Development of oral delivery systems for targeted gastro intestinal tract delivery of nutraceuticals using food grade polymers

• Main Author: Sampathkumar Kaarunya
• Other Authors: Loo Say Chye Joachim
• Format: Theses and Dissertations
• Language: English
• Published: 2019
• Subjects: DRNTU::Engineering::Materials
• Online Access: https://hdl.handle.net/10356/102665; http://hdl.handle.net/10220/47831
• Institution: Nanyang Technological University

The focus on alternative therapeutic strategies to overcome the side effects of the drugs and to act in synergy with drugs to maximize recovery is on the rise. Nutraceuticals are one of the candidates being explored as alternative or adjunctive therapy. Being of plant origin, most of the nutraceuticals are sensitive to degradation and suffer from the disadvantage of loss of bioactivity before they reach the target site. A suitable carrier would help maximize the benefits of these nutraceuticals. Oral route is one of the common methods for the consumption of such nutraceuticals or active ingredients (AI). Despite its numerous advantages, it faces many disadvantages also. Some them being the poor bioavailability of the AI, degradation of the AI during transit of the gastro intestinal tract (GIT), poor absorption and lack of action specificity. In order to overcome this, a food grade carrier system that can encapsulate nutraceuticals of varying solubilities and can also be incorporated into food materials, as a direct food additive is required. In spite of the growing research in this field, a food grade carrier, that can successfully target the delivery of the AI to different parts of the GIT, while preserving its bioactivity, is still lacking commercially. In view of this, a food grade oral delivery system for nutraceuticals was developed using chitosan and starch as the base materials. Chitosan nanoparticles (chnp) were prepared by electrospraying and used for encapsulating the AI. A coating of starch on these particles ensured targeted delivery of the encapsulated AI. The performance of the coating layer was tested in different simulated GIT fluids and was found to be comparable to that of the commercial enteric polymers. The berries of the plant, Withania coagulans, chosen as the nutraceutical candidate, was used to extract the nutraceutical coagulans. The extracts, an aqueous fraction and an organic fraction, were characterized using various analytical techniques and was found to match with that of previously reported extracts from the same plant. Three different bioactive properties of the extract were tested. The aqueous fraction was found to possess wound healing and anti-diabetic effects while the organic fraction was found to have an anti-cancer effect. The small intestine targeting ability of the carrier was proven by encapsulating the aqueous extract into the food grade carrier and demonstrating the anti-diabetic effect both in vitro and in vivo. The large intestine targeting ability of the carrier was proven by encapsulating the organic fraction into the carrier and demonstrating the anti-cancer effect in vitro. Hence the successful working of an oral delivery system, made entirely from food grade materials for targeting nutraceuticals to different parts of the gastro intestinal tract has been showcased as a step towards developing health benefiting food additives.