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Encapsulation of retinods in solid lipid nanoparticles (SLN)

机译:固体脂质纳米颗粒中的视网膜(SLN)的封装

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摘要

SLN have been suggested for a broad range of applications, such as intravenous iniection, peroral, or dermal administration. The incorporation of the drug in the core of the SLN has to be ensured for these applications, but the inclusion of drugs in SLN is poorly understood. This study is a contribution to further describe the inclusion properties of colloidal lipids and to propose incorporation mechanisms. Besides the well known methods to investigate entrapment of actives in nanoparticles such as DSC or microscopy, the present study focussed on vet a different approach. Based on the different chemical stability of retinoids in water and in a lipid phase, a method to derive information on the distribution of the drug between SLN-lipid and the water phase was established. Compar-ing different lipids, glyceryl behenate gave superior entrapment compared to tripalmitate, cetyl palmitate and solid paraffin. Comparing three different drugs, entrapment increased with decreasing polarity of the molecule (treti-noin < retinol < retinyl palmitate). The encapsulation efficacy was successfully enhanced by formulating SLN from mixtures of liquid and solid lipids. These particles were solid and provided better protection of the sensitive drugs than an emulsion. X-ray investigations revealed that good encapsulation correlated with a low degree of crystallinity and lattice defects. With highly ordered crystals, as in the case of cetyl palmitate, drug expulsion from the carrier was more pronounced.
机译:已经提出了广泛的应用,例如静脉内嗜族或皮肤给药。必须确保这些应用的SLN核心中的药物掺入,但是在SLN中包含药物的含量很差。该研究是进一步描述胶体脂质的包涵性和提出掺入机制的贡献。除了众所周知的方法,以研究纳米颗粒(如DSC或显微镜)在纳米颗粒中的夹带,本研究侧重于VET不同的方法。基于水和脂质阶段在水中的不同化学稳定性,建立了一种衍生关于SLN-脂质和水相之间药物分布信息的方法。比较不同的脂质,甘油糖蛋白与三萜酸盐,甘乙酰棕榈酸酯和固体石蜡相比,珍珠酸脱衣。比较三种不同的药物,随着分子的极性降低而增加(Treti-Noin

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