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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Formulation and in vitro evaluation of buoyant controlled release lercanidipine lipospheres
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Formulation and in vitro evaluation of buoyant controlled release lercanidipine lipospheres

机译：浮力控释乐卡地平脂质体的制备及体外评价

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The aim of this study was to prepare and evaluate buoyant lipospheres containing lercanidipine hydrochloride. The lipospheres were prepared by modified melt dispersion technique using hydrophobic matrix of cetostearyl alcohol (CSA). The influence of formulation factors (stirring speed, lipid:drug ratio, lipid:-surfactant polymer composition) on particle size, encapsulation efficiency and in-vitro release characteristics of lipospheres were investigated. The yields of all prepared formulation and encapsulation efficiencies were high for formulations which contain high lipid amount. The mean particle size significantly decreased (p < 0.001) by increasing the lipid:surfactant polymer and stirring speed (p < 0.001) of the system. Reduction in encapsulation efficiency (p < 0.001) and drug content (p < 0.001) was observed with increasing stirring speed and percentage of poloxamer 407 in formulation. Although lercanidipine hydrochloride release from Cetostearyl alcohol lipospheres were very slow and incomplete for all formulations f1-f6 (~65% drug released in 12 h) and was increased (~85% drug released in 12 h) in lipospheres formulations f7-f12, containing Poloxamer 407. Percentage of buoyant lercanidipine lipospheres of CSA (96-100% buoyancy up to 12h) decreases (p < 0.001) with increasing percentage of poloxamer 407 and achieved the release profile suitable for peroral administration.
机译：这项研究的目的是准备和评估含有盐酸乐卡地平的漂浮性脂球。通过使用鲸蜡硬脂醇（CSA）的疏水性基质通过改进的熔融分散技术制备脂质体。研究了制剂因素（搅拌速度，脂质：药物比，脂质：表面活性剂聚合物组成）对脂质体粒径，包封效率和体外释放特性的影响。对于包含高脂质量的制剂，所有制备的制剂的产率和包封效率均很高。通过增加脂质：表面活性剂聚合物和系统的搅拌速度（p <0.001），平均粒径显着降低（p <0.001）。随着搅拌速度和制剂中泊洛沙姆407百分比的增加，观察到包封效率（p <0.001）和药物含量（p <0.001）降低。尽管从鲸蜡硬脂醇醇脂球中盐酸盐酸勒卡地平释放非常缓慢且不完全，但对于所有制剂f1-f6（在12小时内释放约65％的药物），并在脂质球制剂f7-f12中增加（在12 h释放约85％的药物），其中泊洛沙姆407。随着泊洛沙姆407百分比的增加，CSA的可乐乐加地平脂球（96％至100％的浮力）的百分比随泊洛沙姆407百分比的增加而降低（p <0.001），并获得了适合口服给药的释放曲线。

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