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载大麻二酚的纳米结构脂质载体:优化、表征与稳定性

CBD-Loaded Nanostructured Lipid Carriers: Optimization, Characterization, and Stability.

作者信息

Xie Yang, Li Peng, Fu Dong, Yang Fan, Sui Xin, Huang Bo, Liu Jiaying, Chi Jialong

机构信息

Heilongjiang Academy of Sciences, Institute of Advanced Technology, Harbin 150020, China.

出版信息

ACS Omega. 2024 Sep 19;9(39):40632-40643. doi: 10.1021/acsomega.4c04771. eCollection 2024 Oct 1.

Abstract

Cannabidiol (CBD) has demonstrated its potential to enhance depression treatment through various biological pathways. However, the application potential of CBD is significantly impeded by its polymorphic nature, limited water solubility, and hepatic first-pass metabolism. To improve chemical stability and water solubility, nanostructured lipid carriers loaded with CBD (CBD-NLCs) were developed using a hot-melt emulsification method and optimized by response surface methodology (RSM). The process parameters were optimized using a four-factor and three-level Box-Behnken experimental design consisting of 29 experiments. The CBD-NLCs were formulated and characterized, demonstrating desirable properties, including a mean particle size of 54.33 nm, a PDI value of 0.118, a zeta potential of -29.7 mV, and an impressive encapsulation efficiency rate of 87.58%. The nanoparticles were found to possess an approximately spherical shape, as revealed by scanning and transmission electron microscopy. The stability studies have demonstrated that CBD-NLCs effectively mitigated the photodegradation of CBD and exhibited a stable behavior for 42 days when stored. The CBD-NLCs displayed a biphasic release profile characterized by an initial burst release (over 50% of CBD released within 20 min) followed by a subsequent gradual and sustained release, aligned with first-order kinetics and Fickian diffusion. These findings demonstrate the potential suitability of this formulation as a carrier for CBD in food fortification and pharmaceutical applications.

摘要

大麻二酚(CBD)已通过多种生物学途径展现出增强抑郁症治疗效果的潜力。然而,CBD的多晶型性质、有限的水溶性和肝脏首过代谢显著阻碍了其应用潜力。为提高化学稳定性和水溶性,采用热熔乳化法制备了负载CBD的纳米结构脂质载体(CBD-NLCs),并通过响应面法(RSM)进行优化。使用由29个实验组成的四因素三水平Box-Behnken实验设计对工艺参数进行优化。对CBD-NLCs进行了配方和表征,结果显示其具有理想的性能,包括平均粒径为54.33 nm、多分散指数(PDI)值为0.118、zeta电位为-29.7 mV以及令人印象深刻的87.58%的包封率。扫描电子显微镜和透射电子显微镜显示,纳米颗粒呈近似球形。稳定性研究表明,CBD-NLCs有效减轻了CBD的光降解,储存42天时表现出稳定的性能。CBD-NLCs呈现出双相释放曲线,其特征是初始突释(20分钟内释放超过50%的CBD),随后是逐渐的持续释放,符合一级动力学和菲克扩散。这些发现表明该制剂作为CBD在食品强化和药物应用中的载体具有潜在的适用性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/930e/11447858/fcd4e2eb37a7/ao4c04771_0001.jpg

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