Focus on the Lymphatic Route to Optimize Drug Delivery in Cardiovascular Medicine

Abstract

While oral agents have been the gold standard for cardiovascular disease therapy, the new generation of treatments is switching to other administration options that offer reduced dosing frequency and more efficacy. The lymphatic network is a unidirectional and low-pressure vascular system that is responsible for the absorption of interstitial fluids, molecules, and cells from the peripheral tissue, including the skin and the intestines. Targeting the lymphatic route for drug delivery employing traditional or new technologies and drug formulations is exponentially gaining attention in the quest to avoid the hepatic first-pass effect. The present review will give an overview of the current knowledge on the involvement of the lymphatic vessels in drug delivery in the context of cardiovascular disease.

The role of lymphangiogenesis in cardiovascular diseases and heart transplantation

“…Preferential uptake into the lymphatics is highly dependent on the physicochemical properties of the particles, including size, molecular weight, surface charge, and lipophilicity [46]. Initial lymphatics draining the peritoneal submesothelial layer have favorable absorption of lipophilic and unionized compounds [47]. The study by using nonfasted rats has demonstrated that the lipoproteins in lymph are organ specific in composition, and the intestine and liver appear to be the main source of HDL that is modified during transport from the mesenteric and hepatic lymphatics to the thoracic duct [44].…”