Purpose

Macromolecules are important in polymer-based drug delivery systems as they help in specific targeting. This study explores the use of guggul gum (GG) and chitosan (Ch) in encapsulating boswellic acid (BA) which has high first-pass metabolism and low aqueous solubility for possible uses in inflammatory conditions.

Methods

Ionic complexation was used for nanoparticle formulation. The contents of guggul gum, chitosan, and boswellic acid were taken as independent variables, and their influence on encapsulation, particle size, and polydispersity were optimized by using Box-Behnken design. The developed formulation was assessed for drug release (in vitro) and release kinetics, stability, and preclinical pharmacokinetics. The formulation was also evaluated for inhibition of carrageenan-induced hind paw inflammation in rats.

Results

The nanoparticles were successfully prepared by ionic complexation method. The runs suggested by the design yielded a quadratic model for predicting the relationship between independent variables and responses. The optimum condition suggested by point prediction tool yielded spherical nanoparticles with 81.7% encapsulation, drug loading 21.2%, 377.19 nm size, and 0.201 PDI. The nanoparticles showed zero-order kinetics demonstrating an amalgamation of drug diffusion through matrix and erosion of polymeric medium.

Conclusion

Ionic complexation is a suitable method for nanopartile formulation. GG-Ch nanoparticles are beneficial for specific delivery and anti-inflammation of boswellic acid. The bioavailability of boswellic acid was increased by 11.38 times when given as a GG-Ch nanoparticle. The nanoparticles were stable at 25 °C for 6 months.

中文翻译：

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基于Box-Behnken实验设计的乳香酸壳聚糖-古古尔胶纳米颗粒的优化及药代动力学研究

目的

大分子在基于聚合物的药物输送系统中非常重要，因为它们有助于特定的靶向。这项研究探索了古吉尔胶（GG）和壳聚糖（Ch）在封装乳香酸（BA）中的用途，该乳香具有高首过代谢和低水溶性，可用于炎症性疾病。

方法

离子络合用于纳米颗粒制剂。以古吉尔胶，壳聚糖和乳香酸的含量为自变量，并通过Box-Behnken设计优化了它们对包封，粒径和多分散性的影响。评价开发的制剂的药物释放（体外）以及释放动力学，稳定性和临床前药代动力学。还评估了该制剂对角叉菜胶诱导的大鼠后爪炎症的抑制作用。

结果

通过离子络合法成功制备了纳米颗粒。设计建议的运行产生了一个用于预测自变量与响应之间关系的二次模型。点预测工具建议的最佳条件是球形纳米颗粒的包封率为81.7％，载药量为21.2％，粒径为377.19 nm，PDI为0.201。纳米粒子表现出零级动力学，表明药物通过基质的扩散和聚合介质的侵蚀而合并。

结论

离子络合是用于纳米颗粒制剂的合适方法。GG-Ch纳米颗粒有利于乳香酸的特异性递送和抗发炎。当以GG-Ch纳米颗粒形式提供时，乳香酸的生物利用度提高了11.38倍。纳米颗粒在25℃下稳定6个月。