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牛血清白蛋白作为一种纳米载体,用于高效封装疏水性 garcinol-一种用于修饰体外药物释放动力学的策略。

Bovine serum albumin as a nanocarrier for efficient encapsulation of hydrophobic garcinol-A strategy for modifying the in vitro drug release kinetics.

机构信息

Department of Pharmaceutical Technology, Brainware University, Barasat, Kolkata 700125, West Bengal, India; School of Pharmacy, Techno India, University, Saltlake, Sector V, Kolkata 700091, West Bengal, India.

School of Pharmacy, Techno India, University, Saltlake, Sector V, Kolkata 700091, West Bengal, India.

出版信息

Int J Biol Macromol. 2024 Oct;278(Pt 1):134651. doi: 10.1016/j.ijbiomac.2024.134651. Epub 2024 Aug 10.

DOI:10.1016/j.ijbiomac.2024.134651
PMID:39134200
Abstract

Garcinia indica, known as kokum, has been extensively researched for its therapeutic potential. Among the wide variety of phytoconstituents, garcinol is the most efficacious, holding anti-inflammatory, anti-cancer, and anti-diabetic properties. Hydrophobicity and a certain level of toxicity have constrained the drug's application and necessitated a modified dosage form design. The drug has been well explored in the form of extracts but bears very limited application in dosage forms. These prompted in implementation of protein polymers, due to non-toxicity, biocompatibility, and biodegradability. BSA encapsulates the drug, by the desolvation method. The unavailability of past exploration of garcinol with protein polymer accelerated the novelty of this study, to improve the solubility and bioavailability of the drug, modify the drug release kinetics, and ascertain the effectiveness of the NPs to combat inflammation in-vitro. NPs were characterized and satisfactory outcomes were retrieved in terms of all characterizations. The drug release studies depicted a sustained release of up to 85 % over 16 h, ensuring that garcinol can be modulated to give a desired scale of modified release. In vitro cellular uptake studies suggested a substantial uptake of NPs in cell lines and its effectiveness to mitigate inflammation was affirmed by in-vitro anti-inflammatory studies, using ELISA.

摘要

藤黄果,又名罗望果,其药用价值已得到广泛研究。在众多植物成分中,藤黄酚最为有效,具有抗炎、抗癌和抗糖尿病的特性。由于疏水性和一定程度的毒性,限制了该药物的应用,需要对其剂型进行改良设计。该药物已在提取物形式中得到了很好的探索,但在剂型中应用非常有限。这促使人们使用蛋白质聚合物,因为它们具有无毒、生物相容性和可生物降解性。BSA 通过去溶剂化的方法包封药物。由于过去没有用蛋白质聚合物来探索藤黄酚,因此这项研究具有新颖性,旨在提高药物的溶解度和生物利用度,改变药物释放动力学,并确定纳米颗粒在体外对抗炎症的有效性。对 NPs 进行了表征,所有特性的结果都令人满意。药物释放研究表明,在 16 小时内可实现长达 85%的持续释放,确保藤黄酚可以调节至所需的缓释程度。体外细胞摄取研究表明,纳米颗粒在细胞系中有大量摄取,并且通过 ELISA 进行的体外抗炎研究证实了其减轻炎症的有效性。

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