Colon Drug Delivery Systems Based on Swellable and Microbially Degradable High-Methoxyl Pectin: Coating Process and In Vitro Performance

Author:

Moutaharrik Saliha1ORCID,Palugan Luca1,Cerea Matteo1ORCID,Meroni Gabriele2ORCID,Casagni Eleonora3,Roda Gabriella3,Martino Piera Anna2ORCID,Gazzaniga Andrea1,Maroni Alessandra1,Foppoli Anastasia1ORCID

Affiliation:

1. Department of Pharmaceutical Sciences, Section of Pharmaceutical Technology and Legislation “M.E. Sangalli”, University of Milan, Via G. Colombo 71, 20133 Milan, Italy

2. Department of Biomedical, Surgical and Dental Sciences, One Health Unit, University of Milan, Via Pascal 36, 20133 Milan, Italy

3. Department of Pharmaceutical Sciences, Section of Medicinal Chemistry “P. Pratesi”, University of Milan, Via Trentacoste 2, 20134 Milan, Italy

Abstract

Oral colon delivery systems based on a dual targeting strategy, harnessing time- and microbiota-dependent release mechanisms, were designed in the form of a drug-containing core, a swellable/biodegradable polysaccharide inner layer and a gastroresistant outer film. High-methoxyl pectin was employed as the functional coating polymer and was applied by spray-coating or powder-layering. Stratification of pectin powder required the use of low-viscosity hydroxypropyl methylcellulose in water solution as the binder. These coatings exhibited rough surfaces and higher thicknesses than the spray-coated ones. Using a finer powder fraction improved the process outcome, coating quality and inherent barrier properties in aqueous fluids. Pulsatile release profiles and reproducible lag phases of the pursued duration were obtained from systems manufactured by both techniques. This performance was confirmed by double-coated systems, provided with a Kollicoat® MAE outer film that yielded resistance in the acidic stage of the test. Moreover, HM pectin-based coatings manufactured by powder-layering, tested in the presence of bacteria from a Crohn’s disease patient, showed earlier release, supporting the role of microbial degradation as a triggering mechanism at the target site. The overall results highlighted viable coating options and in vitro release characteristics, sparking new interest in naturally occurring pectin as a coating agent for oral colon delivery.

Publisher

MDPI AG

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