Development and In-Vitro Tuning of Piperine Containing Solid Lipid Microparticles for the Treatment of Rheumatoid Arthritis

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY AAPS PharmSciTech Pub Date : 2025-01-22 DOI:10.1208/s12249-024-03034-y
Muneeba Aziz, Sajid Bashir, Rai Muhammad Sarfraz, Hira Ijaz, Asif Mahmood,  Zulcaif, Bilal Haroon, Milad A. Mezher, Mohamed M. Salem, Sami Al Zahrani, Mounir M. Bekhit
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Abstract

The current project was designed to develop piperine-loaded solid lipid microparticles (SLMs) to assess the anti-arthritic potential of piperine (PIP). Variable proportions of carnauba wax, beeswax, and tween 80 were employed for preparing SLMs by using the solvent evaporation technique. The developed formulations were subjected to particle size measurements, entrapment efficiency (EE), and zeta potential (ZP) determination. Microparticles were also investigated for piperine-lipid compatibility, thermal analysis, surface morphology, piperine (PIP) release trend, and anti-rheumatic activity in rats. The network's grafting was confirmed by FTIR and XRD results. The thermal stability of the constructed network was confirmed by the DSC and TGA results. SEM findings confirm porous surface morphology. The dissolution experiments on SLMs confirmed the sustained release profile, delivering 87.82% to 94.92% of piperine at 7.4 pH for 24 h. All developed formulations followed a zero-order kinetic model and the Korsmeyer-Peppas model. Furthermore, the anti-rheumatic potentials of piperine from SLMs were also investigated and compared with diclofenac sodium (the standard treatment) in a rat model. The analysis revealed that PIP significantly reduced the severity of arthritis, as confirmed by the findings of multiple arthritic assessment parameters.

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含胡椒碱固体脂质微颗粒治疗类风湿性关节炎的研制及体外调节
目前的项目旨在开发装载胡椒碱的固体脂质微粒(SLMs),以评估胡椒碱(PIP)的抗关节炎潜力。采用溶剂蒸发法制备了不同比例的巴西棕榈蜡、蜂蜡和t80。对所研制的配方进行了粒径测定、包封效率(EE)和ζ电位(ZP)测定。研究了微颗粒的胡椒-脂相容性、热分析、表面形态、胡椒碱(PIP)释放趋势和大鼠抗风湿病活性。FTIR和XRD结果证实了网络的接枝效果。DSC和TGA结果证实了所构建网络的热稳定性。SEM结果证实了多孔表面形貌。在slm上的溶出实验证实了其缓释特性,在7.4 pH下释放87.82%至94.92%的胡椒碱24小时。所有开发的配方都符合零级动力学模型和korsmemeyer - peppas模型。此外,还研究了slm中胡椒碱的抗风湿潜能,并在大鼠模型中与双氯芬酸钠(标准治疗)进行了比较。分析显示PIP显著降低了关节炎的严重程度,正如多个关节炎评估参数的结果所证实的那样。图形抽象
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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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