Mechanochemical preparation and pharmacological activities of water-soluble intermolecular complexes of arabinogalactan with medicinal agents

Abstract

A possibility of mechanochemical preparation of water soluble complexes of a plant polysac charide arabinogalactan and poorly soluble medicinal agents (Sibazon(=Diazepam), Meza pam(=Medazepam), Indometacin, and Azaleptin(=Clozapine)) has been investigated. Their molec ular dynamics (NMR relaxation method in solution) and some pharmacological properties have been studied in comparison with the original pharmaceutical drugs.

New composites of betulin esters with arabinogalactan as highly potent anti-cancer agents

“…Upon dissolution of the ballmilled mixtures in water, the concentration of BDA increased up to 8 times (Shakhtshneider et al 2013) Ball-milling AG resulted in decreasing the molecular weight of the polymer as was observed also for AG treated in other mills (Dushkin et al 2008). The same effect was observed for the ball-milled mixtures of BDA with AG (Figure 4).…”

“…In the SEM photographs, the pure drugs, BDA This may be the distribution of molecules (or molecular ensembles) of betulin ester in the polymer as supposed for some other low molecular weight drug substances (Dushkin et al 2008). The stability of this composite at heating (Drebushchak et al 2014) is possibly due to complexation of the components under ball-milling.…”

“…Preparation of intermolecular AG complexes with poorly water-soluble drugs enabled their pharmacological properties to be improved (Dushkin et al 2008;Tolstikova et al 2009;Khvostov et al 2013). In a previous work (Shakhtshneider et al 2013), we obtained the composites of AG with BDA by ball-milling.…”

Polysaccharides from Larch Biomass

“…Essentially (up to 50 times) increased solubility of MS and dramatically decreased therapeutic doses of the same efficiency are reported for clathrates of poorly soluble anti-inflammatory, psychotropic and hypotensive drugs [51,52]; for instance, clathrates of AG with nifedipine containing a 10 times lower dose than the starting MS show pronounced hypotensive and antiarrhythmic effects [52]. Additionally, the side effects of MS in clathrates are decreased, for instance in the ulcerogenity of nonsteroidal anti-inflammatory drugs.…”

“…Combined mechanochemical activation of MS with AG (pharmacon clathration) is even more effective in improving safety and bioavailability of drugs [50][51][52][53]. Essentially (up to 50 times) increased solubility of MS and dramatically decreased therapeutic doses of the same efficiency are reported for clathrates of poorly soluble anti-inflammatory, psychotropic and hypotensive drugs [51,52]; for instance, clathrates of AG with nifedipine containing a 10 times lower dose than the starting MS show pronounced hypotensive and antiarrhythmic effects [52].…”