牛血清白蛋白作为纳米载体,用于有效封装疏水性山竹醇-A策略,以改变体外药物释放动力学。
Bovine serum albumin as a nanocarrier for efficient encapsulation of hydrophobic garcinol-A strategy for modifying the in vitro drug release kinetics.
发表日期:2024 Aug 10
作者:
Shayeri Chatterjee Ganguly, Beduin Mahanti, Soumya Ganguly, Subhabrota Majumdar
来源:
Int J Biol Macromol
摘要:
藤黄果(Garcinia indica),又名 kokum,因其治疗潜力而被广泛研究。在多种植物成分中,山竹酚是最有效的,具有抗炎、抗癌和抗糖尿病特性。疏水性和一定程度的毒性限制了该药物的应用,需要修改剂型设计。该药物以提取物的形式得到了很好的探索,但在剂型方面的应用非常有限。由于无毒、生物相容性和生物可降解性,这些促使蛋白质聚合物的应用。 BSA 通过去溶剂化方法封装药物。过去对藤黄酚与蛋白质聚合物的探索的不可用性加速了这项研究的新颖性,以提高药物的溶解度和生物利用度,改变药物释放动力学,并确定纳米粒子对抗体外炎症的有效性。对 NP 进行了表征,并在所有表征方面均获得了满意的结果。药物释放研究表明,在 16 小时内持续释放高达 85%,确保可以调节山楂醇以达到所需的修饰释放规模。体外细胞摄取研究表明,细胞系中纳米粒子大量摄取,并且使用 ELISA 进行的体外抗炎研究证实了其减轻炎症的有效性。版权所有 © 2024 Elsevier B.V. 保留所有权利。
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.Copyright © 2024 Elsevier B.V. All rights reserved.