Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins

In the present study, gastro-resistant microparticles (MPs) were produced using the spray-drying technique as controlled-release systems for some model liposoluble vitamins, including retinyl-palmitate, retinyl-acetate, β-carotene, cholecalciferol and α-tocopherol. The gastroprotective action of thr...

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Main Authors: Francesca Terracina, Roberto Caruana, Francesco Paolo Bonomo, Francesco Montalbano, Mariano Licciardi
Format: Article
Language:English
Published: MDPI AG 2022-07-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/14/7/1480
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author Francesca Terracina
Roberto Caruana
Francesco Paolo Bonomo
Francesco Montalbano
Mariano Licciardi
author_facet Francesca Terracina
Roberto Caruana
Francesco Paolo Bonomo
Francesco Montalbano
Mariano Licciardi
author_sort Francesca Terracina
collection DOAJ
description In the present study, gastro-resistant microparticles (MPs) were produced using the spray-drying technique as controlled-release systems for some model liposoluble vitamins, including retinyl-palmitate, retinyl-acetate, β-carotene, cholecalciferol and α-tocopherol. The gastroprotective action of three different gastro-resistant excipients, the anionic methacrylic copolymer (Eudraguard<sup>®®</sup> Biotic, E1207), the cellulose acetate phthalate (CAP) and whey proteins (WPs), was compared. The latter was used to produce a novel delivery system manufactured with only food-derived components, such as milk, and showed several improvements over the two synthetic gastro-resistant agents. Scanning electron microscopy (SEM) images showed a quite homogeneous spherical shape of all microparticle batches, with an average diameter between 7 and 15 μm. FTIR analysis was used to evaluate the effective incorporation of vitamins within the microparticles and the absence of any degradation to the components of the formulation. The comparison graphs of differential scanning calorimetry (DSC) confirmed that the spray drying technique generates a solid in which the physical interactions between the excipients and the vitamins are very strong. Release studies showed a prominent pH-controlled release and partially a delayed-release profile. Ex vivo permeation studies of retinyl palmitate, retinyl acetate and α-tocopherol revealed greater transmucosal permeation capacity for microparticles produced with the WPs and milk.
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spelling doaj.art-7eea78ac5ef3481ca259c655ec9163fb2023-11-30T21:42:25ZengMDPI AGPharmaceutics1999-49232022-07-01147148010.3390/pharmaceutics14071480Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble VitaminsFrancesca Terracina0Roberto Caruana1Francesco Paolo Bonomo2Francesco Montalbano3Mariano Licciardi4Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, 90123 Palermo, ItalyTechnology Scientific S.r.l., Viale delle Scienze, Edificio 18, 90128 Palermo, ItalyAdvanced Technologies Network Center (ATeN Center), Università degli Studi di Palermo, 90100 Palermo, ItalyTechnology Scientific S.r.l., Viale delle Scienze, Edificio 18, 90128 Palermo, ItalyDipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, 90123 Palermo, ItalyIn the present study, gastro-resistant microparticles (MPs) were produced using the spray-drying technique as controlled-release systems for some model liposoluble vitamins, including retinyl-palmitate, retinyl-acetate, β-carotene, cholecalciferol and α-tocopherol. The gastroprotective action of three different gastro-resistant excipients, the anionic methacrylic copolymer (Eudraguard<sup>®®</sup> Biotic, E1207), the cellulose acetate phthalate (CAP) and whey proteins (WPs), was compared. The latter was used to produce a novel delivery system manufactured with only food-derived components, such as milk, and showed several improvements over the two synthetic gastro-resistant agents. Scanning electron microscopy (SEM) images showed a quite homogeneous spherical shape of all microparticle batches, with an average diameter between 7 and 15 μm. FTIR analysis was used to evaluate the effective incorporation of vitamins within the microparticles and the absence of any degradation to the components of the formulation. The comparison graphs of differential scanning calorimetry (DSC) confirmed that the spray drying technique generates a solid in which the physical interactions between the excipients and the vitamins are very strong. Release studies showed a prominent pH-controlled release and partially a delayed-release profile. Ex vivo permeation studies of retinyl palmitate, retinyl acetate and α-tocopherol revealed greater transmucosal permeation capacity for microparticles produced with the WPs and milk.https://www.mdpi.com/1999-4923/14/7/1480gastro-resistant microparticlesvitaminsspray-dryingwhey proteinsEudraguardcellulose acetate phthalate
spellingShingle Francesca Terracina
Roberto Caruana
Francesco Paolo Bonomo
Francesco Montalbano
Mariano Licciardi
Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
Pharmaceutics
gastro-resistant microparticles
vitamins
spray-drying
whey proteins
Eudraguard
cellulose acetate phthalate
title Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
title_full Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
title_fullStr Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
title_full_unstemmed Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
title_short Gastro-Resistant Microparticles Produced by Spray-Drying as Controlled Release Systems for Liposoluble Vitamins
title_sort gastro resistant microparticles produced by spray drying as controlled release systems for liposoluble vitamins
topic gastro-resistant microparticles
vitamins
spray-drying
whey proteins
Eudraguard
cellulose acetate phthalate
url https://www.mdpi.com/1999-4923/14/7/1480
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