Inclusion Complexes for controlled release 

The research has been focused particularly on structure and properties of inclusion complexes of biologically active molecules. 

(a) CD/pheromone systems have been developed for the controlled release and protection of two pheromones of the olive pests Bactrocera oleae and Prays oleae (Figs.1 and 2) and have been tested successfully in the field by entomological groups in the Institute of Biology, NCSR "Demokritos” (Dr. V. Mazomenos).

 

Fig.1 Dominant structures of Bactrocera Oleae pheromone/cyclodextrins in aqueous solution by NMR (J. Org. Chem. 1995, 60, 4017; Carbohydr. Res. 1996,283, 1)

Fig. 2 X-ray structure of Prays oleae pheromone in βCD (left). There are pheromone molecules inside the βCD cavity but also outside in the crystal lattice  (J. Chem Soc Perkin II, 2002, 1639; European Patent No 92 401 709.8, 1992; US Patent NoΒ US00650160A, 1997). The Prays oleae pheromone is spontaneously released (right) from the solid complex up to 50% of its content.

b)βCD/Acemetacin

There is extensive self-association of the NSAID drug Acemetacin in aqueous solution and strong βCD binding. Inclusion complexation does not influence the rate of hydrolysis of the drug into its active metabolite, indomethacin, as found by NMR and HPLC studies(in collaboration with assoc. prof. A.Antoniadou-Vyza (Pharmacy Dept., Univ. Of Athens).

Fig. 3 Multiple equilibria in in βCD/acemetacin solution(Carbohydr. Res., 2002, 337, 1387).