Department of Pharmaceutics, Annasaheb Dange College of B. Pharmacy, Shivaji University , Kolhapur , India.
Bharati Vidyapeeth's College of Pharmacy, Shivaji University , Kolhapur , India.
J Liposome Res. 2019 Dec;29(4):332-342. doi: 10.1080/08982104.2018.1531022. Epub 2019 May 23.
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 3 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 aerosol performance using Andersen Cascade Impactor. Optimized liposomal formulation revealed prolonged 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.
本工作的目的是为了解决硫酸沙丁胺醇(SS)因首过肝脏代谢、半衰期短和高剂量下的全身毒性而导致口服生物利用度降低的问题。肺部给药提供了一种替代的给药途径,可以避免 SS 的肝脏代谢,此外,通过将其纳入脂质体,可以实现促进扩散和延长保留。脂质体采用薄膜水化技术制备,使用 3 因素完全设计,根据脂质体的粒径和药物包封率(PDE)对制剂进行优化。优化的脂质体制剂的平均粒径约为 167.2±0.170nm,药物包封率为 80.68±0.74%,Zeta 电位为 9.74±1.10mV。然后,将脂质体分散体喷雾干燥,并使用 Andersen 级联撞击器进一步评估其气溶胶性能。优化的脂质体制剂在 14 小时内按照 Higuchi 控释模型显示出超过 90%的延长药物释放。因此,拟议的新型脂质体制剂将是一种有前途的替代传统疗法的方法,可有效和系统地治疗哮喘和类似的呼吸道疾病。