文摘
This study describes the development of α-bisabolol-loaded lipid-core nanocapsules (α-BLNC) and Cocoa-theospheres (α-BCT), aiming oral use for gastroprotection. α-Bisabolol was efficiently encapsulated in high drug loading (25%) in lipid-core nanocapsules and cocoa-theospheres. Laser diffraction analysis showed nanometric and unimodal distributions (mean diameters of 216 and 148 nm, respectively). The gastroprotective indexes in rats for the ethanol-induced ulcers were 0.11 (α-BCT), 0.68 (blank-CT), 0.29 (α-BLNC) and 0.37 (blank-LNC), while for the indomethacin-induced ulcer model, the results were 37.33 (α-BCT), 48.14 (blank-CT), 31.33 (α-BLNC) and 45.33 (blank-LNC). SEM analysis of the stomach mucosa showed more homogenous and cohesive coatings for α-BLNC and α-BCT treatments in comparison with the blank formulations. In histological evaluations, protection against the tissue damage and Periodic Acid-Schiff-positive increase were observed after the pretreatment with α-bisabolol nanoparticles in ethanol and indomethacin-induced ulcers. α-Bisabolol-loaded in cocoa-theospheres provided a gastroprotective effect absent in blank-cocoa-theospheres, while the drug-loaded lipid-core nanocapsules maintained the gastroprotective effect observed for blank lipid-core nanocapsules, which are per se antioxidant agents. The nanoencapsulation enabled a dose reduction of α-bisabolol. Moreover, lipid-core nanocapsules and cocoa-theospheres have mucoadhesive properties even though they present diverse supramolecular structures. Both lipid-core nanocapsules and cocoa-theospheres are promising platforms for the development of prophylactic formulations.
