Improving solubility and chemical stability of natural compounds for medicinal use by incorporation into liposomes

Maria Coimbra, Benedetta Isacchi, Louis van Bloois, Javier Sastre Torano,  Aldo Ket, Xiaojie Wu, Femke Broere, Josbert M. Metselaar, Cristianne J.F. Rijcken, Gert Storm, Rita Bilia, Raymond M. Schiffelers, 

Abstract

Natural bioactive compounds have been studied for a long time for their chemopreventive and therapeutic potential in several chronic inflammatory diseases, including cancer. However, their physicochemical properties generally result in poor chemical stability and lack of in vivo bioavailability. Very few human clinical trials have addressed absorption, distribution, metabolism, and excretion of these compounds in relation to efficacy. This limits the use of these valuable natural compounds in the clinic.

In this study, we examined caffeic acid (derivatives), carvacrol (derivatives), thymol, pterostilbene (derivatives), and N-(3-oxo-dodecanoyl)-l-homoserine lactone. These are natural compounds with strong anti-inflammatory properties derived from plants and bacteria. However, these compounds have poor water solubility or are chemically unstable. To overcome these limitations we have prepared liposomal formulations. Our results show 

Resveratrol was purchased from Chengdu Biopurify Phytochemicals Ltd. (China).