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设计负载菠萝蛋白酶的肠溶纳米制剂对其口服给药后的稳定性和抗炎潜力的影响。

Implications of designing a bromelain loaded enteric nanoformulation on its stability and anti-inflammatory potential upon oral administration.

作者信息

Sharma Manu, Sharma Rishu

机构信息

Department of Pharmacy, Banasthali Vidyapith Banasthali Rajasthan India-304022

出版信息

RSC Adv. 2018 Jan 11;8(5):2541-2551. doi: 10.1039/c7ra13555f. eCollection 2018 Jan 9.

Abstract

The objective of the present investigation was to develop an enteric nano-formulation of bromelain to improve its stability and anti-inflammatory potential. Bromelain loaded nanoparticles (Br-NPs) were developed using a Eudragit L 100 polymer by a double emulsion solvent evaporation method to obtain gastro-resistant properties. Br-NPs were characterized for particle size (248.89 ± 22.76 nm), zeta potential (-27.34 ± 2.17 mV), entrapment efficiency (85.42 ± 5.34%), surface morphology (spherical) and release profile. Infrared spectroscopy confirmed the entrapment of bromelain while thermal and pXRD analysis concomitantly corroborated the reduced crystallinity of bromelain in nanoparticles. Formulations showed gastro-resistant behavior at gastric pH and sustained bromelain release up to 10 h in phosphate buffer at pH 6.8 and followed Higuchi square root release kinetics. The optimized lyophilized formulation ensured 2 year shelf-life at room temperature. studies revealed significantly improved performance of entrapped bromelain in inhibiting carrageenan induced paw edema by mitigating leucocyte migration and release of nitric oxide, TNFα and IL-1β in paw compared to bromelain solution. In conclusion, enteric Br-NPs could be a viable drug delivery system for effective oral bromelain delivery in inflammatory conditions.

摘要

本研究的目的是开发一种菠萝蛋白酶的肠溶纳米制剂,以提高其稳定性和抗炎潜力。采用Eudragit L 100聚合物通过复乳溶剂蒸发法制备了负载菠萝蛋白酶的纳米颗粒(Br-NPs),以获得抗胃溶性。对Br-NPs的粒径(248.89±22.76 nm)、zeta电位(-27.34±2.17 mV)、包封率(85.42±5.34%)、表面形态(球形)和释放曲线进行了表征。红外光谱证实了菠萝蛋白酶的包封,而热分析和粉末X射线衍射分析同时证实了纳米颗粒中菠萝蛋白酶结晶度的降低。制剂在胃pH值下表现出抗胃溶性,在pH 6.8的磷酸盐缓冲液中菠萝蛋白酶可持续释放长达10小时,并遵循Higuchi平方根释放动力学。优化的冻干制剂在室温下保证了2年的保质期。研究表明,与菠萝蛋白酶溶液相比,包封的菠萝蛋白酶在抑制角叉菜胶诱导的爪肿胀方面表现出显著改善的性能,通过减轻白细胞迁移以及爪中一氧化氮、TNFα和IL-1β的释放来实现。总之,肠溶Br-NPs可能是一种可行的药物递送系统,用于在炎症条件下有效地口服递送菠萝蛋白酶。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3198/9077456/622806100754/c7ra13555f-f1.jpg

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