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A Novel Brucine Gel Transdermal Delivery System Designed for Anti-Inflammatory and Analgesic Activities.

Abstract
The seeds of Strychnosnux-vomica L., as a traditional Chinese medicine, have good anti-inflammatory and analgesic activities. However, it usually leads to gastrointestinal irritation and systemic toxicity via oral administration. In the study, it was discovered that a novel gel transdermal delivery system contained brucine, the main effective component extracted from Strychnosnux-vomica. Results showed that the brucine gel system inhibited arthritis symptoms and the proliferation of the synoviocytes in the rat adjuvant arthritis model, which indicated its curative effect for rheumatoid arthritis. Meanwhile, it significantly relieved the xylene-induced ear edema in the mouse ear swelling test, which manifested its anti-inflammatory property. Moreover, the brucine gel eased the pain of paw formalin injection in the formalin test, which demonstrated its analgesic effects. In addition, the brucine significantly inhibited lipopolysaccharide (LPS)-induced Prostaglandin E2 (PGE2) production without affecting the viability of cell in vitro anti-inflammatory test, which proved that its anti-inflammatory and analgesic actions were related to inhibition of prostaglandin synthesis. It is suggested that the brucine gel is a promising vehicle for transdermal delivery on the treatment of inflammatory disease.
AuthorsPing Wu, Qin Liang, Pei Feng, Chunyan Li, Chunguang Yang, Hongsuo Liang, Huaibo Tang, Cijun Shuai
JournalInternational journal of molecular sciences (Int J Mol Sci) Vol. 18 Issue 4 (Apr 03 2017) ISSN: 1422-0067 [Electronic] Switzerland
PMID28368343 (Publication Type: Journal Article)
Chemical References
  • Analgesics
  • Anti-Inflammatory Agents
  • Gels
  • Formaldehyde
  • brucine
  • Strychnine
  • Dinoprostone
Topics
  • Administration, Cutaneous
  • Analgesics (administration & dosage, pharmacology)
  • Animals
  • Anti-Inflammatory Agents (administration & dosage, pharmacology)
  • Arthritis, Experimental (pathology)
  • Cell Line
  • Cell Proliferation (drug effects)
  • Cell Survival (drug effects)
  • Cells, Cultured
  • Dinoprostone (biosynthesis)
  • Disease Models, Animal
  • Drug Delivery Systems (methods)
  • Edema (prevention & control)
  • Formaldehyde
  • Gels
  • Humans
  • Macrophages (cytology, drug effects, metabolism)
  • Male
  • Mice
  • Pain (chemically induced, prevention & control)
  • Phytotherapy
  • Rats, Wistar
  • Strychnine (administration & dosage, analogs & derivatives, pharmacology)
  • Strychnos nux-vomica (chemistry)
  • Synoviocytes (drug effects, pathology)

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