Reformulating cyclosporine A (CsA): More than just a life cycle management strategy

J Control Release. 2016 Mar 10:225:269-82. doi: 10.1016/j.jconrel.2016.01.056. Epub 2016 Jan 30.

Abstract

Cyclosporine A (CsA) is a well-known immunosuppressive agent that gained considerable importance in transplant medicine in the late 1970s due to its selective and reversible inhibition of T-lymphocytes. While CsA has been widely used to prevent graft rejection in patients undergoing organ transplant it was also used to treat several systemic and local autoimmune disorders. Currently, the neuro- and cardio-protective effects of CsA (CiCloMulsion®; NeuroSTAT®) are being tested in phase II and III trials respectively and NeuroSTAT® received orphan drug status from US FDA and Europe in 2010. The reformulation strategies focused on developing Cremophor® EL free formulations and address variable bioavailability and toxicity issues of CsA. This review is an attempt to highlight the progress made so far and the room available for further improvements to realize the maximum benefits of CsA.

Keywords: Cyclosporine A; Drug delivery system; Immunosuppressant; Microparticle; Nanoparticle.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Cyclosporine / administration & dosage*
  • Cyclosporine / chemistry
  • Cyclosporine / pharmacology
  • Cyclosporine / therapeutic use
  • Drug Compounding
  • Drug Delivery Systems*
  • Humans
  • Immunosuppressive Agents / administration & dosage*
  • Immunosuppressive Agents / chemistry
  • Immunosuppressive Agents / pharmacology
  • Immunosuppressive Agents / therapeutic use

Substances

  • Immunosuppressive Agents
  • Cyclosporine