Incorporation of mangiferin in liposomes: studies of characterization and formulation stability for applications in studies of antiallergic potential

• Grant number: 13/26577-2
• Support type: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): April 01, 2014
• Effective date (End): January 31, 2015
• Field of knowledge: Health Sciences - Pharmacy
• Principal researcher: Rose Mary Zumstein Georgetto Naal
• Grantee: Sarah Angote dos Santos
• Home Institution: Faculdade de Ciências Farmacêuticas de Ribeirão Preto (FCFRP). Universidade de São Paulo (USP). Ribeirão Preto , SP, Brazil

Abstract

The increase in allergic diseases is a major public health problem in the developed world today. It is estimated that approximately one third of the global population is affected by allergic diseases, which are increasing at a rate without precedent, justified not only by genetic factors, but also by changes in the habits of our society, which include high pollution levels, confined housing and processed foods. The current drugs used to treat allergies, such as antihistamines or corticosteroids, improve symptoms but do not prevent the disease's progression. In addition, the side effects of chronic use of these medications are worrying, especially in the case of children, potential users into adulthood. In this context, the bioactive compounds play a key role and have been the subject of considerable studies in the search for new antiallergic therapeutic agents with fewer side effects. Several classes of natural substances have been investigated in recent years, especially flavonoids, which are potential inhibitors of allergic processes. Mangiferin, a xanthone of the flavonoids class, can be cited as an example of a natural bioactive substance, which has been widely studied due to its diverse pharmacological properties, including the antiallergic ones. However, the biological application of mangiferin and other flavonoids is hampered by its low solubility in water and susceptibility to photodegradation or chemical oxidation in solution. Thus, this work proposes the development of a physico-chemically stable liposomal formulation, with good incorporation of mangiferin, based on the lipids DMPC, DOTAP and cholesterol which are feasible for application in tests for antiallergic potential. The success of this work will open up possibilities for the use of other lipidic nanocarriers and the development of new viable formulations for in vivo applications of mangiferin . The biological testing of the antiallergic potential of the free and incorporated mangiferin into the nanocarrier will be conducted based on the direct quantitation of the beta - hexosaminidase enzyme released by mast cells stimulated by antigen, which has been used as a biosensor model (Naal et al. Biosens.Bioelectron,20,790-795,2004), in the screening of molecules with therapeutic potential. In addition to our experience with this assay and the molecular mechanisms involved in mast cell degranulation, our group and collaborators have all the necessary infrastructure for the development of this project. We emphasize finally that, despite its wide pharmacological properties, mangiferin is still little explored in studies about its incorporation into nanocarrier systems and their biological applications, justifying the relevance of this study. (AU)