Exploration of the formative mechanisms of colon-targeting composite particles of natural products prepared via mechanical dry particle coating

IF 4.2 2区 工程技术 Q2 ENGINEERING, CHEMICAL
Zekai Chen , Chenyi Yuan , Weiman Hong , Rong Xie , Liangliang Zhou , Yangbiao Li , Zhenhua Chen
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Abstract

Mechanical dry particle coating, coating fine particles in waterless environment, possesses great potential to prepare colon-targeting composite particles of natural products. However, host and guest particles physical properties may impact its surface coverage efficiency. This study selected 10 natural products and 4 colon-targeting excipients as host and guest particles, respectively, and characterized 13 physical properties. Using planetary ball mill, 40 composite particles were prepared and evaluated for SEM, infrared features, and in vitro release. Grey relation analysis, served as the core method, identified critical materials attributes of host and guest particle physical properties affecting the surface coverage and colon-targeting of composite particles. Results indicated that only 9 composite particles achieved favorable surface coverage and in vitro colon-targeting, like guar gum coated total saponins of Pulsatilla with respective surface area coverage and maximum cumulative drug release in colon of 76.71 % and 83.55 %, and revealed the prerequisite of well-covered structure of composite particle for colon-targeting. Identified critical material attributes, including particle size and specific surface area, etc., affected surface coverage efficiency through influencing interparticle forces for adhesion, particularly in van der Waals forces. Moreover, guest particle with favorable hydrophobicity may form a hydrophobic layer, preventing host particles from dissolving under well-covered structure.

Abstract Image

探索通过机械干法颗粒包衣制备的天然产品结肠靶向复合颗粒的形成机制
机械干法颗粒包衣是在无水环境中对细小颗粒进行包衣,具有制备天然产品结肠靶向复合颗粒的巨大潜力。然而,主客体颗粒的物理特性可能会影响其表面覆盖效率。本研究选择了 10 种天然产品和 4 种结肠靶向辅料分别作为主颗粒和客颗粒,并对 13 种物理性质进行了表征。使用行星球磨机制备了 40 种复合颗粒,并对其进行了扫描电镜、红外特征和体外释放评估。以灰色关系分析为核心方法,确定了影响复合微粒表面覆盖率和结肠靶向性的主客体微粒物理性质的关键材料属性。结果表明,只有 9 种复合微粒达到了良好的表面覆盖和体外结肠靶向效果,如瓜尔胶包覆的白头翁总皂苷的表面覆盖率和结肠内最大累积药物释放率分别为 76.71% 和 83.55%,这也揭示了复合微粒的良好覆盖结构是实现结肠靶向的先决条件。已确定的关键材料属性,包括粒度和比表面积等,通过影响粒子间的粘附力,特别是范德华力,影响表面覆盖效率。此外,具有良好疏水性的客体粒子可能会形成疏水层,阻止主粒子在良好覆盖结构下溶解。
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来源期刊
Advanced Powder Technology
Advanced Powder Technology 工程技术-工程:化工
CiteScore
9.50
自引率
7.70%
发文量
424
审稿时长
55 days
期刊介绍: The aim of Advanced Powder Technology is to meet the demand for an international journal that integrates all aspects of science and technology research on powder and particulate materials. The journal fulfills this purpose by publishing original research papers, rapid communications, reviews, and translated articles by prominent researchers worldwide. The editorial work of Advanced Powder Technology, which was founded as the International Journal of the Society of Powder Technology, Japan, is now shared by distinguished board members, who operate in a unique framework designed to respond to the increasing global demand for articles on not only powder and particles, but also on various materials produced from them. Advanced Powder Technology covers various areas, but a discussion of powder and particles is required in articles. Topics include: Production of powder and particulate materials in gases and liquids(nanoparticles, fine ceramics, pharmaceuticals, novel functional materials, etc.); Aerosol and colloidal processing; Powder and particle characterization; Dynamics and phenomena; Calculation and simulation (CFD, DEM, Monte Carlo method, population balance, etc.); Measurement and control of powder processes; Particle modification; Comminution; Powder handling and operations (storage, transport, granulation, separation, fluidization, etc.)
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上海源叶 Pectin
上海源叶 Mannanase
上海源叶 Pectinase
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