Production and Characterization of a β-Cyclodextrin Inclusion Complex with Platonia insignis Seed Extract as a Proposal for a Gastroprotective System

Abstract

Platonia insignis Mart, Clusiaceae, known as bacuri, is a species native to Brazil that, in studies with extract of the seed of its fruit, showed antioxidant activity against free radicals. Products with such properties may be of great importance in the treatment of peptic ulcers since this pathology may be associated with the inflammatory process caused by the action of free radicals. Cyclodextrins are molecules capable of forming inclusion complexes with other molecules, affecting their physicochemical properties and improving their pharmacokinetic characteristics. Thus, this work aimed to produce, characterize, and evaluate the gastroprotective effect of the inclusion complex of β-cyclodextrin (β-CD) with the bacuri seeds hexanic extract (BSHE). In the characterization of the inclusion complex, an apparent stability constant (Kc) of 416 mol/L was obtained in the solubility study; the BSHE:β-CD m/m (g) complexation ratios at 1:9, 2:8, and 3:7 were 5.51%, 21.46%, and 20.11%, respectively. The formation of the BSHE:β-CD inclusion complex was observed by FTIR technique, indicating the disappearance of bands characteristic of BSHE (2960 cm−1 and 1755 cm−1) when in the complex, compared to the spectra of pure BSHE or in physical mixture with β-CD, and by X-ray diffraction, which indicated a loss of crystallinity, typical signals of pure β-CD, and presentation of intense amorphization, characteristic of BSHE, incorporated in the β-CD pockets. In the evaluation of gastroprotective activity, through absolute ethanol-induced gastric lesions in mice, both BSHE and BSHE:β-CD reduced gastric lesions, with 100 mg/kg dose of the complex having the greatest gastroprotective effect. BSHE:β-CD was also able to reduce gastric lesions from ischemia and reperfusion, with the 50 mg/kg dose being the most effective. BSHE:β-CD, also at this dose, reduced the MDA levels of the gastric mucosa, indicating a possible antioxidant activity in its gastroprotective effect. Thus, it was concluded that inclusion complex formation between β-CD and BSHE is possible, and that this formulation enhanced the gastric protective activity.