Cyclosporine CsA—The Physicochemical Characterization of Liposomal and Colloidal Systems

This paper presents an overview of the possibilities of testing various cyclosporine (CsA) formulations with an emphasis on parameters that may be key to improving the stability and biocompatibility. The feasibility of CsA colloidal systems for oral (injection) administration were investigated using different techniques and compared with similar investigations of other researchers. The chosen CsA systems were developed using dipalmitoylphosphocholine (DPPC) and/or cholesterol as a lipid matrix, stabilized with ethanol, with soybean oil or n-tetradecane as oil phase in emulsions, under natural pH, room and physiological temperature. Their integrity was found to be strictly dependent on the stabilizers. The highest CsA penetrability with the system containing phospholipid in the context of its interactions with lipid membranes was shown. Also, the bioavailability of CsA can be enhanced with the biopolymer antibacterial chitosan. This mini-review suggests the suitability of liposome/microemulsion as promising vehicles for CsA delivery. The most hopeful proved to be formulation with the smaller particle size facilitating absorption, but when safety is assessed, relying on just the particle size cannot be the only criteria. Reassumed, the CsA formulation stability known on the basis of the size and zeta potential measurements guarantees a decrease of the individual variations in the drug bioavailability, toxicity and minimizes rejection.