DESIGN AND EVALUATION OF A DUAL-COATED CAPSULE FOR CONCOMITANT COLON DELIVERY OF LIVING BACTERIA AND SMALL MOLECULE MODEL COMPOUNDS
ALEKSANDAR ALEKSOVSKI 1*, VIVIANE LEOPOLD 1, ANDER SAGASTA 1, MICHAËLA LEITE 1, HANIEH HOSSEINI 1, ELENA MARINELLI 2, HAJAR ALKHAFAJI 2, JETTE JEPMOND MORTENSEN 2, JEANETTE THEIL JOHANSEN 2
1Bacthera AG, Hochbergerstrasse 60A, 4057 Basel, Switzerland
2 Bacthera A/S, Kogle Alle 6, DK-2970 Hørsholm, Denmark
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Live biotherapeutic products, alone or in combination with other medicines, are emerging as promising and novel therapeutic modalities aimed to prevent and treat various types of health conditions and meet the unmet treatment needs. The colon represents one of the major sites of action of living bacteria when applied orally and thus designing a robust and precise delivery system is of crucial importance. Within this research a colon targeting formulation platform has been developed for concomitant delivery of a model living bacteria and model small molecule substance. Dual coating of capsules based on inner dextrin/pH dependent polymer layer enabling precise colon delivery and outer layer based on pH dependent polymer enabling acid-protection and minimal release in the gastric segment has been designed. Variations in the amount of polymer/dextrin in the inner layer tended to affect product performance - disintegration, and dissolution while applying the outer layer provided extensive strain protection and prevention of premature drug release. The formulation containing dextrin:polymer ratio of 20%:80% in the inner coating layer tended to provide the most optimal product performance and proved that the applied approach of dual capsule coating triggering pH- and enzymatic-dependent release is viable manner to precisely target the colon.
