Tadalafil-loaded PLGA microspheres for pulmonary administration: preparation and evaluation
Abstract
Tadalafil, a long-acting PED-5 inhibitor, is commonly used for the treatment of pulmonary arterial hypertension (PAH).However, its efficacy and clinical application are severely limited by the poor water solubility, low bioavailability and a series adverse effects (e.g.headaches, indigestion).In this study, tadalafil was prepared and loaded into biodegradable PLGA (poly(lactic-co-glycolic acid)) microspheres (TDF-PLGA-MS) via emulsification-solvent evaporation.The resulting microspheres were processed into pulmonary inhalant by freeze drying.The TDF-PLGA-MS was spherical and uniform, with an average particle diameter ~10.29 μm.The encapsulation efficiency and drug loading yield of TDF-PLGA-MS were 81.68% and 8.52%, respectively.The investigation of micromeritics showed that the TDF-PLGA-MS had low moisture content.The fluidity of powders was relatively good.The aerodynamic diameter and emptying rate of microspheres powders were 3.92 μm and 95.41%, respectively.Therefore, the microspheres powders were easy to be atomized, and can meet the requirements of pulmonary administration.In vitro release results showed that the microspheres group released slowly.The cumulative release in 24 h and 10 d was 46.87% and 84.06%, respectively.The in vitro release profile of TDF-PLGA-MS was in accordance with the Weibull model.The results of Pharmacokinetics showed that tadalafil from microspheres slowly released into the blood after intratracheal instillation.The pulmonary drug residue in…
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