Spray drying of fenofibrate loaded nanostructured lipid carriers

Spray drying of fenofibrate loaded nanostructured lipid carriers
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负载非诺贝特的纳米结构脂质载体的喷雾干燥

DOI:
10.1016/j.ajps.2016.01.001
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发表时间:
2016-08
影响因子:
10.2
通讯作者:
Mingshi Yang
Mingshi Yang
中科院分区:
医学1区
文献类型:
--
作者:
Dengning Xia;Neha Shrestha;Jacco van de Streek;Huiling Mu;Mingshi Yang

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通过喷雾干燥将纳米结构脂质载体的水分散体转化为干粉,可以使纳米结构脂质载体具有比水分散体更好的物理化学稳定性。在本研究中,采用喷雾干燥法将含有非诺贝特的NLC水相分散体转化为干燥、易重构的粉末。采用中心复合面心设计(CCFD)研究了油脂与保护剂(甘露醇和海藻糖)的比例以及喷雾干粉的结晶度对喷雾干粉粒度、得率和残留水分含量的影响。甘露醇与海藻糖的比例在3:7 ~ 10:0 (w/w)范围内与喷雾干粉结晶含量呈线性关系(R2= 0.9915)。使用甘露醇和海藻糖混合物对NLC水分散体进行喷雾干燥,与初始水分散体相比,NLC在水中重构后的粒径增加。通过降低甘露醇与海藻糖的比例来降低干粉的结晶度,可以改善ncs在水中的重构。随着甘露醇与海藻糖比例的增加,干粉的产率和残余水分含量降低。在喷雾干燥后,脂质纳米颗粒能够保持药物掺入和延长药物释放时间。实验模型具有较强的鲁棒性,表明喷雾干燥是一种可行的将NLCs转化为干粉的技术。
The conversion of aqueous dispersion of nanostructured lipid carriers (NLCs) into dry powder by spray drying could be a useful approach to render NLCs with better physical chemical stability than the aqueous dispersion. In this study, aqueous NLC dispersion containing fenofibrate was converted into dry, easily reconstitutable powder using spray drying. A central composite face centered design (CCFD) was used to investigate the influence of the ratio of lipid to protectant (mannitol and trehalose) and crystallinity of spray-dried powder on the particle size, yield and residual moisture content of the dried powder. A linear relationship (R2= 0.9915) was established between the crystalline content of the spray-dried powders against the ratio of mannitol to trehalose from 3:7 to 10:0 (w/w). Spray drying of NLC aqueous dispersion using a mannitol and trehalose mixture resulted in an increase in particle size of the NLCs after reconstitution in water as compared to that in the initial aqueous dispersion. The decrease in crystallinity of the dry powder by reducing the ratio of mannitol to trehalose could improve the reconstitution of the NLCs in water. However the yield and residual moisture content of dry powder decreased with an increase in the ratio of mannitol to trehalose. Lipid nanoparticles were able to retain the drug incorporation and the prolonged drug release profile after spray drying. The experimental model was robust, and suggested that spray drying is a viable technique for the conversion of NLCs into dry powder.
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