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用于口服给药的齐墩果酸和积雪草苷负载固体脂质纳米粒(SLNs)的表征及体外药物释放曲线

Characterisation and In Vitro Drug Release Profiles of Oleanolic Acid- and Asiatic Acid-Loaded Solid Lipid Nanoparticles (SLNs) for Oral Administration.

作者信息

Oboh Michael, Elhassan Eman, Koorbanally Neil Anthony, Govender Laurencia, Siwela Muthulisi, Govender Thirumala, Mkhwanazi Blessing Nkazimulo

机构信息

Discipline of Dietetics and Human Nutrition, School of Agricultural, Earth and Environmental Sciences, College of Agriculture, Engineering and Science, University of KwaZulu-Natal, Pietermaritzburg 3209, South Africa.

Discipline of Pharmaceutical Sciences, School of Health Sciences, College of Health Sciences, University of KwaZulu-Natal, Durban 4001, South Africa.

出版信息

Pharmaceutics. 2025 May 30;17(6):723. doi: 10.3390/pharmaceutics17060723.

DOI:10.3390/pharmaceutics17060723
PMID:40574036
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12196335/
Abstract

This study characterised and evaluated the stability, solubility, and in vitro drug release of OA- and AA-loaded SLNs. The OA- and AA-SLNs were formulated using the emulsion solvent evaporation method and characterised based on particle size (PS), polydispersity index (PDI), zeta potential (ZP), and transmission electron microscopy (TEM). Solubility studies were conducted in PBS (pH 1.2 and 6.8) and dHO using HPLC, while in vitro drug release was assessed in simulated intestinal fluid (SIF) (pH 6.8). The optimised OA-SLNs (1:1 drug-to-lipid ratio) showed PS, PDI, ZP, and EE% values of 312.9 ± 3.617 nm, 0.157 ± 0.014, -17.0 ± 0.513 mV, and 86.54 ± 1.818%, respectively. The optimised AA-SLNs (1:2 drug-to-lipid: ratio) had a PS of 115.5 ± 0.458 nm, PDI of 0.255 ± 0.007, ZP of -11.9 ± 0.321 mV, and EE% of 76.22 ± 0.436%. The SLNs remained stable for 60 days at 4 °C and room temperature ( < 0.05). The solubility study revealed that free OA and AA showed no measurable values in the three solvents. However, OA-SLNs showed the highest solubility in HO (16-fold) followed by PBS at pH 6.8 (10-fold) and pH 1.2 (10-fold). AA-SLNs significantly improved the solubility in PBS at pH 6.8 (88-fold), compared to dHO (6-fold) and PBS at pH 1.2 (26-fold). In vitro drug release studies showed that OA release from the SLNs was significantly increased within 300 min ( < 0.05) compared to the free drug. Similarly, AA release from the SLNs was significantly increased within 300 min ( < 0.05) compared to free AA. These results demonstrate that SLNs enhance OA and AA solubility and drug release, suggesting a promising strategy for improving oral bioavailability and therapeutic efficacy.

摘要

本研究对负载油酸(OA)和花生四烯酸(AA)的固体脂质纳米粒(SLNs)的稳定性、溶解性及体外药物释放进行了表征和评估。采用乳化溶剂蒸发法制备OA - SLNs和AA - SLNs,并基于粒径(PS)、多分散指数(PDI)、zeta电位(ZP)和透射电子显微镜(TEM)对其进行表征。使用高效液相色谱法(HPLC)在磷酸盐缓冲液(PBS,pH 1.2和6.8)和去离子水(dHO)中进行溶解度研究,同时在模拟肠液(SIF,pH 6.8)中评估体外药物释放。优化后的OA - SLNs(药物与脂质比例为1:1)的PS、PDI、ZP和包封率(EE%)值分别为312.9±3.617 nm、0.157±0.014、 - 17.0±0.513 mV和86.54±1.818%。优化后的AA - SLNs(药物与脂质比例为1:2)的PS为115.5±0.458 nm,PDI为0.255±0.007,ZP为 - 11.9±0.321 mV,EE%为76.22±0.436%。SLNs在4℃和室温下可稳定保存60天(P<0.05)。溶解度研究表明,游离的OA和AA在三种溶剂中均无可测量的值。然而,OA - SLNs在去离子水中的溶解度最高(16倍),其次是pH 6.8的PBS(10倍)和pH 1.2的PBS(10倍)。与去离子水(6倍)和pH 1.2的PBS(26倍)相比,AA - SLNs在pH 6.8的PBS中的溶解度显著提高(88倍)。体外药物释放研究表明,与游离药物相比,OA从SLNs中的释放在300分钟内显著增加(P<0.05)。同样,与游离AA相比,AA从SLNs中的释放在300分钟内显著增加(P<0.05)。这些结果表明,SLNs可提高OA和AA的溶解度及药物释放,提示这是一种改善口服生物利用度和治疗效果的有前景策略。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/21b70ddc4283/pharmaceutics-17-00723-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/dcb858a11e2d/pharmaceutics-17-00723-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/2f19fd10a7c9/pharmaceutics-17-00723-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/987f34443920/pharmaceutics-17-00723-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/bb909a8272c9/pharmaceutics-17-00723-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/c4d95f1fd340/pharmaceutics-17-00723-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/5343f1cd396d/pharmaceutics-17-00723-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/21b70ddc4283/pharmaceutics-17-00723-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/dcb858a11e2d/pharmaceutics-17-00723-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/2f19fd10a7c9/pharmaceutics-17-00723-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/987f34443920/pharmaceutics-17-00723-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/bb909a8272c9/pharmaceutics-17-00723-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/c4d95f1fd340/pharmaceutics-17-00723-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/5343f1cd396d/pharmaceutics-17-00723-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fb9f/12196335/21b70ddc4283/pharmaceutics-17-00723-g007.jpg

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