Drug Delivery Systems for Cyclosporine: Achievements and Complications

Abstract

The review deals with the preparation, properties, and analysis of different kinds of cyclosporine delivery systems, such as solid formulations, liposomes, emulsions and microemulsions and targeted cyclosporine formulations. The review points out a key role of delivery systems in increasing the therapeutic effectiveness of cyclosporine. Comparative studies of the prior marketed formulation, Sandimmune, with a new microemulsion formulation, Neoral, are discussed including some data on clinical development of Neoral.

Preparation and evaluation of cyclosporin A-containing proliposomes: a comparison of the supercritical antisolvent process with the conventional film method

“…1,6 Other marketed drugs of CsA include Sandimmune ® (Novartis International AG, Basel, Switzerland), an oil-based formulation, 7,8 and Neoral ® (Novartis International AG, Basel, Switzerland), a microemulsion-based preconcentrate formulation and both have issues because of their oil and alcohol contents. 2,7,9 Both of these formulations have high intra-and interpatient variability. 10 Considerable efforts have been made to improve the availability and the tolerance of topically applied CsA, but so far, none of the delivery systems have been fully satisfactory.…”

Characterization and stability studies of a novel liposomal cyclosporin A prepared using the supercritical fluid method: comparison with the modified conventional Bangham method

“…1 CsA is a powerful immunosuppressive drug which is used to prevent rejection of transplanted organs, and it is also used for the treatment of several autoimmune and some parasitic diseases. 2,3 CsA is currently the second most commonly used agent in the treatment of immune-mediated ocular surface diseases, following corticosteroids, the side effects of which are well known. 4 Presently there are various dosage forms -eg, capsules (oral), injectables (injection), solution (oral), and emulsion (ophthalmic) -of CsA reported in the market.…”

Cyclosporin Nanoparticulate Lipospheres for Oral Administration

“…3 Various formulations for oral delivery of CyA were prepared. 3,4 Microformulations, [5][6][7][8] complexation with cyclodextrin, 9 and microspheres, [10][11][12] increase the miscibility and oral bioavailability of CyA. A comprehensive review on delivery systems for CyA was published by Klyashchitsky and Owen.…”