Abstract
The bornyl ester derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) including naproxen, ketoprofen and flufenamic acid, were synthesized and their transdermal permeation efficiency and pharmacological activity were determined. The bornyl NSAID esters exhibited more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological evaluations suggested that the bornyl NSAID esters retain most of their inhibition activity toward cyclooxygenase (COX) enzymes and show significant analgesic effect against acetic acid-induced writhing in mice.
Keywords: Anti-nociceptive, borneol, cyclooxygenase, esters, non-steroidal anti-inflammatory drugs, transdermal permeation.
Letters in Drug Design & Discovery
Title:Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters
Volume: 12 Issue: 1
Author(s): Jiufeng Lin, Kefeng Ni, Yang Zhang, Dongzhi Wei and Yuhong Ren
Affiliation:
Keywords: Anti-nociceptive, borneol, cyclooxygenase, esters, non-steroidal anti-inflammatory drugs, transdermal permeation.
Abstract: The bornyl ester derivatives of non-steroidal anti-inflammatory drugs (NSAIDs) including naproxen, ketoprofen and flufenamic acid, were synthesized and their transdermal permeation efficiency and pharmacological activity were determined. The bornyl NSAID esters exhibited more than 10-fold increase of permeation efficiency across mice skin than parent NSAIDs. The preliminary biological and pharmacological evaluations suggested that the bornyl NSAID esters retain most of their inhibition activity toward cyclooxygenase (COX) enzymes and show significant analgesic effect against acetic acid-induced writhing in mice.
Export Options
About this article
Cite this article as:
Lin Jiufeng, Ni Kefeng, Zhang Yang, Wei Dongzhi and Ren Yuhong, Synthesis and Evaluation of Transdermal Permeation, Pharmacological Activity of Bornyl NSAID Esters, Letters in Drug Design & Discovery 2015; 12 (1) . https://dx.doi.org/10.2174/1570180811666140627004820
DOI https://dx.doi.org/10.2174/1570180811666140627004820 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Deciphering the Significance of Plasma Chemokines as Prognostic
Biomarkers in Pegylated IFN-Α-2a /Ribavirin-Treated Chronic Hepatitis
C Genotype 4 Patients
Infectious Disorders - Drug Targets Immunomodulatory Therapies for Renal Cell Carcinoma
Protein & Peptide Letters The Mechanisms Involved in Obesity-Induced Male Infertility
Current Diabetes Reviews Cardiovascular Involvement in Pediatric Systemic Autoimmune Diseases: The Emerging Role of Noninvasive Cardiovascular Imaging
Inflammation & Allergy - Drug Targets (Discontinued) Xenobiotic Acyl Glucuronides and Acyl CoA Thioesters as Protein- Reactive Metabolites With the Potential to Cause Idiosyncratic Drug Reactions
Current Drug Metabolism Ca<sup>2+</sup>/Calmodulin-Dependent Protein Kinase- II in Vasoactive Peptide- Induced Responses and Vascular Biology
Current Vascular Pharmacology The Role of Anionic Polysaccharides in the Preparation of Nanomedicines with Anticancer Applications
Current Pharmaceutical Design Regulation of Innate Immune Responses in the Central Nervous System
CNS & Neurological Disorders - Drug Targets Soluble Epoxide Hydrolase, a Target with Multiple Opportunities for Cardiovascular Drug Discovery
Current Topics in Medicinal Chemistry Editorial [Hot topic: Drug Targeting of Autoimmunity (Guest Editor: Manfred Kunz)]
Current Drug Discovery Technologies Humanized Cobra Venom Factor: Experimental Therapeutics for Targeted Complement Activation and Complement Depletion
Current Pharmaceutical Design Protein Geranylgeranyltransferase Type 1 as a Target in Cancer
Current Cancer Drug Targets Insights into the Microbial L-Asparaginases: from Production to Practical Applications
Current Protein & Peptide Science Hangover Research Needs: Proceedings of the 5th Alcohol Hangover Research Group Meeting
Current Drug Abuse Reviews Alcohol Abuse, Immunosuppression, and Pulmonary Infection
Current Drug Abuse Reviews A Review of Pediatric Mediastinal Masses and Castlemans Disease
Current Pediatric Reviews Rodent Models of Persistent Pain in Drug Discovery and Development
Current Pharmaceutical Biotechnology Vitamin D Supplementation for Obesity: Potential Mechanisms of Action and an Update of Randomized Controlled Trials
Current Nutrition & Food Science Lipid-Based Systems for Delivery of Biological Macromolecules
Recent Patents on Nanomedicine Severe Influenza: Clinical Features and Treatment Options
Current Respiratory Medicine Reviews