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Article

Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery

1
College of Pharmacy, Chungbuk National University, Cheongju 28160, Korea
2
DONG-A Pharm. Co., Ltd., Yongin 17073, Korea
3
Department of Pharmaceutical Engineering, Cheongju University, Cheongju 28503, Korea
*
Authors to whom correspondence should be addressed.
Academic Editors: Eneida de Paula and Lígia N. M. Ribeiro
Pharmaceutics 2021, 13(9), 1468; https://doi.org/10.3390/pharmaceutics13091468
Received: 14 August 2021 / Revised: 8 September 2021 / Accepted: 10 September 2021 / Published: 14 September 2021
(This article belongs to the Special Issue Nanolipid-Based Pharmaceutical Dosages Releasing Local Anesthetics)
Lidocaine, a commonly used local anesthetic, has recently been developed into a number of ointment products to treat hemorrhoids. This study examined its efficient delivery to the dermis through the pharmaceutical improvement of hemorrhoid treatment ointments. We attempted to increase the amount of skin deposition of lidocaine by forming a nanoemulsion through the self-nanoemulsifying effect that occurs when glycerol monostearate (GMS) is saturated with water. Using Raman mapping, the depth of penetration of lidocaine was visualized and confirmed, and the local anesthetic effect was evaluated via an in vivo tail-flick test. Evaluation of the physicochemical properties confirmed that lidocaine was amorphous and evenly dispersed in the ointment. The in vitro dissolution test confirmed that the nanoemulsifying effect of GMS accelerated the release of the drug from the ointment. At a specific concentration of GMS, lidocaine penetrated deeper into the dermis; the in vitro permeation test showed similar results. When compared with reference product A in the tail-flick test, the L5 and L6 compounds containing GMS had a significantly higher anesthetic effect. Altogether, the self-nanoemulsifying effect of GMS accelerated the release of lidocaine from the ointment. The compound with 5% GMS, the lowest concentration that saturated the dermis, was deemed most appropriate. View Full-Text
Keywords: hemorrhoids; local anesthetic ointment; lidocaine; glycerol monostearate; self-nanoemulsification hemorrhoids; local anesthetic ointment; lidocaine; glycerol monostearate; self-nanoemulsification
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MDPI and ACS Style

Kang, J.-H.; Yoo, K.-H.; Park, H.-Y.; Hyun, S.-M.; Han, S.-D.; Kim, D.-W.; Park, C.-W. Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery. Pharmaceutics 2021, 13, 1468. https://doi.org/10.3390/pharmaceutics13091468

AMA Style

Kang J-H, Yoo K-H, Park H-Y, Hyun S-M, Han S-D, Kim D-W, Park C-W. Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery. Pharmaceutics. 2021; 13(9):1468. https://doi.org/10.3390/pharmaceutics13091468

Chicago/Turabian Style

Kang, Ji-Hyun, Kwang-Hwi Yoo, Hyo-Young Park, Seung-Min Hyun, Sang-Duk Han, Dong-Wook Kim, and Chun-Woong Park. 2021. "Preparation and In Vivo Evaluation of a Lidocaine Self-Nanoemulsifying Ointment with Glycerol Monostearate for Local Delivery" Pharmaceutics 13, no. 9: 1468. https://doi.org/10.3390/pharmaceutics13091468

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