Oral nanoparticles based on gellan gum/pectin for colon-targeted delivery of resveratrol

Abstract

Nanoparticles based on gellan gum/pectin blends were designed for colon-targeted release of resveratrol (RES). Their impact on drug release rates and permeability were evaluated using Caco-2 cell model and mucus secreting triple co-culture model. Polymeric nanoparticles (PNP) were successfully prepared by nebulization/ionotropic gelation, achieving high drug loading (>80%). PNP were spherical with a low positive charge density (+5mV) and exhibited diameters of around 330 nm. Developed PNP were able to promote effective modulation of drug release rates, so that only 3% of RES was released in acidic media over 2 h, and, in pH 6.8, the drug was released in a sustained manner, reaching 85% in 30 h. The permeability of RES-loaded PNP in the Caco-2 model was 0.15%, while in the triple co-culture model, in the presence of mucus, it reached 5.5%. The everted gut sac experiment corroborated the low permeability of RES-loaded PNP in the presence or absence of mucus and highlighted their high ability to interact with the intestinal tissue. Results indicate that the novel PNP developed in this work are safe and promising carriers for controlled delivery of RES at the colon.

Keywords:

• Polymeric nanoparticles
• colon-targeted release
• in vitro permeability
• caco-2 cells
• triple co-culture model
• everted gut sac

Disclosure statement

The authors declare that they have no conflict of interest.

Additional information

Funding

This study is part of the National Institute of Science and Technology in Pharmaceutical Nanotechnology: a transdisciplinary approach INCT-NANOFARMA, which is supported by São Paulo Research Foundation (FAPESP, Brazil) [Grant #2014/50928-2], and by ‘‘Conselho Nacional de Desenvolvimento Científico e Tecnológico’’ (CNPq, Brazil) [Grant # 465687/2014-8]. Authors would like to thank financial support provided by Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) and Fundação de Amparo e Pesquisa do Estado de São Paulo (FAPESP). This work was financed by the project NORTE-01-0145-FEDER-000012 by Norte Portugal Regional Operational Programme (NORTE 2020), and COMPETE 2020 - Operacional Programme for Competitiveness and Internationalisation (POCI), under the PORTUGAL 2020 Partnership Agreement, through the FEDER - Fundo Europeu de Desenvolvimento Regional, and by Portuguese funds through FCT - Fundação para a Ciência e a Tecnologia/ Ministério da Ciência, Tecnologia e Ensino Superior in the framework of the project "Institute for Research and Innovation in Health Sciences" UID/BIM/04293/2019.Andreia Almeida would like to thank Fundação para a Ciência e a Tecnologia (FCT), Portugal for financial support [Grant SFRH/BD/118721/2016].