Formulation and optimization of sildenafil citrate-loaded PLGA large porous microparticles using spray freeze-drying technique: A factorial design and in-vivo pharmacokinetic study.

摘要: The oral administration of sildenafil citrate (SC) for the treatment pulmonary arterial hypertension is associated with several drawbacks. study aimed to design and formulate SC-loaded inhalable poly (lactic-co-glycolic acid) [PLGA] large porous microparticles (LPMs) delivery. A factorial was used effect composition LPMs on physicochemical properties. also evaluated glucose L-leucine concentration formulation. developed demonstrated an acceptable yield% (≤48%), geometric particle size (>5µm) a spherical surface, sustained drug release (up 48 h). Increasing poly(ethyleneimine) from 0.5% 1% in led increase entrapment efficiency ~3.02% ~94.48%. optimum showed adequate aerodynamic properties 97.68 ± 1.07% recovery, 25.33 ± 3.32% fine fraction, low cytotoxicity. Intratracheal significantly higher lung deposition, systemic bioavailability, longer retention time (p < 0.05) compared orally administered Viagra® tablets. concluded that could provide better therapeutic efficacy, reduced dosing frequency, enhanced patient compliance.