Sandimmune Neoral® Novartis

The new cyclosporine formulation (Sandimmun Neoral, Novartis Pharmaceuticals Corporation, East Hanover, NJ) is a self-microemulsifying drug delivery system, which consists of the drug in a lipophilic solvent (corn oil), hydrophilic cosolvent (propylene glycol) surfactant and an antioxidant [37]. Upon contact with GI fluids, Sandimmun Neoral readily forms a homogenous, monophasic microemulsion, which allows the absorption of the drug molecules. Unlike Sandimmun, the formation of this microemulsion is independent of bile salt activity, and indeed, studies have shown that the absorption of cyclosporine from the new formulation is much less dependent on bile flow [38] and is unaffected by food intake [39],... 

A formulation of ciclosporin (Sandimmun Neoral, Novartis) incorporates the drug in a preconcentrate which forms a microemulsion on dilution in aqueous fluids. This formulation offers an alternative to the oil formulation of ciclosporin (Sandimmun) which in vivo would be emulsified by bile salts and pancreatic enzymes. The residence time of ciclosporin in the gastrointestinal tract is shorter and the rate of absorption is faster with the microemulsion formulation (Fig. 7.19). 

There are a few marketed drug delivery systems containing microemulsions that are related to the lipid systems we describe here. Sandimmune Neoral (Novartis, Switzerland) [17], which delivers the lipophilic peptide cyclosporin A, is based on medium-chain triglycerides obtained from coconut oil, a semisynthetic emulsifier (ricinoleate), and propylene glycol. The absorption of the drug taken orally as a microemulsion increases dramatically compared to that of an aqueous suspension [17]. Another marketed example, in which Cs/Cio triglycerides from coconut oil are used, is a soft gelatin capsule of vitamin D3 [18]. 

Cyclosporine Immunosuppressant Sandimmune , Neoral Novartis Pharmaceuticals... 

Unfortunately, the number of commercial formulations is very limited, primarily because of stability and manufacturing problems encountered during large-scale production. The list includes Sandimmune Neoral (cyclosporine A Novartis AG, Switzerland), which contains a microemulsion preconcentrate and is available as soft gels and solutions. Sandimmune (cyclosporine A Novartis AG, Switzerland), which contains an emulsion preconcentrate, and lipid soluble vitamins. Both formulations of cyclosporine have self-emulsifying properties and spontaneously form an o/w microemulsion (particle size <0.15 pm) and an o/w emulsion, respectively in the aqueous fluids of the GI tract. Although the discussion concerning potential of liposomes, niosomes, microemulsions, and solid dispersions for oral delivery is outside the scope of this chapter, the interested reader is referred to recently published reviews on these topics. " ... 

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