Dipropionato de beclometasona em formulação lipossomal como po inalavel para o tratamento de doenças pulmonares

AUTOR(ES)
DATA DE PUBLICAÇÃO

2007

RESUMO

The liposomal drug encapsulation for medical applications is in many instances the most efficient way to ensure good storage, transport, targeting, and controlled release of the drug, thus reducing toxicity. Liposomes have been extensively studied as vehicles for efficient drug delivery. The objective of the present work is to develop a formulation of the corticosteroid Beclomethasone Dipropionate (BecD) encapsulated in liposomes to be used in the form of an inhalable dry powder for the treatment of asthma and other chronic obstructive pulmonary diseases (COPD). Liposomal formulations with incorporated BecD were prepared with Lipoid E80 and Epikuron 200SH phospholipids. The liposomal dispersions were produced by the hydration of dry films composed of lipids and DBec by using the Bangham, Lyophilization-Hydration, and Multitubular System methods. The obtained liposomal dispersions were characterized as to their mean hydrodynamic diameter and polydispersity, their phosphate content, the BecD encapsulation efficiency, and the level of lipid peroxidation. The small angle X-ray scattering (SAXS) method was utilized to determine the liposome bilayer thickness and the effect of BecD in the lipid/water system main phase transition temperature. The excipients lactose monohydrate, magnesium stearate, L-leucine, trehalose, and ?-tocopherol were added to the liposomal dispersions, which were further lyophilized to produce the inhalable powder. The characterization of the inhalable powder fluidity was performed through Carr?s compressibility index method, and angle of repose measurements. The best efficiency for the encapsulation of BecD was obtained with the Lyophilization-Hydration method, however, all methods were able to produce BecD encapsulated liposomes with diameters adequate for pulmonary administration (<6 µm). As to easy operation and scale-up potential, the Multitubular System method showed to be very promising for the production of liposomal formulations with BecD

ASSUNTO(S)

drogas sinteticas lipossomos asma medicaments medicamentos biotecnologia farmaceutica lipossoms surfactante pulmonar

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