title: Effect of liquid-to-solid lipid ratio on characterizations of flurbiprofen-loaded solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) for transdermal administration.
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.
authors.affiliation: a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.
authors.forename: Aihua
authors.initials: A
authors.lastname: Song
authors.affiliation: a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.
authors.forename: Xiaoshu
authors.initials: X
authors.lastname: Zhang
authors.affiliation: a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.
authors.forename: Yanting
authors.initials: Y
authors.lastname: Li
authors.affiliation: a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.
authors.forename: Xinjuan
authors.initials: X
authors.lastname: Mao
authors.affiliation: a College of Pharmacy, Shenyang Pharmaceutical University , Shenyang , PR China.
authors.forename: Fei
authors.initials: F
authors.lastname: Han
mesh_terms: D000279:Administration, Cutaneous; D000818:Animals; D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D005480:Flurbiprofen / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017208:Rats, Wistar; D012867:Skin / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D008055:Lipids; D005480:Flurbiprofen
keywords: Flurbiprofen; nanostructured lipid carriers; solid lipid nanoparticles; stability; transdermal