Abstract

DESIGN OF A PHARMACEUTICAL FORMULATION: DEVELOPMENT AND CHARACTERIZATION OF GUATTERIOPSISCINE INCLUSION COMPLEX WITH ?-CYCLODEXTRIN

Valéria Lima Silva Veras*, Mônica Regina Silva de Araújo, Felipe Pereira da Silva Santos, Antonio do Nascimento Cavalcante, Emmanoel Vilaça Costa and Chistiane Mendes Feitosa

ABSTRACT

The species Guatteria friesiana (W. A. Rodrigues) Erkens & Maas, known as "envireira", is a plant native to Brazil, found particularly in the Amazon region. This plant has important active ingredients, such as the essential oil constituents of leaves and their alkaloids. In other studies, G. friesiana has been shown to have antimicrobial activity, and no cytotoxic effect. In our search for new inhibitors of the acetylcholinesterase enzyme, some alkaloids isolated from G. friesiana were tested in vitro and one of these alkaloids, guatteriopsiscine, showed a promising anticholinesterase activity superior to the standard drug, rivastigmine. However, guatteriopsiscine has a crystalline profile, which suggests a lower solubility in relation to an amorphous compound. Therefore, the search for an efficient and non-toxic carrier for the guatteriopsiscine has important clinical application, the pharmaceutical excipient cyclodextrin can be mentioned as an example of this carrier. This study aimed to obtain and characterize inclusion complexes of guatteriopsiscine with β-cyclodextrin (β-CD). This preparation was done using the technique of malaxation and this characterization was done through several techniques, namely: infrared spectroscopy, thermogravimetric analysis, X-ray diffraction, scanning electron microscopy, nuclear magnetic resonance of hydrogen and tests of dissolution. These techniques confirmed the formation of inclusion complexes between guatteriopsiscine and β-CD. Therefore, the results obtained are promising for the preparation of a future pharmaceutical formulation with that complex.

Keywords: Guatteriopsiscine, Inclusion complex, Anticholinesterase activity.