A time-controlled delivery system for nicotine using a nicotine pectin salt formulation for colon-targeted delivery

Deborah Shalev, Department of Pharmaceutical Engineering , Azrieli College of Engineering Jerusalem, Jerusalem, Israel (debbie@jce.ac.il)
Mila Gomberg, Department Of Research And Development, Polycaps Ltd., Jerusalem, Israel
Noa Badel, Department Of Pharmaceutical Engineering , Azrieli College Of Engineering Jerusalem, Jerusalem, Israel
Adel Penhasi, Department Of Research And Development, Polycaps Ltd. , Jerusalem, Israel

Local delivery of nicotine to the colon may be effective in therapy for patients suffering from ulcerative colitis. Nicotine was incorporated into a colon-specific formulation by preparing nicotine pectinate (NiP) salts from methoxylated pectin and nicotine in a water-isopropanol mixture. The water-isopropyl alcohol ratio was found to be central to the ability to form the NiP.The tablets were coated by a combination of Eudragit E (Eud.E) and calcium pectinate (CaP) particulates to obtain a delayed release corresponding to the planned time of delivery in the colon. The rate and time of onset of release of nicotine from the tablets could be controlled to provide precise delivery in the colon by optimizing the core formulation and adjusting the ratio between Eud. E and CaP, and the thickness of the film coating. The dissolution profiles of nicotine release from the coated tablets were compared to those of a commercial nicotine resinate product, Polacrilex.

The mode of binding was determined at the molecular level by nuclear magnetic resonance (NMR) and infrared spectroscopy (ATR-FTIR) to verify the interactions between the nicotine and pectin. Differential scanning calorimetry (DSC) was used to determine the thermal properties of the nicotine pectinate complexes for pectin with differing low degrees of methoxylation. 

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Abstract Reference & Short Personal Biography of Presenting Author

Deborah Shalev is a Professor of Chemistry and Head of the Department of Pharmaceutical Engineering at Azrieli College of Engineering Jerusalem. She did all her degrees at Tel Aviv University and then served as the liaison between academia and industry in a consortium for drug design of the Chief Scientist of Israel. She continued working with NMR as a research scientist at the Wolfson Centre for Applied Structural Biology at the Hebrew University of Jerusalem where she still holds a partial position. In 2011, Deborah joined the faculty at the Azrieli College where her interests are in spectroscopic and thermal analyses of polymeric systems for extended release.