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Design and Development of Lidocaine Microemulsions for Transdermal Delivery

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Abstract

Topical administration is a preferable choice for local anesthetic delivery. Microemulsions have shown great effectiveness for transdermal transport of lidocaine. However, fabrication of microemulsions containing highly concentrated lidocaine (10%) to provide an extended local anesthetic effect is still a challenge. This study investigated the feasibility of using microemulsions for transdermal delivery of a high dosage of lidocaine (10%). At first, eutectic mixtures by kneading lidocaine with thymol were tailored to form a lipophilic solution, then the mixtures were readily incorporated into the oil phase of microemulsions after addition of proper surfactants and cosurfactants. The physicochemical properties, the skin permeation, local anesthetic efficacy, and the irritation experiment of the developed microemulsions were evaluated. The optimum composition was as follows: 12% of ethyl oleate as oil phase, 28% of the mixed surfactant, and cosurfactant (polyoxyl 15 hydroxystearate and ethanol) and 60% of the aqueous phase. The average particle size was about 13 nm. The transmission electron microscope (TEM) studies revealed almost homogeneous spherical globules without aggregation. The Fourier-transform infrared spectroscopy (FTIR) results highlighted the drugs homogeneously dispersed in the microemulsions. In vitro skin permeation and in vivo anesthesia effect evaluation indicated that microemulsions can enhance and extend the anesthetic effect of lidocaine. The irritable results indicated that the microemulsions had the better biocompatibility and the negligible influence on the dermal. Therefore, incorporating the eutectic mixtures into microemulsions could be proposed as an attractive choice and a promising transdermal delivery strategy for the future topical anesthetic therapy.

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Acknowledgements

This work was supported by National Nature Science Foundation of China (No.81102820), and Natural Science Foundation of Shandong Province (No.ZR2016HM21), Scientific development program of Traditional Chinese Medicine of Shandong Province (2017-240; 2017-243), the Open Project of Shandong Collaborative Innovation Center for Antibody Drugs (No. CIC-AD1813), and Project of China Medical Education Association (No. 2016SKT-M030).

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  1. Yaping Wang and Xihui Wang contributed equally to this work.

Authors and Affiliations

  1. College of Pharmacy, Taishan Medical University, Taian, 271016, People’s Republic of China

    Yaping Wang, Xihui Wang, Xiangyu Wang, Yilei Song, Xiaodan Wang & Jifu Hao

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  1. Yaping Wang
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  2. Xihui Wang
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  3. Xiangyu Wang
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  5. Xiaodan Wang
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Correspondence to Xiaodan Wang or Jifu Hao.

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Wang, Y., Wang, X., Wang, X. et al. Design and Development of Lidocaine Microemulsions for Transdermal Delivery. AAPS PharmSciTech 20, 63 (2019). https://doi.org/10.1208/s12249-018-1263-1

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