Department of Pharmaceutical Sciences, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
Int J Pharm. 2013 Jan 20;440(2):238-49. doi: 10.1016/j.ijpharm.2012.06.004. Epub 2012 Jun 9.
An original formulative/manufacturing approach for the development of a multi-composite wound dressing able to control the release of a water soluble API (lidocaine HCl) for several days was evaluated. The prepared multi-composite wound dressing is a microstructured spongy matrix, which embeds solid lipid microparticles (SLMs). The matrices were obtained by freeze drying of polyelectrolyte complexes made up two biopolymers: three different chitosan to alginate weight ratios (1:1, 3:1 and 1:3) were studied. The drug-loaded matrices were investigated as regards water uptake ability, swelling, drug loading, morphology and release profiles. SLMs were prepared at two different drug loadings (5% and 25%, w/w) by the spray congealing technology and were then incorporated in the spongy matrices. The characterization of the SLMs evidenced their spherical shape, mean dimensions lower than 20 μm, controlled release and the modification of the drug crystalline state. Comparing the release profiles of the SLMs-loaded sponges, the matrices with 1:3 chitosan/alginate ratio displayed a sustained release profile with the lower burst effect. Then hyaluronan and cysteine were embedded into the matrix to enhance the wound healing properties of the dressing. The final multi-composite platform was able to promote the growth of fibroblasts maintaining its prolonged release characteristic.
一种用于开发能够控制水溶性 API（盐酸利多卡因）几天内释放的多复合伤口敷料的原始配方/制造方法进行了评估。所制备的多复合伤口敷料是一种微结构化的海绵基质，其中嵌入了固体脂质微球（SLM）。这些基质是通过冷冻干燥由两种生物聚合物组成的聚电解质复合物获得的：研究了三种不同的壳聚糖与海藻酸钠重量比（1:1、3:1 和 1:3）。对载药基质的吸水能力、溶胀、载药量、形态和释放曲线进行了研究。通过喷雾凝固技术制备了两种不同载药量（5%和 25%，w/w）的 SLM，然后将其掺入海绵基质中。SLM 的表征表明其具有球形形状、低于 20μm 的平均尺寸、控制释放和药物结晶状态的修饰。比较载有 SLM 的海绵的释放曲线，壳聚糖/海藻酸钠比例为 1:3 的基质显示出持续释放的特性，具有较低的突释效应。然后将透明质酸和半胱氨酸嵌入基质中，以增强敷料的伤口愈合性能。最终的多复合平台能够促进成纤维细胞的生长，同时保持其延长的释放特性。
