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Effect of liquid-to-solid lipid ratio on characterizations of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for transdermal administration
Authors:Aihua Song  Xiaoshu Zhang  Yanting Li  Xinjuan Mao
Affiliation:College of Pharmacy, Shenyang Pharmaceutical University, Shenyang, PR China
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, 78%, >35, and >240?μg/cm2, respectively, however, for SLNs were 280?nm,??29.11?mV, 63.2%, 32.54, and 225.9?μg/cm2, 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/cm2 (25?°C) and 184.4?μg/cm2 (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.
Keywords:Flurbiprofen  nanostructured lipid carriers  solid lipid nanoparticles  stability  transdermal
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