Abstract
During the long period of cyclosporine-containing dosage forms development a lot of significant findings have been done especially in the field of drug delivery systems. Currently available drugs are based, from technological point of view, on self-dispersible drug delivery systems, which contain cyclosporine solved in pharmaceutically acceptable vehicle. One can find difference among particular systems a) at particle size distribution after dispergation, b) at composition and c) at bioavailability of cyclosporine. As far as improvement of bioavailability between original brand leader formulation Sandimmune and recent brand leader formulation Neoral was followed by significant improvement in particle size distribution it was generally assumed that the reason for this improvement have been found. Several other formulations e.g. Consupren or SangCyA--self-dispersible systems, more or less correspond with above mentioned theory that smaller is better and by this principle bridged liquid based dosage forms with solid dosage forms. Bioavailability of novel drug delivery system which gives coarse dispersion with average particle size between 1-150 microns when dispersed have been tested on healthy volunteers. No difference among pharmacokinetic parameters of novel drug delivery system and microemulsion system have been observed in spite of fact that average particle size of novel system is almost 1000x bigger.
Highlights
Cyclosporine containing dosage forms were introduced for use in transplantations two decades ago, and are the basis of most immunosuppressive protocols after solid organ transplantation[1]
As far as improvement of bioavailability between original brand leader formulation Sandimmune® and recent brand leader formulation Neoral® was followed by significant improvement in particle size distribution it was generally assumed that the reason for this improvement have been found
Bioavailability of novel drug delivery system which gives coarse dispersion with average particle size between 1–150 μm when dispersed have been tested on healthy volunteers
Summary
Cyclosporine containing dosage forms were introduced for use in transplantations two decades ago, and are the basis of most immunosuppressive protocols after solid organ transplantation[1]. The first registered dosage form with cyclosporine (Sandimmune®, Novartis, Switzerland) was designed as an emulsion pre-concentrate, which mean that dispersed droplets were above 1 μm. Current brand leader formulation (Neoral®, Novartis, Switzerland) is in form of microemulsion pre-concentrat (e.g. dispersed particles were < 100 nm) and was launched on the market more than 10 years after the first one. Significant improvement of treatment efficacy[2] and bioavailability[3] with Neoral® was reported. This improvement was connected with microemulsion character of administered drug.[4, 5, 6, 7] the concept known from powder material that “smaller is better” was adopted for liquid based dispersion systems
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