药剂学与药物输送研究杂志

A Novel Microparticulate Formulation with Allicin In Situ Synthesis

Boris Strehlow, Udo Bakowsky, Shashank Reddy Pinnapireddy, Jan Kusterer, Gabriela Mielke and Michael Keusgen

A Novel Microparticulate Formulation with Allicin In Situ Synthesis

Abstract

The development of Garlic as a commercial antibiotic has come to a halt. Although its efficiency is scientifically proven; it has only been used as dietary supplement or as traditional medicine. In this study we investigated the use of spray drying to obtain a powder which releases allicin, the most important antibiotic active compound in garlic. Alliin and alliinase, which serve as precursors for allicin production, were encapsulated separately into microspheres consisting of lactose as a stabiliser and as an excipient. The resulting powders, containing spray dried alliin (AllSP) or alliinase (AseSP), could be mixed and stored as a single entity without the risk of interaction. The particles from the combined powders dissolute the moment they come in contact with water and release alliin and alliinase which readily react to allicin (Figure 1). This production of allicin works successfully in a surfactant too. Allicin from AllSP and AseSP showed an antimicrobial effect against E.coli. Through Spray drying, particles small enough for alveolar application, can be obtained. The motive behind our formulation is the on-thespot synthesis of the very unstable allicin. For the first time in situ synthesised allicin was made available under safe and reproducible conditions for pulmonary application. This helps treating lung infections caused by a broad spectrum of pathogens at a low level of toxicity.