In vivo prophylactic gastroprotection using α-bisabolol encapsulated in lipid-core nanocapsules and in cocoa-theospheres

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• 作者：Thatiana Ferreira Terroso^a ; Kelly Bueno Condotta^a ; Francisco Noé ; da Fonseca^a ; Denise Soledade Jornada^a ; Greice Oliveira Ferreira^a ; Joel Henrique Ellwanger^c ; ^d ; Juarez Alaor Schmidt^c ; Adriana Raffin Pohlmann^a ; ^b ; Sí ; lvia Stanisç ; uaski Guterres^a ; ^{silvia.guterres@ufrgs.br}
• 关键词：Cocoa-theospheres ; Lipid and polymeric nanoparticles ; Lipid-core nanocapsules ; α-Bisabolol ; Gastroprotection
• 刊名：Journal of Drug Delivery Science and Technology
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：36
• 期：Complete
• 页码：99-109
• 全文大小：3811 K
• 卷排序：36

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.