Núcleo de Investigações Químico-Farmacêuticas (Niqfar), Programa de Mestrado em Ciências Farmacêuticas, Universidade do Vale do Itajaí (UNIVALI), Itajaí, Santa Catarina, Brazil.
Nanomedicine. 2010 Dec;6(6):745-52. doi: 10.1016/j.nano.2010.06.006. Epub 2010 Jul 3.
Nanoparticles based on chitosan (Ch) and N-carboxymethylchitosan (N-CMCh) cross-linked with tripolyphosphate (TPP) were developed by co-drying with idebenone in different polymer-to-drug ratios (1.3:1 to 16:1) with 20% (wt/wt) colloidal silicon dioxide and tripolyphosphate (0.2 mg/mL). At high ratios (8:1 and 16:1) the spray-dried powder showed spherical and dense particles with a size close to 1 μm, allowing almost complete drug coating by the polymeric system and a high efficiency of drug incorporation (>90% and >80%, for Ch and N-CMCh, respectively). The nanoparticles showed a 10-fold increase of drug stability in comparison with free drug and preserved antioxidant activity in vitro. Compared with the severely irritative free form of idebenone, the nanoparticle formulation showed decreased mucous membrane irritation. These results revealed the potential of Ch and N-CMCh nanoparticles as carriers for a hydrophobic and irritative drug such as idebenone for topical or nasal use.
采用共干燥法，将壳聚糖（Ch）和 N-羧甲基壳聚糖（N-CMCh）与三聚磷酸钠（TPP）交联，制备了纳米粒子。在不同的聚合物-药物比例（1.3:1 至 16:1）下，与 20%（重量/重量）胶体二氧化硅和三聚磷酸钠（0.2mg/mL）共干燥。在高比例（8:1 和 16:1）下，喷雾干燥的粉末显示出球形和致密的颗粒，大小接近 1μm，允许聚合物系统几乎完全包裹药物，并且药物包封效率很高（分别为>90%和>80%）。与游离药物相比，纳米颗粒显示出药物稳定性提高了 10 倍，并在体外保留了抗氧化活性。与伊地苯醌的刺激性游离形式相比，纳米颗粒制剂显示出降低的粘膜刺激性。这些结果表明，壳聚糖和 N-CMCh 纳米颗粒作为载体，可用于局部或鼻腔使用，用于携带疏水性和刺激性药物，如伊地苯醌。
