Department of Biomedical Engineering, Faculty of Chemical Engineering, Tarbiat Modares University, Tehran, Iran.
Department of Biomedical Engineering, Faculty of Chemical Engineering, Tarbiat Modares University, Tehran, Iran.
Mater Sci Eng C Mater Biol Appl. 2019 Apr;97:230-244. doi: 10.1016/j.msec.2018.12.036. Epub 2018 Dec 12.
This work aimed to develop a mucoadhesive buccal film for potential co-delivery of rizatriptan benzoate (RB) and propranolol hydrochloride (PRH). Kollicoat ® IR, polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC K4M), glycerol, stevia, and Aloe vera gel powder (AVgel powder) were used to prepare film by solvent casting method. In order to characterize and optimize formulations, Design-Expert software with central composite design (CCD) was used. The selected independent variables were concentrations of Kollicoat ® IR, PEO, glycerol, and AVgel powder. Five selected dependent variables were in vitro disintegration time, folding endurance, swelling ratio, and in vitro drugs release. Film with 50 mg PRH, 25 mg RB, 5 mg stevia, 63 mg HPMC K4M, 100 mg Kollicoat ® IR, 66.33 mg PEO, 0.22 ml glycerol, and 0.8 mg AVgel powder was selected as optimized formulation. The optimized film was characterized by scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) to evaluate morphology, chemical structure, and physical properties of the film. The mechanical properties of optimized film were measured by Santam instrument. Ex vivo permeation were studied by Franz diffusion cell, while rat buccal mucosa was used as a model membrane. The optimized film with incorporation of AVgel powder as a natural permeation enhancer could transport 73.22% of PRH and 96.11% of RB over 100 min through rat buccal mucosa and showed no buccal mucosal damage after histopathological evaluation. Overall, the optimized film could be a potential candidate for the effective treatment of migraine.
本工作旨在开发一种具有黏膜黏附性的颊膜，用于潜在地共递送苯甲酸瑞扎曲普坦（RB）和盐酸普萘洛尔（PRH）。使用 Kollicoat ® IR、聚氧化乙烯（PEO）、羟丙基甲基纤维素（HPMC K4M）、甘油、甜菊糖和芦荟凝胶粉（AVgel 粉）通过溶剂浇铸法制备薄膜。为了对配方进行特征描述和优化，使用 Design-Expert 软件和中心复合设计（CCD）。选择的独立变量是 Kollicoat ® IR、PEO、甘油和 AVgel 粉的浓度。五个选择的因变量是体外崩解时间、折叠耐力、溶胀比和体外药物释放。选择含有 50mg PRH、25mg RB、5mg 甜菊糖、63mg HPMC K4M、100mg Kollicoat ® IR、66.33mg PEO、0.22ml 甘油和 0.8mg AVgel 粉的薄膜作为优化配方。通过扫描电子显微镜（SEM）、傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）对优化薄膜进行特征描述，以评估薄膜的形态、化学结构和物理性质。使用 Santam 仪器测量优化薄膜的机械性能。通过 Franz 扩散池研究了体外渗透，同时使用大鼠颊黏膜作为模型膜。含有 AVgel 粉作为天然渗透增强剂的优化薄膜可以在 100 分钟内通过大鼠颊黏膜输送 73.22%的 PRH 和 96.11%的 RB，并且在组织病理学评价后没有颊黏膜损伤。总的来说，含有 AVgel 粉的优化薄膜可以作为治疗偏头痛的有效候选药物。
