Drug Delivery to the Intestinal Lymphatic System.

A prodrug formulation to improve drug delivery to the intestinal lymphatic system

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Background.

The intestinal lymphatic system is the central organ for the immune system as it accommodates more than half of the body’s lymphocytes. Therefore, it offers a merit as a physiological compartment with enormous potential in improving treatment of immune system related diseases such as autoimmune diseases, lymphatic system- associated cancers, human immunodeficiency virus (HIV) infections and cancer metastasis.

However, only a very limited proportion of a drug can usually be distributed from the systemic circulation into the lymphatic system. Consequently, in order to achieve sufficient concentrations of the drugs in the affected lymph nodes, the required levels in the systemic circulation will be very high and associated with significant side effects. Accordingly, there is an unmet need for targeted increased delivery of therapeutic agents to the intestinal lymphatics.

The technology developed by the University of Nottingham is a novel method of delivering drugs to the intestinal lymphatic system, when the active drug molecule does not have right physicochemical properties. The advancement through employing the activated prodrug approach has been demonstrated to deliver a 17-fold increase of the active drug delivered to the mesenteric lymph nodes when compared to the drug alone. This enables a therapeutic dose to reach the lymphatic system after administration of a tolerable oral dose.

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