Lactose-Gated Mesoporous Silica Particles for Intestinal Controlled Delivery of Essential Oil Components: An In Vitro and In Vivo Study
Elisa Poyatos-Racionero,
Isabel González-Álvarez,
Paola Sánchez-Moreno,
Leopoldo Sitia,
Francesca Gatto,
Pier Paolo Pompa,
Elena Aznar,
Marta González-Álvarez,
Ramón Martínez-Máñez,
María Dolores Marcos,
Andrea Bernardos
Affiliations
Elisa Poyatos-Racionero
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain
Isabel González-Álvarez
Departamento de Ingeniería, Sección de Farmacia y Tecnología Farmacéutica, Universidad Miguel Hernández, 03550 Alicante, Spain
Paola Sánchez-Moreno
Department of Applied Physics, Faculty of Sciences, University of Granada, Avenida Fuente Nueva s/n, 18071 Granada, Spain
Leopoldo Sitia
Nanomedicine Laboratory, Department of Biomedical and Clinical Sciences “Luigi Sacco”, University of Milano, 20157 Milan, Italy
Francesca Gatto
Nanobiointeractions & Nanodiagnostics, Istituto Italiano di Tecnologia (IIT), Via Morego, 30, 16163 Genova, Italy
Pier Paolo Pompa
Nanobiointeractions & Nanodiagnostics, Istituto Italiano di Tecnologia (IIT), Via Morego, 30, 16163 Genova, Italy
Elena Aznar
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain
Marta González-Álvarez
Departamento de Ingeniería, Sección de Farmacia y Tecnología Farmacéutica, Universidad Miguel Hernández, 03550 Alicante, Spain
Ramón Martínez-Máñez
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain
María Dolores Marcos
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain
Andrea Bernardos
Instituto Interuniversitario de Investigación de Reconocimiento Molecular y Desarrollo Tecnológico (IDM), Universitat Politècnica de València, Universitat de València, Camino de Vera s/n, 46022 Valencia, Spain
Mesoporous silica microparticles functionalized with lactose for the specific release of essential oil components (EOCs) in the small intestine are presented. In vitro and in vivo intestinal models were applied to validate the microparticles (M41-EOC-L), in which the presence of lactase acts as the triggering stimulus for the controlled release of EOCs. Among the different microdevices prepared (containing thymol, eugenol and cinnamaldehyde), the one loaded with cinnamaldehyde showed the most significant Caco-2 cell viability reduction. On the other hand, interaction of the particles with enterocyte-like monolayers showed a reduction of EOCs permeability when protected into the designed microdevices. Then, a microdevice loaded with cinnamaldehyde was applied in the in vivo model of Wistar rat. The results showed a reduction in cinnamaldehyde plasma levels and an increase in its concentration in the lumen of the gastrointestinal tract (GIT). The absence of payload release in the stomach, the progressive release throughout the intestine and the prolonged stay of the payload in the GIT-lumen increased the bioavailability of the encapsulated compound at the site of the desired action. These innovative results, based on the specific intestinal controlled delivery, suggest that the M41-payload-L could be a potential hybrid microdevice for the protection and administration of bioactive molecules in the small intestine and colon.
