Nanostructure of DiR-Loaded Solid Lipid Nanoparticles with Potential Bioimaging Functions

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Brief/Technical Note Nanostructure of DiR-Loaded Solid Lipid Nanoparticles with Potential Bioimaging Functions Lei Shu,1 Fangqin Fu,2 Zhengwei Huang,2,4 Ying Huang,2 Ping Hu,2 and Xin Pan3,4

Received 24 August 2020; accepted 8 October 2020 Abstract. The fluorescence dye-loaded nanoparticles are widely used as bioimaging agents in the field of nanotheranostics. However, the nanoparticles for nanotheranostics usually consist of synthetic materials, such as metal, silica, and organic polymers, which are often biologically incompatible and may arouse toxicity issues. Herein, the potential of nearinfrared probe DiR-containing solid lipid nanoparticle suspensions (DiR-SLNS) as the bioimaging agent, which was prepared by lipids and surfactants with excellent biocompatibility, was investigated in this study. The nanostructure of DIR-SLNS system and the distribution of DiR were studied by dissipative particle dynamics (DPD) simulations. The stability of physicochemical properties and fluorescence spectra of DIR-SLNS system were investigated using dynamic laser scattering (DLS), nanoparticle tracking analysis (NTA), and fluorescence spectra. The fluorescence intensity-concentration correlation of DIR-SLNS was also evaluated. As a result, DiR-SLNS demonstrated a “core-shell”-like nanostructure and DiR was mainly distributed in the cetyl palmitate (CP) core rather than the surface of SLNS, which was beneficial to its potential applications in bioimaging. DiR-SLNS exhibited remarkable physicochemical stability as the nanoparticles maintained ~ 90% fluorescence intensity during the 10-day storage time. The correlation between fluorescence intensity and concentration was established and validated using a linear regression model. This study proposed a type of promising candidates in nano-scale with higher safety and fluorescence stability for bioimaging. KEY WORDS: solid lipid nanoparticle; bioimaging; DiR; nanostructure.

In recent years, the cooperation of nanotechnology and theranostics gives birth to the new concept “nanotheranostics” (1). Generally, nanotheranostics refers to using nanoparticles as the contrast agent for bioimaging. The nanoparticles per se or the payload can emit detectable signals with high signal-to-noise ratios. Along with the welldeveloped fluorescence bioimaging techniques, a convenient and widely applied method to achieve nanotheranostics is to prepare fluorescence dye-loaded nanoparticles (2). Recently, nanosafety has become a public concern for the

Lei Shu and Fangqin Fu are regarded as co-first authors. Electronic supplementary material The online version of this article (https://doi.org/10.1208/s12249-020-01847-1) contains supplementary material, which is available to authorized users. 1

Guangzhou Novaken Pharmaceutical Co., Ltd., Guangzhou, 510006, People’s Republic of China. 2 College of Pharmacy, Jinan University, Guangzhou, 510632, People’s Republic of China. 3 School of Pharmaceutical Sciences, Sun Yat-Sen University, Guangzhou, 510006, Guangdong, People’s Republic of China. 4 To whom correspondence sh