Modification and stabilizing effects of PEG on resveratrol-loaded solid lipid nanoparticles

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• 作者：Jun-Qing Su ; Zhen Wen ; Yi-Ai Wen ; Wan-Ni Xiao…
• 关键词：Solid lipid nanoparticles ; PEG2000 ; Stability ; Resveratrol ; Doping effect ; Steric hindrance
• 刊名：Journal of the Iranian Chemical Society
• 出版年：2016
• 出版时间：May 2016
• 年：2016
• 卷：13
• 期：5
• 页码：881-890
• 全文大小：1,186 KB
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• 作者单位：Jun-Qing Su (1)
  Zhen Wen (1)
  Yi-Ai Wen (1)
  Wan-Ni Xiao (1)
  Jing Lin (1)
  Zong-Kun Zheng (1)
  
  1. College of Chemistry and Chemical Engineering, Shenzhen University, Shenzhen, 518060, Guangdong, China
  
• 刊物主题：Analytical Chemistry; Inorganic Chemistry; Physical Chemistry; Biochemistry, general; Organic Chemistry;
• 出版者：Springer Berlin Heidelberg
• ISSN：1735-2428

文摘

Resveratrol-loaded solid lipid nanoparticles (SLNs) modified by polyethylene glycol (PEG2000) (RES–PEG–SLNs) were prepared to study the stabilizing influences of PEG2000 on SLNs properties including loading capacity, particle size, photostability, and release. The micromorphology, particle size distribution, drug–lipid–modifier interaction and crystalline structure were characterized to elucidate stabilizing effects of PEG2000 on SLNs. Compared with ordinary SLNs, SLNs modified by PEG2000 at relatively low amounts of [m(PEG2000):m(lipids) = 1:10] exhibit high drug loading, steady nanoparticle size distributions, photostability and sustained release. According to characterizations, RES–PEG–SLNs formation is dependent on the physical interactions of drug–lipid–modifier. Since PEG2000 is doped into lipid matrix in a non-crystalline state, the lipids crystalline arrangement is disrupted. Additionally, RES–PEG–SLNs are crystallized in a PEG2000/lipid eutectic mixture rather than a simple mixture, inhibiting the lipid polymorphism transformation from α- to β-form, and therefore preventing drug exclusion from the lipid matrix. The PEG2000/lipid matrix contains lattice defects, which allow for the incorporation of more resveratrol and preventing it from photodegradation effectively. In contrast to the burst release of SLNs modified without PEG2000, resveratrol is released more slowly from the lattice defects in lipid matrix of RES–PEG–SLNs, resulting in a sustained release fitted by a two-stage exponential kinetic equation. PEG2000 is distributed on the RES–PEG–SLNs surface, increasing repulsion between nanoparticles and avoiding particles aggregation. These results confirm that both matrix doping effects and surface steric hindrance produced by the presence of PEG2000 play important roles in maintaining high loadings, nanoparticle size, photostability and sustained release.