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Formulation, characterization and statistical optimization of enalapril-loaded lipospheres
Bioinspired, Biomimetic and Nanobiomaterials ( IF 1.3 ) Pub Date : 2020-12-23 , DOI: 19.00065
Safirah Maheen, Akhtar Rasul

Lipid-based polymers have been proved efficient drug carriers for overcoming the insufficiencies of conventional formulations. Ceresin wax was employed to improve permeability, oral bioavailability and patient compliance by preparing enalapril (EP)-loaded lipospheres with a simple solvent evaporation method. A Box–Behnken design with the proposed polynomial equations and quadratic model was applied to investigate and statistically validate the collective influence of formulation variables on lipospheres. Spherical smooth-surfaced lipospheres with an average size of 55 μm with excellent micromeritic properties were produced. Differential scanning calorimetry, X-ray diffraction and Fourier transmission infrared spectroscopy findings proved the lack of any possible interaction between formulation components. The zeta potential ranged from −5 to −20 mV, suggesting the significant stability of lipospheres. Responses such as percentage yield (29–68%), entrapment efficiency (21–53%) and drug release (42–93%) were found to be affected greatly by the concentrations of lipids and the surfactant, and the stirring speed. Reduced and sustained EP release from lipospheres may lower treatment cost and enhance hypertensive patients’ compliance.

中文翻译:

依那普利脂质体的配制,表征和统计学优化

脂质类聚合物已被证明是克服常规制剂不足的有效药物载体。通过简单的溶剂蒸发方法制备负载依那普利(EP)的脂球,使用蜡质蜡来改善通透性,口服生物利用度和患者依从性。采用拟议的多项式方程式和二次模型的Box-Behnken设计用于调查和统计验证配方变量对脂球的集体影响。制备了平均粒径为55μm且具有优异微团性质的球形光滑表面脂球。差示扫描量热法,X射线衍射和傅立叶透射红外光谱法的发现证明制剂组分之间没有任何可能的相互作用。ζ电势的范围为-5至-20 mV,表明脂球具有显着的稳定性。发现诸如脂类和表面活性剂的浓度以及搅拌速度对诸如百分产率(29-68%),截留率(21-53%)和药物释放(42-93%)等反应的影响很大。脂球中EP释放的减少和持续释放可能会降低治疗成本并增强高血压患者的依从性。
更新日期:2020-12-23
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