environment of covalent triazine frameworks through F, N co-modification towards optimized oxygen reduction reaction. Chinese Chemical Letters, 2025, 36(1): 110235-. doi: 10.1016/j.cclet.2024.110235
9. [9]
  Jing Zhang , Charles Wang , Yaoyao Zhang , Haining Xia , Yujuan Wang , Kun Ma , Junfeng Wang . Application of magnetotactic bacteria as engineering microrobots: Higher delivery efficiency of antitumor medicine. Chinese Chemical Letters, 2024, 35(10): 109420-. doi: 10.1016/j.cclet.2023.109420
10. [10]
  Yujie Li , Ya-Nan Wang , Yin-Gen Luo , Hongcai Yang , Jinrui Ren , Xiao Li . Advances in synthetic biology-based drug delivery systems for disease treatment. Chinese Chemical Letters, 2024, 35(11): 109576-. doi: 10.1016/j.cclet.2024.109576
11. [11]
  Weiyu Chen , Zenghui Li , Chenguang Zhao , Lisha Zha , Junfeng Shi , Dan Yuan . Enzyme-modulate conformational changes in amphiphile peptide for selectively cell delivery. Chinese Chemical Letters, 2024, 35(12): 109628-. doi: 10.1016/j.cclet.2024.109628
12. [12]
  Zhenchun Yang , Bixiao Guo , Zhenyu Hu , Kun Wang , Jiahao Cui , Lina Li , Chun Hu , Yubao Zhao . Molecular engineering towards dual surface local polarization sites on poly(heptazine imide) framework for boosting H₂O₂ photo-production. Chinese Chemical Letters, 2024, 35(8): 109251-. doi: 10.1016/j.cclet.2023.109251
13. [13]
  Guangchang Yang , Shenglong Yang , Jinlian Yu , Yishun Xie , Chunlei Tan , Feiyan Lai , Qianqian Jin , Hongqiang Wang , Xiaohui Zhang . Regulating local chemical environment in O3-type layered sodium oxides by dual-site Mg²⁺/B³⁺ substitution achieves durable and high-rate cathode. Chinese Chemical Letters, 2024, 35(9): 109722-. doi: 10.1016/j.cclet.2024.109722
14. [14]
  Wen Xiao , Fazhan Wang , Yangzhuo Gu , Xi He , Na Fan , Qian Zheng , Shugang Qin , Zhongshan He , Yuquan Wei , Xiangrong Song . PEG400-mediated nanocarriers improve the delivery and therapeutic efficiency of mRNA tumor vaccines. Chinese Chemical Letters, 2024, 35(5): 108755-. doi: 10.1016/j.cclet.2023.108755
15. [15]
  Ningyue Xu , Jun Wang , Lei Liu , Changyang Gong . Injectable hydrogel-based drug delivery systems for enhancing the efficacy of radiation therapy: A review of recent advances. Chinese Chemical Letters, 2024, 35(8): 109225-. doi: 10.1016/j.cclet.2023.109225
16. [16]
  Qiang Li , Jiangbo Fan , Hongkai Mu , Lin Chen , Yongzhen Yang , Shiping Yu . Nucleus-targeting orange-emissive carbon dots delivery adriamycin for enhanced anti-liver cancer therapy. Chinese Chemical Letters, 2024, 35(6): 108947-. doi: 10.1016/j.cclet.2023.108947
17. [17]
  Zhilong Xie , Guohui Zhang , Ya Meng , Yefei Tong , Jian Deng , Honghui Li , Qingqing Ma , Shisong Han , Wenjun Ni . A natural nano-platform: Advances in drug delivery system with recombinant high-density lipoprotein. Chinese Chemical Letters, 2024, 35(11): 109584-. doi: 10.1016/j.cclet.2024.109584
18. [18]
  Liqing Chen , Zheming Zhang , Yanhong Liu , Chenfei Liu , Congcong Xiao , Liming Gong , Mingji Jin , Zhonggao Gao , Wei Huang . Systemically intravenous siRNA delivery into brain with a targeting and efficient polypeptide carrier and its evaluation on anti-glioma efficacy. Chinese Chemical Letters, 2025, 36(3): 110228-. doi: 10.1016/j.cclet.2024.110228
19. [19]
  Junfei Yang , Ke Wang , Shuxin Sun , Tianqi Pei , Junxiu Li , Xunwei Gong , Cuixia Zheng , Yun Zhang , Qingling Song , Lei Wang . A "spore-like" oral nanodrug delivery platform for precision targeted therapy of inflammatory bowel disease. Chinese Chemical Letters, 2025, 36(3): 110180-. doi: 10.1016/j.cclet.2024.110180
20. [20]
  Jiaqi Huang , Renjiang Kong , Yanmei Li , Ni Yan , Yeyang Wu , Ziwen Qiu , Zhenming Lu , Xiaona Rao , Shiying Li , Hong Cheng . Feedback enhanced tumor targeting delivery of albumin-based nanomedicine to amplify photodynamic therapy by regulating AMPK signaling and inhibiting GSTs. Chinese Chemical Letters, 2024, 35(8): 109254-. doi: 10.1016/j.cclet.2023.109254

Get Citation

PDF

XML

Metrics

PDF Downloads(1)
Abstract views(257)
HTML views(6)

通讯作者: 陈斌, bchen63@163.com

1.
沈阳化工大学材料科学与工程学院沈阳 110142