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橙皮素及其新型制剂在KB细胞中的抗氧化和抗癌活性。

Antioxidant and anticancer activities of hesperetin and its novel formulations in KB cells.

作者信息

Chauhan Arunima, Shedgaonkar Gayatri Gopal, Kumar Lalit, Karmakar Arka, Khajuria Salil, Raghavendra Archana Parampalli, Verma Ruchi

机构信息

Faculty of Dentistry, Melaka-Manipal Medical College, Manipal Academy of Higher Education, Manipal, India.

Faculty of Dentistry, Manipal University College Malaysia, Jalan Batu Hampar, Bukit Baru, Melaka, Malaysia.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2025 May;398(5):5213-5236. doi: 10.1007/s00210-024-03581-y. Epub 2024 Nov 12.

Abstract

This study aimed to formulate the hesperetin nanostructured lipid carriers (NLCs) containing oro-mucosal gel for its activity assessment on the KB cell line. NLCs were prepared with glyceryl monostearate, oleic acid, and lecithin using a modified constant-temperature emulsification technique. The particle size analysis, in vitro drug release studies, etc., of prepared NLCs were evaluated. The formulated gels were analyzed with respect to spreadability, extrudability, swelling index, texture analysis, etc. The particle size, polydispersity index, zeta potential, and drug entrapment of nanocarriers were recorded to be 221.733 ± 61.536 nm, 0.381 ± 0.091, - 51.433 ± 4.143 mV, and 89.29%, respectively. The optimized NLCs in 24 h released 87.14 ± 6.62% of the drug. The round shape of NLCs was noticed with scanning electron microscopy. The pH, spreadability, extrudability, swelling index, content uniformity, and drug release studies of hesperetin NLCs-containing gel (HNG) were found to be 6.81 ± 0.04, 2.49 ± 0.04 cm.mg/s, 539.04 ± 32.88 g/cm, 4.27 ± 0.47, 107.98 ± 1.93%, and 90.17 ± 6.67% (in 48 h), respectively. The developed formulations showed promising in vitro anticancer and antioxidant activities. HNP results authorize that the formulation may be beneficial for the treatment of oral cancer.

摘要

本研究旨在制备含橙皮素的纳米结构脂质载体(NLCs)口腔黏膜凝胶,并对其在KB细胞系上的活性进行评估。采用改良的恒温乳化技术,以单硬脂酸甘油酯、油酸和卵磷脂制备NLCs。对制备的NLCs进行粒径分析、体外药物释放研究等评估。对所制备的凝胶进行铺展性、挤出性、溶胀指数、质地分析等方面的分析。纳米载体的粒径、多分散指数、zeta电位和药物包封率分别记录为221.733±61.536nm、0.381±0.091、-51.433±4.143mV和89.29%。优化后的NLCs在24小时内释放了87.14±6.62%的药物。通过扫描电子显微镜观察到NLCs呈圆形。含橙皮素NLCs的凝胶(HNG)的pH值、铺展性、挤出性、溶胀指数、含量均匀度和药物释放研究结果分别为6.81±0.04、2.49±0.04cm.mg/s、539.04±32.88g/cm、4.27±0.47、107.98±1.93%和90.17±6.67%(48小时)。所开发的制剂显示出有前景的体外抗癌和抗氧化活性。HNP结果表明该制剂可能对口腔癌的治疗有益。

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