School of Pharmacy, Anhui University of Chinese Medicine, Hefei, PR China.
Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, PR China.
Pharm Dev Technol. 2022 Dec;27(10):1038-1048. doi: 10.1080/10837450.2022.2147542. Epub 2022 Nov 24.
The purpose of this experiment was to explore the effect of Solid lipid nanoparticles (SLNs) on improving the oral absorption and bioavailability of cinnamaldehyde (CA).
CA-SLNs were prepared by high-pressure homogenization and characterized by particle size, entrapment efficiency, and morphology, thermal behavior and attenuated total reflection Fourier transform infrared (ATR-FTIR). characteristics of release, stability experiments, cytotoxicity, uptake and transport across Caco-2 cell monolayer of CA-SLNs were studied as well. In addition, CA-SLNs underwent pharmacokinetic and gastrointestinal mucosal irritation studies in rats.
CA-SLNs exhibited a spherical shape with a particle size of 44.57 ± 0.27 nm, zeta potential of -27.66 ± 1.9 mV and entrapment efficiency of 83.63% ± 2.16%. Differential scanning calorimetry (DSC) and ATR-FTIR confirmed that CA was well encapsulated. release of CA-SLNs displayed that most of the drug (90.77% ± 5%) was released in the phosphate buffer, and only a small amount of drug (18.55% ± 5%) was released in the HCl buffer. CA-SLNs were taken up by an energy-dependent, endocytic mechanism mediated by caveolae mediated endocytosis across Caco-2 cells. The CA permeation through Caco-2 cell was facilitated by CA-SLNs. The outcome of the gastrointestinal irritation test demonstrated that CA-SLNs had no irritation to the rats' intestines. Compared with CA dispersions, incorporation of SLNs increased the oral bioavailability of CA more than 1.69-fold.
It was concluded that CA-SLNs improved the absorption across Caco-2 cell model and improved the oral administration bioavailability of CA in rats.
本实验旨在探讨固体脂质纳米粒（SLNs）对改善肉桂醛（CA）口服吸收和生物利用度的作用。
采用高压匀质法制备 CA-SLNs，通过粒径、包封率、形态、热行为和衰减全反射傅里叶变换红外光谱（ATR-FTIR）对其进行表征。研究了 CA-SLNs 的释放特性、稳定性实验、细胞毒性、Caco-2 细胞单层摄取和转运特性。此外，还对 CA-SLNs 在大鼠体内的药代动力学和胃肠道黏膜刺激性进行了研究。
CA-SLNs 呈球形，粒径为 44.57±0.27nm，Zeta 电位为-27.66±1.9mV，包封率为 83.63%±2.16%。差示扫描量热法（DSC）和 ATR-FTIR 证实 CA 被很好地包封。CA-SLNs 的释放研究表明，大部分药物（90.77%±5%）在磷酸盐缓冲液中释放，只有少量药物（18.55%±5%）在 HCl 缓冲液中释放。CA-SLNs 通过能量依赖的、网格蛋白介导的内吞作用被 Caco-2 细胞摄取。CA-SLNs 促进了 CA 通过 Caco-2 细胞的渗透。胃肠道刺激性试验的结果表明，CA-SLNs 对大鼠肠道无刺激性。与 CA 分散体相比，SLNs 的加入使 CA 的口服生物利用度提高了 1.69 倍以上。
CA-SLNs 改善了 Caco-2 细胞模型的吸收，并提高了 CA 在大鼠体内的口服生物利用度。
