Department of Chemistry, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
Istituto di Biochimica e Biochimica Clinica, Università Cattolica del "Sacro Cuore", L.go F. Vito 1, 00168 Rome, Italy.
N Biotechnol. 2016 Jan 25;33(1):23-31. doi: 10.1016/j.nbt.2015.07.005. Epub 2015 Aug 7.
The goal of this study was to develop an optimized drug delivery carrier for oral mucosa applications able to release in situ bioactive molecules by using biopolymeric materials. Among them chitosan and poly(lactic-co-glycolic acid) (PLGA) have gained considerable attention as biocompatible carriers able to improve the delivery of active agents. The formulation of such vehicles in the form of nanoparticles (NPs) could permit to exploit the peculiar properties of nanomaterials in order to enhance the efficacy of active agents. Chitosan (CS) and PLGA chlorexidine dihydrochloride (CHX)-loaded NPs were synthesized by ionotropic gelation and osmosis based methodology respectively. In order to facilitate NPs adhesion on human dental surfaces, two different strategies were employed: PLGA particles with an external shell of CS to produce a positive surface charge allowing CHX loaded PLGA NPs to interact with the negative charged dental surfaces, while CS particles were functionalized with peptidomimetic derivative glutathione (GSH). The morphology was investigated by scanning electron microscopy. A sustained release profile of CHX from CS NPs was achieved. CS-based NPs adhered on human tooth surfaces in a simulated brushing and rinsing process and their in vitro toxicity evaluation on Human Gingival Fibroblasts (HGFs) was between 20 and 60% in all experimental conditions. Thanks to their adhesion properties and low cytotoxicity, the synthesized CS-based formulations may be efficiently exploited for therapy purposes or to enhance in vivo dental care (i.e. preparation of toothpastes or other cosmetics for daily oral care).
本研究的目的是开发一种用于口腔黏膜给药的优化药物传递载体，该载体能够使用生物聚合材料原位释放生物活性分子。其中，壳聚糖和聚（乳酸-共-乙醇酸）（PLGA）作为生物相容性载体已引起广泛关注，能够提高活性药物的传递效率。将这些载体制成纳米颗粒（NPs）的形式可以利用纳米材料的特殊性质来增强活性药物的疗效。通过离子凝胶化和渗透压方法分别合成了壳聚糖（CS）和载有氯己定二盐酸盐（CHX）的 PLGA NPs。为了促进 NPs 在人牙表面的黏附，采用了两种不同的策略：PLGA 颗粒的外壳为 CS，产生正表面电荷，允许载有 CHX 的 PLGA NPs 与带负电荷的牙表面相互作用，而 CS 颗粒则被肽模拟物衍生物谷胱甘肽（GSH）功能化。通过扫描电子显微镜研究了形态。CS 纳米颗粒实现了 CHX 的持续释放。CS 基 NPs 在模拟刷牙和冲洗过程中黏附在人牙表面，其对人牙龈成纤维细胞（HGFs）的体外毒性评估在所有实验条件下均在 20%至 60%之间。由于其黏附性能和低细胞毒性，合成的 CS 基制剂可有效地用于治疗目的或增强体内牙齿护理（例如，制备牙膏或其他用于日常口腔护理的化妆品）。
