Investigation of Mucoadhesion and Degradation of PCL and PLGA Microcontainers for Oral Drug Delivery.

Zarmeena Abid,Stephan Sylvest Keller,Line Hagner Nielsen,Ritika Singh Petersen,Mette Dalskov Mosgaard,Anette Müllertz,Anja Boisen,Giorgio Manfroni

doi:10.3390/polym11111828

Abstract

Microfabricated devices have been introduced as a promising approach to overcome some of the challenges related to oral administration of drugs and, thereby, improve their oral bioavailability. In this study, we fabricate biodegradable microcontainers with different polymers, namely poly-ɛ-caprolactone (PCL), poly(lactic-co-glycolic acid) (PLGA) 50:50 and PLGA 75:25 by hot punching. The mucoadhesion of the microcontainers is assessed with an ex vivo retention model on porcine intestinal tissue. Finally, in vitro degradation studies of the biodegradable microcontainers are completed for six weeks in simulated intestinal medium with the addition of pancreatic enzymes. Through SEM inspection, the PLGA 50:50 microcontainers show the first signs of degradation already after two weeks and complete degradation within four weeks, while the other polymers slowly degrade in the medium over several weeks.

Highlights

Oral drug delivery is the most preferred administration route due to its minimally invasive nature and high patient compliance
Based on the demand of fabricating microdevices in biocompatible and biodegradable materials, we recently demonstrated the successful fabrication of biodegradable microcontainers using hot punching, which is a modified hot embossing method [12]
The aim of this work is to evaluate the suitability of different polymeric materials for microfabricated drug delivery devices where mucoadhesive properties and biodegradability are important

Summary

Introduction

Oral drug delivery is the most preferred administration route due to its minimally invasive nature and high patient compliance. Oral drug delivery faces several challenges, such as pre-systemic intestinal degradation, hepatic first pass elimination, as well as low solubility of some drugs in the fluids of the gastrointestinal (GI) tract, leading to reduced oral bioavailability of the drug [1,2]. One goal in the development of oral drug delivery systems is to reduce the dosage and thereby minimize the adverse effects of the drug, which can be achieved by increasing the amount of drug released and absorbed at the targeted site in the GI tract. Polymers 2019, 11, 1828 mucoadhesion has been shown increased interest in oral drug delivery as it potentially enhances the bioavailability due to longer retention times of drug at the intended sites of absorption [3,4]. Numerous methods have been proposed to assess the mucoadhesive properties of drug formulations in vitro and ex vivo

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Conclusion