Abstract

Aim

The present study endeavours to develop a solid self-microemulsifying nutraceutical drug delivery system for hesperidin (HES) using quality by design (QbD) to improve its biopharmaceutical attributes.

Methods

A 3² full factorial design was employed to study the influence of factors on selected responses. Risk assessment was performed by portraying Ishikawa fishbone diagram and failure mode effect analysis (FMEA). The in vivo antidiabetic study was carried on induced diabetic rats.

Results

The optimised liquid SMEDDS-HES (OF) formulation showed emulsification time (Y ₁) = 102.5 ± 2.52 s, globule size (Y ₂) = 225.2 ± 3.40 nm, polydispersity index (Y ₃) = 0.294 ± 0.62, and zeta potential (Y ₄) = –25.4 ± 1.74 mV, respectively. The solid SMEDDS-HES (SOF-7) formulation was characterised by FTIR, PXRD, DSC, and SEM. The shelf life of SOF-7 was found to be 32.88 months. The heamatological and histopathological data of diabetic rats showed prominent antidiabetic activity.

Conclusions

The optimised formulation showed improved dissolution, desired stability, and promising antidiabetic activity.

中文翻译：

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使用质量源于设计的橙皮苷固体自微乳化营养输送系统：生物药物属性和保质期的评估

摘要

目的

本研究致力于开发一种用于橙皮苷 (HES) 的固体自微乳化营养药物递送系统，使用质量源于设计 (QbD) 来改善其生物制药属性。

方法

采用 3 ²全因子设计来研究因子对选定响应的影响。通过描绘石川鱼骨图和失效模式效应分析（FMEA）进行风险评估。该体内降糖研究进行了诱导的糖尿病大鼠。

结果

优化的液体 SMEDDS-HES (OF) 配方显示乳化时间 ( Y ₁ ) = 102.5 ± 2.52 s，小球大小 ( Y ₂ ) = 225.2 ± 3.40 nm，多分散指数 ( Y ₃ ) = 0.294 ± 0.62，以及 zeta 电位Y ₄ ) = –25.4 ± 1.74 mV，分别。固体 SMEDDS-HES (SOF-7) 配方通过 FTIR、PXRD、DSC 和 SEM 进行表征。发现 SOF-7 的保质期为 32.88 个月。糖尿病大鼠的血液学和组织病理学数据显示出显着的抗糖尿病活性。

结论

优化后的配方显示出更好的溶出度、所需的稳定性和有希望的抗糖尿病活性。