Surface Engineering and Optimizing DepoFoam System: A Robust Quality by Design Approach for Optimal Drug Delivery, Stability, and Quality

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY

Journal of Pharmaceutical Innovation Pub Date : 2024-01-18 DOI:10.1007/s12247-024-09808-y

Jebastin Koilpillai, Damodharan Narayanasamy

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引用次数: 0

Abstract

Purpose

The study utilized non-ionic polymer macrogol to transform the surface properties of the DepoFoam drug carrier system, developing “surface-remodeled DepoFoam (SR-DFO)” following quality by design (QbD) principles. The primary objectives were to prolong drug delivery, reduce sudden releases, and enhance the overall quality and stability of DepoFoam. The research hypotheses are centered on the capability of macrogol-based surface modification to create an optimized drug delivery system with improved stability, extended drug release, and enhanced pharmacokinetic properties.

Methods

In this research, surface remodeling was achieved through a series of processes, including high-shear homogenizer-assisted double emulsification, PEGylation, and purification. The resulting SR-DFO formulations were comprehensively characterized for critical quality attributes. Optimization was conducted using the Box-Behnken design, resulting in significant enhancements in both quality and stability compared to conventional liposomes and unmodified DepoFoam.

Results

Comprehensive product characterization validates anticipated quality parameters: entrapment efficiency (86.16 ± 0.44%), drug-loading capacity (25.28 ± 0.07%), vesicle size (40.47 ± 0.1 µm), polydispersity index (PDI) of 0.051 ± 0.03, lipocrit of 90.67 ± 0.26%, and zeta potential of − 31.25 ± 3.25 mV. Remarkably, macrogol-based SR-DFO consistently sustains drug release above 90% for 168 h, devoid of sudden spikes, and maintains stability at 4 °C for 180 days. Mathematical models confirm drug release mechanisms’ validity. Moreover, this study emphasizes the critical influence of key materials like macrogol, phospholipids, triglycerides, and process variables on shaping product quality.

Conclusion

These findings highlight the inventive promise of macrogol-coated DFO in transforming drug delivery, quality, and stability. This research, driven by a well-formed hypothesis, meticulous execution, and precise data analysis, opens new horizons in polymer-based DepoFoam systems.

Graphical Abstract

First author: Jebastin Koilpillai, M.Pharm.

Abstract Image

查看原文本刊更多论文

表面工程和优化 DepoFoam 系统：优化药物输送、稳定性和质量的可靠质量设计方法

目的该研究利用非离子聚合物大观醇改变了DepoFoam药物载体系统的表面特性，按照质量源于设计（QbD）原则开发出了 "表面重塑DepoFoam（SR-DFO）"。研究的主要目标是延长给药时间，减少药物的突然释放，并提高 DepoFoam 的整体质量和稳定性。研究假设的核心是基于大环内酯的表面改性能否创造出一种具有更高的稳定性、更长的药物释放时间和更强的药代动力学特性的优化给药系统。对所得到的 SR-DFO 配方的关键质量属性进行了全面表征。结果全面的产品表征验证了预期的质量参数：夹带效率（86.16 ± 0.44%）、药物负载能力（25.28 ± 0.07%）、囊泡大小（40.47 ± 0.1 µm）、多分散指数（PDI）为 0.051 ± 0.03、脂容积为 90.67 ± 0.26%、Zeta 电位为 - 31.25 ± 3.25 mV。值得注意的是，基于大环内酯的 SR-DFO 在 168 小时内药物释放量始终保持在 90% 以上，没有突然的峰值，并在 4 °C 下保持稳定 180 天。数学模型证实了药物释放机制的有效性。此外，这项研究还强调了大环内酯、磷脂、甘油三酯等关键材料和工艺变量对产品质量形成的重要影响。这项研究由完善的假设、细致的执行和精确的数据分析所驱动，为基于聚合物的DepoFoam系统开辟了新天地：Jebastin Koilpillai，药学硕士。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.