# Steering the Clinical Translation of Delivery Systems for Drugs and Health Products
## 3 Poster Presentations
### Colon Delivery of Nutraceutical Ingredients Using Food-Grade Polymer-Based Microparticles  
[PERSON] 1, [PERSON] 1, [PERSON] 1, [PERSON] 1, [PERSON] 2 and [PERSON] 1,*  
1 Department of Drug Sciences, University of Catania, 95125 Catania, Italy  
2 Department of Life Sciences, University of Modena and Reggio Emilia, 41121 Modena, Italy  
* Correspondence: [EMAIL_ADDRESS]  
Nutraceuticals are naturally occurring substances defined as nutritional components that induce physiological or therapeutic benefits able to prevent the onset of chronic diseases. Compared to pharmacological treatments, they have an intrinsically reduced toxicity and generate less side effects. Nutraceuticals include lipids, vitamins, phenolic compounds, peptides, and other compounds isolated from various sources such as spices, herbs and fruit. Oral administration of nutraceuticals is preferred in the case of chronic diseases, because it follows the same natural processes of food and nutrient intake in the body, being a non-invasive and high-compliance route. However, the limited solubility of most nutraceuticals, as well as the conditions of the gastro-intestinal tract (GIT) to which they are exposed, such as the low pH in the stomach, or presence of degradative and metabolic enzymes in the gut, largely reduce their overall bioavailability and therefore the therapeutic efficacy. In this respect, delivery systems, already exploited for the controlled and targeted oral release of drugs, become to be applied also in the nutraceutical field with some success [67]. In particular, conditions such as inflammatory bowel diseases (IBD), including ulcerative colitis and Crohn disease, as well as colorectal cancer would benefit of a specific colon delivery of active ingredients, without a systemic adsorption during the transit of the gut. pH-dependent drug release is one of the strategies proposed to focalize the delivery of actives within the colon, taking advantage of the relatively higher pH value of this area compared to the previous GIT sections [68]. The aim of this study was the production of polymeric microparticles for the controlled intestinal release of natural compounds, with adjuvant activity in the treatment of IBD and other colon diseases. In particular, we chose a class of acrylate polymers, commercialized as Eudraguard(r) by Evonik (Germany); they are included in the EU food additive list and received GRAS status in the USA. As well as the analogous 'pharma-grade' Eudragit(r) copolymers, Eudraguard(r) have been essentially proposed by the manufacturer for coating solid oral dosage forms, to achieve a pH-dependent controlled release. In previous works of ours, Eudragit(r) RS100 and RL100 matrices have been instead investigated for producing micro- and nanosized systems for the modified delivery of drugs and natural ingredients [69; 70; 71; 72]. We therefore hypothesized that also Eudraguard(r) polymers, and in particular Eudraguard(r) Control (EUG-C) and Biotic (EUG-B) could be suitable ingredients to produce microparticulate systems for the pH-controlled oral delivery of bioactive compounds. EUG-C is a neutral copolymer based on ethyl acrylate and methyl methacrylate with a ratio of 2:1. Coating with this material can protect nutraceuticalt actives from the acidic environment of the stomach. EUG-B is an anionic methacrylate copolymer based on methacrylate acid, methyl methacrylate and methyl acrylate. The ratio of the free carboxyl groups to the ester groups is approx. 1:10. Being soluble at pH values above 7.0, it can be used as a pH-triggered polymer to protect compounds from gastric acid in the stomach and bile acid in the small intestine, ensuring a release once the systems reach the colon. We used EUG-B and EUG-C, alone or in combination, to produce microparticles loaded with quercetin and resveratrol as models of a low-solubility and a high-solubility active compound, respectively. Different production techniques were investigated to optimize yields and quality of the microparticles.