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In silico and in vitro study of epiisopiloturine/ hydroxypropyl-β-cyclodextrin inclusion complexes obtained by different methods

2021; Elsevier BV; Volume: 65; Linguagem: Inglês

10.1016/j.jddst.2021.102658

2588-8943

Cybelly Marques de Melo, Andréa Luciana Da Silva, Karolynne Rodrigues de Melo, Paulo César Dantas da Silva, Myla Lôbo de Souza, André Luiz Moreira Domingues de Sousa, Marcelo Montenegro Rabello, Leiz Maria Costa Véras, Larissa Araújo Rolim, Pedró José Rolim Neto,

Drug Transport and Resistance Mechanisms

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.