Articulo
Polyethylene glycol-phosphatidylethanolamine conjugate as a pulmonary nanocarrier for poorly soluble drug
Autor
Tan, Yvonne T.F.
Abdulameer, Shaymaa A.
Peh, Kok K.
Darwis, Yusrida
Sahib, Mohanad N.
Institución
Resumen
The aim of this study was to investigate the potential of a polyethylene glycol-phosphatidylethanolamine conjugate (PEG<sub>2000</sub> -DSPE) to solubilize budesonide (BUD) for pulmonary delivery. The BUD-strictly stabilized phospholipid nanomicelles (SSMs) were prepared using the coprecipitation and reconstitution method and the physicochemical characteristics and pharmacodynamic duration of the BUD-SSMs were determined. The solubility of BUD was highly improved by at least 52 times its intrinsic solubility. The hydrodynamic particle size and zeta potential were 14.31 ± 1.40 nm and -46.61 ± 2.94 mV, respectively. The in vitro release of BUD from SSMs was completed within 6 days. Aerosolization of rehydrated BUD-SSMs with different nebulizers showed superior and significant aerodynamic characterizations compared to Pulmicort Respules® (PR). An in vivo study showed a significant reduction in the inflammatory cell counts of bronchoalveolar lavage fluid compared to PR. As a result, this study suggested that PEG<sub>2000</sub> -DSPE is a promising candidate as a budesonide carrier for pulmonary delivery. Colegio de Farmacéuticos de la Provincia de Buenos Aires