1-Laurin-3-Palmitin as a Novel Matrix of Solid Lipid Particles: Higher Loading Capacity of Thymol and Better Stability of Dispersions Than Those of Glyceryl Monostearate and Glyceryl Tripalmitate.

Hao Shi,Weinong Zhang,Qixin Zhong,Lijuan Han,Shuangshuang Huang,Junbo He

doi:10.3390/nano9040489

Hao Shi, Weinong Zhang + Show 4 more

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https://doi.org/10.3390/nano9040489

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Abstract

To develop solid lipid nanoparticles (SLNs) with a new lipid matrix for delivery of hydrophobic bioactive molecules, high purity 1-laurin-3-palmitin (1,3-LP) was synthesized and the prepared 1,3-LP SLNs were compared with those of two common SLN matrices in glyceryl monostearate (GMS) and glyceryl tripalmitate (PPP). Conditions of preparing SLNs were first optimized by evaluating the particle size, polydispersity index (PDI), zeta-potential, and stability. Thereafter, the performance of SLN loading of a model compound in thymol was studied. The loading capacity of thymol in 1,3-LP SLNs was 16% of lipids and higher than 4% and 12% for GMS- and PPP-SLNs, respectively. The 1,3-LP SLNs also had the best efficiency to entrapment thymol during the prolonged storage. X-ray diffraction (XRD) analyses confirmed the excellent crystalline stability of 1,3-LP leading to the stable entrapment efficiency and better stability of thymol-loaded SLNs. Conversely, the polymorphic transformation of GMS and PPP resulted in the declined entrapment efficiency of thymol in the corresponding SLNs. This work indicated the 1,3-diacylglycerol (DAG) SLNs could be used as a promising delivery system for the encapsulation of hydrophobic bioactive molecules with high loading capacity and stability.

Highlights

Colloidal delivery systems are frequently studied to encapsulate and control the release of bioactive molecules relevant to drugs, agrochemicals, cosmetics, and food [1,2,3]
The present method gives an efficient approach to prepare unsymmetrical 1,3-DAG with good yield and high purity, which can be used as a lipid matrix for fabricating 1,3-DAG solid lipid nanoparticles (SLNs)
The synthesis of high purity 1,3-LP was achieved for use as a solid lipid matrix to prepare SLNs

Summary

Introduction

Colloidal delivery systems are frequently studied to encapsulate and control the release of bioactive molecules relevant to drugs, agrochemicals, cosmetics, and food [1,2,3]. These systems include microemulsions [4], nanoemulsions [5], solid lipid nanoparticles (SLNs) [6], nanogels [7], and nanoliposomes [8]. Solid lipids used in SLN formulations include fatty acids [12], triacylglycerols (TAGs) [13,14,15], monoacylglycerols (MAGs) [16,17], and waxes [18,19]. Novel lipid matrices overcoming this disadvantage are significant to advance the science and technology of SLNs

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