Abstract The motive behind present work was to discover a solution for overcoming the problems allied with a deprived oral bioavailability of salbutamol sulfate (SS) due to its first pass hepatic metabolism, shorter half-life, and systemic toxicity at high doses. Pulmonary delivery provides an alternative route of administration to avoid hepatic metabolism of SS, moreover facilitated diffusion and prolonged retention can be achieved by incorporation into liposomes. Liposomes were prepared by thin film hydration technique using 32 full factorial design and formulation was optimized based on the vesicle size and percent drug entrapment (PDE) of liposomes. Optimized liposomal formulation exhibited an average size of about 167.2 ± 0.170 nm, with 80.68 ± 0.74% drug entrapment, and 9.74 ± 1.10 mV zeta potential. The liposomal dispersion was then spray dried and further characterized for in-vitro aerosol performance using Andersen Cascade Impactor. Optimized liposomal formulation revealed prolonged in-vitro drug release of more than 90% up to 14 h following Higuchi’s controlled release model. Thus, the proposed new-fangled liposomal formulation would be a propitious alternative to conventional therapy for efficient and methodical treatment of asthma and alike respiratory ailments.

中文翻译：

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纳米脂质体硫酸沙丁胺醇干粉吸入的肺递送用于促进哮喘治疗

摘要 目前工作背后的动机是发现一种解决方案，以克服硫酸沙丁胺醇 (SS) 由于首过肝脏代谢、半衰期较短和高剂量全身毒性而导致口服生物利用度不足的问题。肺部给药提供了另一种给药途径，以避免 SS 的肝脏代谢，此外，通过掺入脂质体可以促进扩散和延长滞留时间。脂质体通过薄膜水合技术使用 32 全因子设计制备，并根据脂质体的囊泡大小和药物包封率 (PDE) 优化配方。优化的脂质体制剂的平均尺寸约为 167.2 ± 0.170 nm，药物包封率为 80.68 ± 0.74%，zeta 电位为 9.74 ± 1.10 mV。然后将脂质体分散体喷雾干燥，并使用 Andersen Cascade Impactor 进一步表征体外气溶胶性能。优化的脂质体配方显示，按照 Higuchi 的控释模型，体外药物释放时间延长了 90% 以上，最长可达 14 小时。因此，所提出的新型脂质体制剂将是常规疗法的有利替代品，用于有效和有条理地治疗哮喘和类似的呼吸系统疾病。