Nanocochleate-based delivery of quercetin with enhanced therapeutic potential: formulation, cytotoxicity and pharmacokinetics study

IF 3.4 Q2 PHARMACOLOGY & PHARMACY Future Journal of Pharmaceutical Sciences Pub Date : 2024-11-21 DOI:10.1186/s43094-024-00732-z

Harshad S. Kapare, Nagesh Patil, Mayuri Bhosale, Deepak Kulkarni, Ritesh Bhole

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Abstract

Background

Quercetin has well-proven anticancer potential through various mechanisms, but its applications in drug delivery are limited due to poor biopharmaceutical properties. The present study was aimed to formulate quercetin nanocochleates (QNC) in order to overcome these limitations. QNC formulation was fabricated by a trapping method, optimized and evaluated for various formulation aspects, in vitro cytotoxicity and pharmacokinetic parameters.

Result

Developed nanocochleates possess particle size and encapsulation efficiency of 205.6 ± 2.55 nm and 76.36 ± 0.88%, respectively. In vitro cytotoxicity study performed using MCF-7 cell lines revealed the comparative efficiency of QNC over pure quercetin. Total growth inhibition concentration (TGI) for pure quercetin was 96.73 μg/ml, while for QNC it was 83.29 μg/ml. Pharmacokinetic study results showed improvement in Cmax and AUC after QNC formulation with increased Tmax showing sustained release.

Conclusion

Overall, the developed QNC formulation markedly improved cytotoxic potential and biopharmaceutical aspects.

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基于纳米絮凝剂的槲皮素递送具有更高的治疗潜力：配方、细胞毒性和药代动力学研究

背景槲皮素通过各种机制被证实具有抗癌潜力，但由于其生物制药特性较差，其在给药方面的应用受到限制。本研究旨在制备槲皮素纳米絮凝物（QNC），以克服这些局限性。采用捕集法制备了 QNC 制剂，并对制剂的各个方面、体外细胞毒性和药代动力学参数进行了优化和评估。利用 MCF-7 细胞系进行的体外细胞毒性研究表明，QNC 比纯槲皮素更有效。纯槲皮素的总生长抑制浓度（TGI）为 96.73 μg/ml，而 QNC 为 83.29 μg/ml。药代动力学研究结果表明，QNC 制剂的 Cmax 和 AUC 均有所改善，Tmax 增加，显示出持续释放。

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来源期刊

Future Journal of Pharmaceutical Sciences PHARMACOLOGY & PHARMACY-

自引率

0.00%

发文量

审稿时长

23 weeks

期刊介绍： Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.