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.