Drug delivery system for administration of poorly water soluble pharmaceutically active substances

摘要

This invention relates to a drug delivery system for administration of poorly water soluble pharmaceutically active substance, a pharmaceutical composition comprising such a drug delivery system, and a method for the preparation of such a drug delivery system. The invention also relates to a method for controlling the particle size and/or particle shape and/or particle size distribution in such a drug delivery system, and to a method for increasing the drug loading capacity of the particles. Furthermore the invention also relates to the use of such a drug delivery system for the preparation of a medicament for the treatment of cancer.

主权项

1. A drug delivery system for administration of at least one pharmaceutically active substance having a solubility per se in water of less than about 100 μg/ml, said substance being in particulate form with an effective average particle size of less than about 100 nm, wherein
the substance particles are essentially amorphous; the substance particles are entrapped in nanoparticles formed of a sodium salt of the methyl ester of N-all-trans-retinoyl cysteic acid, sodium salt of methyl ester of N-13-cis-retinoyl cysteic acid, or a combination thereof; the weight-to-weight ratio of said sodium salt of methyl ester of N-all-trans-retinoyl cysteic acid, sodium salt of methyl ester of N-13-cis-retinoyl cysteic acid, or a combination thereof, to said substance is in the range from about 0.5:1 to about 20:1; and said substance is an immunosuppressant chosen from among ciclosporin, sirolimus, tacrolimus and derivatives thereof.