Method Article

Analgesic and Anti-inflammatory Effects of Xueshan Jinluohan Coating Agent and Its Transdermal Mechanism

DOI:

10.3791/70480

⸱

April 30th, 2026

 ,  ,  ,  ,  ,  ,  ,  , 
1Qingdao Academy of Chinese Medicinal Sciences, Shandong University of Traditional Chinese Medicine, 2State Key Laboratory of Southwestern Chinese Medicine Resources, School of Ethnic Medicine, Chengdu University of Traditional Chinese Medicine, 3Tibet Rhodiola Pharmaceutical Holding Co. Ltd, 4State Key Laboratory of Southwestern Chinese Medicine Resources, School of pharmacy, Chengdu University of Traditional Chinese Medicine, 5Laboratory of Epigenetics and Immunology, West China Institute of Women and Children's Health, NHC Key Laboratory of Chronobiology, Department of Obstetric and Pediatric, Key Laboratory of Birth Defects and Related Diseases of Women and Children of MOE, State Key Laboratory of Biotherapy, West China Second University Hospital, Sichuan University

In This Article

Summary

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This study presents an integrated approach to evaluate the analgesic and anti-inflammatory effects of Xueshan Jinluohan Pain-Relieving Coating Agent. The effects were area- and time-dependent, and transdermal analysis identified benzoylaconine as the primary permeating component with diffusion-controlled release.

Abstract

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Topical traditional Chinese medicine (TCM) preparations are widely used for the management of inflammatory and pain-related conditions because they provide local therapeutic effects while potentially reducing systemic adverse reactions. However, the pharmacodynamic characteristics and transdermal mechanisms underlying many clinically applied formulations remain insufficiently characterized. Xueshan Jinluohan Pain-Relieving Coating Agent (XJCA), a Tibetan medicine formulation, is commonly prescribed for inflammatory pain, yet the influence of application area, duration of action, and the relative contributions of local versus systemic effects have not been systematically evaluated. This study establishes an integrated in vivo–in vitro methodological framework to investigate these parameters. Multiple complementary animal models were employed to assess central and peripheral analgesic activity and acute inflammatory responses, enabling evaluation of area-, time-, and local-versus-systemic-dependent effects. In parallel, a Franz diffusion cell system coupled with ultra-high-performance liquid chromatography–tandem mass spectrometry (UPLC-MS/MS) was used to characterize the percutaneous absorption kinetics of two principal alkaloids, benzoylaconine and aconitine. XJCA demonstrated significant area- and time-dependent analgesic and anti-inflammatory effects, and larger application areas were associated with greater systemic contribution to analgesic efficacy. Transdermal kinetic analysis revealed that benzoylaconine exhibited a substantially higher steady-state flux and followed diffusion-controlled release consistent with the Higuchi model, whereas aconitine showed lower permeability and a more complex release profile. These findings link transdermal delivery behavior with observed pharmacodynamic outcomes and provide a structured framework for evaluating and optimizing topical TCM formulations.

Introduction

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Inflammation and pain are interrelated physiological and pathological responses that play a key role in the body’s defense against injury and infection1. However, persistent or excessive inflammation and pain, such as osteoarthritis, rheumatoid arthritis, or post-traumatic pain, can lead to tissue damage that can seriously impair the physical functioning and mental health of patients2,3. Currently, clinical treatments for inflammation and pain mainly rely on non-steroidal anti-inflammatory drugs (NSAIDs) (e.g., diclofenac, ibuprofen) and opioids. While NSAIDs are widely used for t....

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Protocol

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This study was conducted in accordance with the Guidelines for Ethical Review of Welfare of Laboratory Animals (GB/T 35892-2018) and the Guiding Opinions on the Humane Treatment of Laboratory Animals. All animal procedures were approved by the Experimental Animal Ethics Committee of Chengdu University of Traditional Chinese Medicine (Approval No. TCM-09-315).

Experimental animals and housing
Specific pathogen-free (SPF) Kunming mice (20~25 g, male/female = 1:1) and SPF Sprague-Dawley (SD) rats (180~200 g) were used. Animals were housed under controlled conditions: a 12 h light/dark cycle, a temperature of 23 ± 2 ....

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Results

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Dependence of analgesic and anti-inflammatory efficacy on application area
XJCA exhibited a positive correlation between application area and analgesic/anti-inflammatory efficacy in mouse models, following 7 consecutive days of administration at a fixed dose of 0.03 g/cm2. In the hot plate test, the NC group exhibited the shortest mean PWL, indicating the strongest pain response. In contrast, XJCA-treated groups showed an area-dependent prolongation of PWL: XJCASAAG, XJCAMAAG, and XJCALAAG.......

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Discussion

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Inflammation and pain are complex pathological processes involving multiple signaling pathways. Topical preparations have been increasingly favored because they can accurately act on lesions and minimize systemic adverse reactions21,22. This study successfully established and validated a systematic methodological framework for evaluating topical TCM formulations, using XJCA as a demonstration case. The integrated approach, combining strategically designed in vivo.......

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Disclosures

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The authors have no conflicts of interest to declare.

Acknowledgements

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This study was supported by the Taishan Scholars Program of Shandong Province (tsqn20250730), the University (Sichuan University)-Enterprise (Tibet Rhodiola Pharmaceutical Holding Co., Ltd.) Cooperation Project (24H0764, 24H1043) and the Bian Que Scholar Programme of Shandong University of Traditional Chinese Medicine.

....

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Materials

List of materials used in this article
NameCompanyCatalog NumberComments
0.22 μm microporous membrane filtersMilliporeSigma, Burlington, MA, USAGSWP04700
Acetic acidCNW Technologies GmbHN3800060Chromatography grade
AcetonitrileMerck KGaAI1241129242Mass spectrometry grade
AconitineChengdu Lemeitian Pharmaceutical Technology Co., Ltd.DSTDW00060220 mg, ≥98% purity
Agilent ZORBAX SB-C18 columnAgilent2.1 × 100 mm, 1.8 μm
Ammonium acetateGENERAL-REAGENTP1492146Analytical grade
BenzoylaconineChengdu Lemeitian Pharmaceutical Technology Co., Ltd.DSTDB00550220 mg, ≥98% purity
DichloromethaneCINC Chemical Co., Ltd.P3048495Analytical grade
Diclofenac Diethylamine Emulgel (DDE)Novartis Pharma Beijing Co., Ltd.H20020176
Formalin solutionSinopharm Chemical Reagent Co., Ltd.10010061
Franz diffusion cellsShenzhen Ruituo Analytical Instruments Co., Ltd.RT806
GraphPad Prism 9.0 softwareGraphPad Software, Inc.Version 9.0
IsopropanolGENERAL-REAGENT0530240601DChromatography grade
Normal salineSinopharm Chemical Reagent Co., Ltd.SY15931
Pentobarbital sodiumSigma-Aldrich, St. Louis, MO, USAP3761
Purified waterGuangzhou Watson's Food and Beverage Co., Ltd.Batch No. 20240717C
SPF Kunming miceChengdu Enswell Biotechnology Co., Ltd.License: SYXK (Sichuan) 2019-049
SPF Sprague-Dawley ratsBeijing Speifu Biotechnology Co., Ltd.License: SYXK (Beijing) 2024-0010
UPLC-MS/MS systemAgilent Technologies, Santa Clara, CA, USAAgilent 1260 Infinity
Xueshan Jinluohan Pain-Relieving Coating Agent (XJCA)Tibet Pharmaceutical Co., Ltd.Z20010095
XyleneSinopharm Chemical Reagent Co., Ltd.10023418

References

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  1. Kang, S. Y., Ryu, Y. Editorial: Chronic inflammation and related diseases: From mechanisms to therapies. Int J Mol Sci. 24 (13), (2023).
  2. Liu, Y., et al. The analgesic effects of Yu-Xue-Bi tablet (YXB) on m....

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Tags

Analgesic EffectsAnti Inflammatory EffectsTransdermal MechanismXueshan JinluohanTopical TCMPercutaneous AbsorptionFranz Diffusion CellUPLC MS MSBenzoylaconineAconitine

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