Pharmacy Department, Federal University of Sergipe, São Cristóvão, SE, Brazil.
Instituto de Tecnologia e Pesquisa (ITP), Tiradentes University, Aracaju, SE, Brazil.
Carbohydr Polym. 2018 Jun 15;190:339-345. doi: 10.1016/j.carbpol.2018.02.079. Epub 2018 Mar 6.
Mucoadhesive membranes were proposed in this study as drug delivery system for betamethasone-17-valerate (BMV) in the treatment of recurrent aphthous stomatitis (RAS). The membranes were obtained by using the polymers chitosan (CHI) in both presence and absence of polyvinilpyrrolidone (PVP), following the solvent evaporation method. The presence of PVP in the membranes causes significant modifications in its thermal properties. Changes in the thermal events at 114 and 193 °C (related to BMV melting point), and losses in mass (39.38 and 30.68% for CH:PVP and CH:PVP-B, respectively), suggests the incorporation of BMV in these membranes. However, the morphological aspects of the membranes do not change after adding PVP and BMV. PVP causes changes in swelling ratios (>80%) of the membranes, and it is suggested that the reorganization of the polymer mesh was highlighted by the chemical interactions between the polymers leading to different percentages of BMV released ∼40% and ∼80% from CH-B and CH:PVP-B. BMV release profile follows Korsmeyer and Peppas model (n > 0.89) which suggests that the diffusion of the drug in the swollen matrix is driven by polymer relaxation. In addition, the membranes containing PVP (higher swelling ability) present high rates of tensile strength, and therefore, higher mucoadhesion. Moreover, given the results presented, the developed mucoadhesive membranes are a promising system to deliver BMV for the treatment of RAS.
本研究提出了一种将倍他米松-17-戊酸酯(BMV)制成口腔黏附膜给药系统的方法,用于治疗复发性阿弗他口腔炎(RAS)。采用溶剂蒸发法,以壳聚糖(CHI)为主要原料,添加或不添加聚维酮(PVP)制备黏附膜。PVP 的存在会引起其热性能的显著变化。在 114°C 和 193°C 处的热事件(与 BMV 熔点有关)发生变化,以及质量损失(CH:PVP 和 CH:PVP-B 分别为 39.38%和 30.68%),表明 BMV 被掺入到这些膜中。然而,添加 PVP 和 BMV 后,膜的形态没有变化。PVP 会引起膜的溶胀比(>80%)发生变化,这表明聚合物之间的化学相互作用突出了聚合物网格的重组,导致 CH-B 和 CH:PVP-B 中分别有 ∼40%和 ∼80%的 BMV 释放。BMV 的释放曲线符合 Korsmeyer 和 Peppas 模型(n>0.89),这表明药物在溶胀基质中的扩散是由聚合物松弛驱动的。此外,含有 PVP(具有更高的溶胀能力)的膜具有较高的拉伸强度,因此具有更高的黏膜黏附性。此外,鉴于所呈现的结果,开发的口腔黏附膜是一种有前途的用于治疗 RAS 的 BMV 给药系统。