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首页> 外文期刊>International Journal of Pharmaceutics >Development of liposomal capreomycin sulfate formulations: effects of formulation variables on peptide encapsulation.
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Development of liposomal capreomycin sulfate formulations: effects of formulation variables on peptide encapsulation.

机译：脂质体硫酸卡普霉素制剂的开发：制剂变量对肽包封的影响。

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PURPOSE: The aim of this work was the investigation of the effects of preparation variables on drug content for the development of capreomycin sulfate (CS) liposomal formulations as potential aerosol antitubercular agents. METHODS: Dipalmitoylphosphatidylcholine (DPPC), hydrogenated phosphatidylcholine (HPC) and distearoylphosphatidylcholine (DSPC) were used for liposome preparation. A freeze-thawing method was chosen for CS encapsulation. Peptide entrapment, size and morphology were evaluated by UV spectrophotometry, photocorrelation spectroscopy (PCS) and transmission electron microscopy (TEM), respectively. A 2(3) full factorial protocol was designed to evaluate the conditions for CS encapsulation improvement. RESULTS: Peptide content ranged between 1 and 8%. Vesicles showed a narrow size distribution, with average diameters around 1 microm and a good morphology. A mathematical model was generated for each liposomal system and check point analyses revealed good agreement between experimental and predicted values. DPPC liposomes were found to provide the highest CS content. CONCLUSIONS: Peptide content was successfully increased by assessing formulation variable effects using a 2(3) factorial design that proved to be a time saving method helpful in developing new CS liposomal formulations for a possible application in aerosol antitubercular therapies.
机译：目的：这项工作的目的是研究制备变量对药物含量的影响，以开发硫酸卡普霉素（CS）脂质体制剂作为潜在的气溶胶抗结核剂。方法：采用双棕榈酰磷脂酰胆碱（DPPC），氢化磷脂酰胆碱（HPC）和二硬脂酰磷脂酰胆碱（DSPC）制备脂质体。选择冻融法进行CS封装。分别通过紫外分光光度法，光相关光谱法（PCS）和透射电子显微镜（TEM）评估了肽的包封，大小和形态。设计了2（3）个全因子协议以评估CS封装改进的条件。结果：肽含量介于1和8％之间。囊泡显示出狭窄的尺寸分布，平均直径约为1微米，并且形态良好。为每个脂质体系统生成一个数学模型，检查点分析显示实验值和预测值之间具有良好的一致性。发现DPPC脂质体提供最高的CS含量。结论：通过使用2（3）因子设计评估制剂的变量效应，成功地增加了肽含量，这被证明是一种节省时间的方法，有助于开发新的CS脂质体制剂，从而可能在气溶胶抗结核治疗中应用。

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