Abstract
Epiisopiloturine (EPI) is the highest yielding alkaloid generated by the pilocarpine extraction process. Recent studies proved its anti-leishmaniasis, anti-schistosomiasis, anti-inflammatory and gastric protective activities. However, EPI presents a technological challenge regarding its low aqueous solubility. Thus, one of the ways to reduce this physicochemical limitation is the complexation with cyclodextrins (CDs), like hydroxypropyl-β-cyclodextrin (HP-β-CD). The present study aimed to develop and characterize the inclusion complex (EPI:HP-β-CD) obtained by kneading, nebulization and lyophilization. Molecular modelling showed that the EPI:HP-βC-D complex is more stable than β-CD:EPI complex. Inclusion complexes provided an increase in dissolution rate, greater than 90% of dissolved EPI, compared to 26.62% of the isolated prototype in the first 10 min. The FTIR, X-RD, SEM, DSC, TG tests demonstrated that there is a reduction in the crystallinity of the systems, providing an increase in EPI solubility. Thus, the inclusion complex is an interesting alternative for increasing solubility of EPI and developing a pharmaceutical dosage form.
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