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液固脂质比对用于透皮给药的氟比洛芬固体脂质纳米粒(SLNs)和纳米结构脂质载体(NLCs)特性的影响。

Effect of liquid-to-solid lipid ratio on characterizations of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for transdermal administration.

作者信息

Song Aihua, Zhang Xiaoshu, Li Yanting, Mao Xinjuan, Han Fei

机构信息

a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.

出版信息

Drug Dev Ind Pharm. 2016 Aug;42(8):1308-14. doi: 10.3109/03639045.2015.1132226. Epub 2016 Jan 20.

Abstract

The aim of this study is to evaluate the effect of liquid-to-solid lipid ratio on properties of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs), and to clarify the superiority of NLCs over SLNs for transdermal administration. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, differential scanning calorimetry, X-ray diffractometry, in vitro percutaneous permeation profile, and stability of SLNs and NLCs were compared. Particle size, zeta potential, drug encapsulation efficiency, in vitro occlusion factor, and in vitro percutaneous permeation amount of the developed NLCs were all <200 nm, < -20 mV, >78%, >35, and >240 μg/cm(2), respectively, however, for SLNs were 280 nm, -29.11 mV, 63.2%, 32.54, and 225.9 μg/cm(2), respectively. After 3 months storage at 4 °C and 25 °C, almost no significant differences between the evaluated parameters of NLCs were observed. However, for SLNs, particle size was increased to higher than 300 nm (4 °C and 25 °C), drug encapsulation efficiency was decreased to 51.2 (25 °C), in vitro occlusion factor was also decreased to lower than 25 (4 °C and 25 °C), and the cumulative amount was decreased to 148.9 μg/cm(2) (25 °C) and 184.4 μg/cm(2) (4 °C), respectively. And DSC and XRD studies indicated that not only the crystalline peaks of the encapsulated flurbiprofen disappeared but also obvious difference between samples and bulk Compritol® ATO 888 was seen. It could be concluded that liquid-to-solid lipid ratio has significant impact on the properties of SLNs and NLCs, and NLCs showed better stability than SLNs. Therefore, NLCs might be a better option than SLNs for transdermal administration.

摘要

本研究旨在评估液固脂质比对氟比洛芬固体脂质纳米粒(SLNs)和纳米结构脂质载体(NLCs)性质的影响,并阐明NLCs在经皮给药方面优于SLNs的优势。比较了SLNs和NLCs的粒径、zeta电位、药物包封率、体外封闭因子、差示扫描量热法、X射线衍射法、体外经皮渗透曲线以及稳定性。所制备的NLCs的粒径、zeta电位、药物包封率、体外封闭因子和体外经皮渗透量分别均<200 nm、<-20 mV、>78%、>35和>240 μg/cm²,然而,SLNs的分别为280 nm、-29.11 mV、63.2%、32.54和225.9 μg/cm²。在4°C和25°C储存3个月后,未观察到NLCs评估参数之间有明显差异。然而,对于SLNs,粒径增加到高于300 nm(4°C和25°C),药物包封率降至51.2(25°C),体外封闭因子也降至低于25(4°C和25°C),累积量分别降至148.9 μg/cm²(25°C)和184.4 μg/cm²(4°C)。差示扫描量热法(DSC)和X射线衍射(XRD)研究表明,不仅包封的氟比洛芬的结晶峰消失,而且样品与Compritol® ATO 888原料药之间也存在明显差异。可以得出结论,液固脂质比对SLNs和NLCs的性质有显著影响,且NLCs显示出比SLNs更好的稳定性。因此,对于经皮给药,NLCs可能是比SLNs更好的选择。

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