Cyclosporine A and New Approaches to Cyclosporine A Formulations

Sıla GÜLBAĞ*°, Nevin ÇELEBİ*

*Gazi Üniversitesi Eczacılık Fakültesi, Farmasötik Teknoloji Anabilim Dalı, 06330, Etiler/ANKARA

°Corresponding Author:
Phone: +90 (312) 202 30 52
E-Mail: silagulbag@gazi.edu.tr

 

Summary

The development of nanoformulations/nanosystems with different active ingredients has become an interesting subject, after the pharmaceutical field has increased as nanotechnology has been the subject of many different areas in recent years. Cyclosporine A (CsA); it is a neutral hydrophobic cyclic peptide containing 11 amino acids. It has been used for the suppression of the immune system after organ transplantation but nowadays it is used for the treatment of many autoimmune diseases also. Low solubility, narrow therapeutic range, effect of p-glycoprotein efflux in enterocytes, significant intra- and inter-individual variability (20-50%) in bioavailability, severe side effects in overdose and severe nephrotoxicity show problems with treatment with CsA. CsA has serious nephrotoxicity but is one of the most commonly used drugs for immunosuppression in autoimmune diseases and especially organ transplantations. In addition to increasing the solubility and thus the bioavailability of CsA, many studies based on current approaches to formulations of CsA have been conducted for purposes such as reducing the side effects seen and showing similar effects with lower doses of active substance and studies for this purpose are still in progress today. In this review, the basic structure of CsA, mechanism of action, its biopharmaceutical properties and drug delivery systems (nanoparticles, solid lipid nanoparticles, lipospheres, micelles, liposomes, microspheres, self emulsifying systems, carbon nanotubes, nanogels) for oral administration, which is one of the most suitable ways of using nanotechnology based formulations are briefly described. Also; nanocrystal formulations of CsA on oral administration have also been evaluated.

Key Words :
Cyclosporine A, solubility, bioavailability, pharmacokinetic, oral administration, nano carrier systems.