Encapsulation and controlled release formulations of 5-fluorouracil from natural Lycopodium clavatum spores

Cost effective, uniform-size multiparticulate formulations of the chemotherapeutic agent 5-fluorouracil (5-FU) loaded in natural Lycopodium clavatum spores were developed by three different encapsulation techniques: passive, compression and vacuum loading. The surface morphology, and micromeritic properties of 5-FU spore formulations were characterized by scanning electron microscopy and dynamic image particle analysis, respectively. The encapsulation efficiency of spores by vacuum-assisted loading was higher (49%) compared to passive and compression loading techniques. The vacuum-loaded formulation was selected for further development with a Eudragit RS 100 (EUD), coating that enabled controlled 5-FU release in simulated gastric (pH 1.2) and intestinal (pH 7.4) conditions. The surface morphology analysis after EUD coating at two different EUD concentrations (2.5% wiv and 10% wiv) indicates that a thin, conformal layer of EUD was deposited on the spore surface. The in-vitro release of 5 FU from coated spores exhibited a slower release profile compared to uncoated spores, and was extended for up to 30 h in simulated gastrointestinal conditions. Collectively, the findings demonstrate that EUD coated 5-FU loaded natural L. clavatum spores provide a controlled release formulation that would aid treatment options against gastrointestinal cancer and other related maladies. (C) 2016 The Korean Society of Industrial and Engineering Chemistry. Published by Elsevier B.V. All rights reserved.