期刊
PHARMACEUTICS
卷 13, 期 9, 页码 -出版社
MDPI
DOI: 10.3390/pharmaceutics13091468
关键词
hemorrhoids; local anesthetic ointment; lidocaine; glycerol monostearate; self-nanoemulsification
资金
- National Research Foundation of Korea Grant - Korean government [NRF-2021R1A2C4002746, 2017R1A5A2015541]
- DONG-A Pharm. Co., Ltd. (Yongin, Korea)
- National Research Foundation of Korea [2017R1A5A2015541] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
The study improved the formulation of lidocaine ointments through nanoemulsion technology, resulting in deeper skin penetration of lidocaine and enhanced local anesthetic effects.
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.
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