Wróblewska Magdalena, Winnicka Katarzyna
Department of Pharmaceutical Technology, Faculty of Pharmacy, Medical University of Białystok, Mickiewicza 2c, 15-222 Białystok, Poland.
Int J Mol Sci. 2015 Aug 27;16(9):20277-89. doi: 10.3390/ijms160920277.
Polyamidoamine dendrimers (PAMAM) represent a new class of hyperbranched, monodisperse, three-dimensional polymers with unique properties, which make them very promising carriers of antimicrobial agents. The present study aimed to evaluate the influence of PAMAM-NH₂ dendrimers generation two (G2) or three (G3) on physicochemical characteristics and structure of hydrogels with a model antibacterial lipophilic drug-erythromycin-commonly used in topical applications. From the obtained rheograms, it can be concluded that tested hydrogels were non-Newtonian thixotropic systems with shear-thinning behaviour. The dissolution tests revealed that erythromycin was definitely faster released from formulations containing PAMAM-NH₂ in concentration and generation dependent manner. However, the addition of PAMAM-NH₂ to hydrogels evoked only slight improvement of their antibacterial activity. It was also shown that the structure of hydrogels changed in the presence of PAMAM-NH₂ becoming less compact, diversified and more porous. Designed hydrogels with PAMAM-NH₂ G2 or G3 were stable stored up to three months at 40 ± 2 °C and 75% ± 5% RH.
聚酰胺-胺树枝状大分子（PAMAM）是一类新型的超支化、单分散三维聚合物，具有独特的性质，这使其成为非常有前景的抗菌剂载体。本研究旨在评估第二代（G2）或第三代（G3）PAMAM-NH₂树枝状大分子对含有一种常用于局部应用的模型抗菌亲脂性药物——红霉素的水凝胶的物理化学特性和结构的影响。从所得流变图可以得出结论，测试的水凝胶是非牛顿触变体系，具有剪切变稀行为。溶出试验表明，红霉素从含有PAMAM-NH₂的制剂中的释放速度明显更快，且呈浓度和代数依赖性。然而，向水凝胶中添加PAMAM-NH₂仅使其抗菌活性略有提高。还表明，在PAMAM-NH₂存在下，水凝胶的结构发生变化，变得不那么致密、更加多样且孔隙更多。设计的含有G2或G3 PAMAM-NH₂的水凝胶在40±2°C和75%±5%相对湿度下稳定储存长达三个月。
Zotero 插件
