Solid lipidic nanospheres suitable to a fast internalization into cells

#The present invention relates to pharmaceutical compositions in form of solid lipidic nanospheres able to fast penetrate into the cells, the process for their preparation and their use in the treatment of tumoral pathologies and of Mediterranean anaemia.

#It is known from literature that the carboxylic acids having a low number of carbon atoms, such as acetic acid, propionic acid, butyric acid and succinic acid, and their derivatives, may inhibit the proliferation of the tumoral cells, in particular in the case of colon cancers (H. P. Scheppach, F. Ritcher, Eur. J. Cancer Prevention, 4, 373-378, 1995, and 31, 1077-1080, 1995).

#There are in particular experimental proofs showing the antiproliferative activity of the butyric acid salts, for example of the sodium salt, towards a great variety of neoplastic cells (S. P. Landon et al., Cancer res., 48, 6161-6165, 1988; D. Coradini et al., Cell Prolif., 30, 149-159, 1997; H. Yamamoto et al., Int. J. Cancer, 76, 897-902, 1998). Recent studies showed that sodium butyrate is able to modulate the expression of the oncogenes and of the genes regulating the apoptosis in cells from different histotypes (O. C. Velasquez et al., J. Parenteral Enteral Nutr., 20, 243-250, 1996; M. Mandal, R. Kumar, Cell Growth Diff., 7, 311-318, 1996).

#a) 15 mg of Epikuron 200® (95% phosphatidylcholine) and 1 mg of phosphatidylinositol are added to 9 mg of cholesteryl butyrate, and such a mixture is heated to melting at about 75° C.;

#b) a mixture consisting of water (62 mg), sodium glycocholate (3 mg) and butyl alcohol (10 mg) is heated at the same temperature of the mixture of the step a);

#c) under mild stirring and at the same. temperature of the preceding steps, the mixture of the step b) is added to the mixture of the step a), obtaining a microemulsion, which turns out to be clear;