Phytoconstituents as pharmacotherapeutics in rheumatoid arthritis: challenges and scope of nano/submicromedicine in its effective delivery

J Pharm Pharmacol. 2017 Jan;69(1):1-14. doi: 10.1111/jphp.12661. Epub 2016 Oct 24.

Abstract

Objectives: The present review explores the therapeutic application of herbals in rheumatoid arthritis (RA) therapy, and how nano/submicromedicine can be fit in the scope of its therapeutic delivery in RA has been addressed.

Key findings: Incorporation of bioactive such as polyphenols, thymoquinone, resveratrol, hesperidin, curcumin, celastrol and gambogic acid in a dose-dependent manner showed quite high efficacy for the treatment of RA. It can be attributed to their targeting ability against various inflammatory mediators including nitric oxide (NO), cytokines, chemokines, adhesion molecules, NF-kβ, lipoxygenase (LOXs) and arachidonic acid (AA). Despite the presence of significant merits, the use of these bioactives has several demerits such as poor bioavailability as a function of low aqueous solubility and higher first-pass metabolism upon oral administration. The impact of nano/submicromedicine in the delivery of these bioactives against RA has gained wider attention owing to bioavailability enhancement, higher stability and better efficacy.

Conclusion: Phytoconstituents possess immense potential in RA pharmacotherapy, but the obstacles for their effective delivery can be overcome using nano/submicrocarrier-based drug delivery technologies, which maximize the efficacy of these herbal antirheumatic drugs without any systemic adverse effects.

Keywords: liposomes; nan/submicro-medicine; nanoemulsion; phytoconstituents; rheumatoid arthritis.

Publication types

  • Review

MeSH terms

  • Antirheumatic Agents / administration & dosage
  • Antirheumatic Agents / pharmacokinetics
  • Antirheumatic Agents / pharmacology
  • Antirheumatic Agents / therapeutic use*
  • Arthritis, Rheumatoid / drug therapy*
  • Biological Availability
  • Drug Delivery Systems*
  • Humans
  • Magnoliopsida / chemistry*
  • Nanoparticles
  • Phytochemicals / administration & dosage
  • Phytochemicals / pharmacokinetics
  • Phytochemicals / pharmacology
  • Phytochemicals / therapeutic use*
  • Phytotherapy*
  • Plant Extracts / administration & dosage
  • Plant Extracts / pharmacokinetics
  • Plant Extracts / pharmacology
  • Plant Extracts / therapeutic use*

Substances

  • Antirheumatic Agents
  • Phytochemicals
  • Plant Extracts