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首页> 外文期刊>The Open Drug Delivery Journal >Formulation of Nano and Micro PLGA Particles of the Model Peptide Insulin: Preparation, Characterization, Stability and Deposition in Human Skin
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Formulation of Nano and Micro PLGA Particles of the Model Peptide Insulin: Preparation, Characterization, Stability and Deposition in Human Skin

机译：模型肽胰岛素的纳米PLGA微粒的配制：在人体皮肤中的制备，表征，稳定性和沉积

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The primary objective of this study was to develop a particulate formulation for peptide delivery that wouldprovide enhanced peptide stability, controlled release and the potential for targeting to specific tissues. Biodegradable hydrophobicparticles were prepared from poly (D,L-lactide-co-glycolide) (PLGA) by both solvent evaporation and solventdiffusion methods. Bovine insulin was chosen as a model peptide for formulation development and evaluation. By forminga complex between insulin and protamine, 50% incorporation of the model peptide in PLGA particles was achievedand a sustained release of insulin was observed over one week with improved stability of insulin in the PLGA matrix. Theformation of an insulin-protamine complex and the method of manufacture are important determinants of the physicochemicalcharacteristics of the particles formed. Preliminary evaluation of the deposition of the particles within skin wasdetermined by fluorescent images following topical application to excised human skin. Microparticles with size above 7μm remained on the surface of the skin. Nanoparticles (<1 μm) showed permeation into the viable epidermis and dermiswith deposition concentrated around the hair follicles and sebaceous glands.
机译：这项研究的主要目的是开发一种用于肽递送的颗粒制剂，该制剂将提供增强的肽稳定性，控释和靶向特定组织的潜力。通过溶剂蒸发和溶剂扩散方法，由聚（D，L-丙交酯-共-乙交酯）（PLGA）制备可生物降解的疏水颗粒。选择牛胰岛素作为制剂开发和评估的模型肽。通过在胰岛素和鱼精蛋白之间形成复合物，在PLGA颗粒中实现了50％的模型肽掺入，并且观察到胰岛素持续释放超过一周，并改善了PLGA基质中胰岛素的稳定性。胰岛素-鱼精蛋白复合物的形成和制造方法是所形成颗粒的物理化学特征的重要决定因素。在局部施用于切除的人皮肤上之后，通过荧光图像确定对颗粒在皮肤内的沉积的初步评估。尺寸大于7μm的微粒残留在皮肤表面。纳米颗粒（<1μm）渗透到活的表皮和真皮中，沉积物集中在毛囊和皮脂腺周围。

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