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首页> 外文期刊>Materials science & engineering >Design and optimization of kollicoat ® IR based mucoadhesive buccal film for co-delivery of rizatriptan benzoate and propranolol hydrochloride
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Design and optimization of kollicoat ® IR based mucoadhesive buccal film for co-delivery of rizatriptan benzoate and propranolol hydrochloride

机译：基于kollicoat®IR的粘膜粘膜颊膜的设计和优化，用于共同递送利扎曲普坦苯甲酸酯和盐酸普萘洛尔

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摘要

This work aimed to develop a mucoadhesive buccal film for potential co-delivery of rizatriptan benzoate (RB) and propranolol hydrochloride (PRH). Kollicoat (R) 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 (R) 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 (R) 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.
机译：这项工作的目的是开发一种粘膜粘膜颊膜，以潜在地共同递送利扎曲普坦苯甲酸酯（RB）和盐酸普萘洛尔（PRH）。使用Kollicoat IR，聚环氧乙烷（PEO），羟丙基甲基纤维素（HPMC K4M），甘油，甜叶菊和芦荟凝胶粉（AVgel粉）通过溶剂流延法制备薄膜。为了表征和优化配方，使用了具有中央复合设计（CCD）的Design-Expert软件。选择的独立变量是IR，PEO，甘油和AVgel粉末的浓度。选择的五个因变量是体外崩解时间，耐折性，溶胀率和体外药物释放。选择具有50 mg PRH，25 mg RB，5 mg甜菊糖，63 mg HPMC K4M，100 mg IR，66.33 mg PEO，0.22 ml甘油和0.8 mg AVgel粉末的薄膜作为优化配方。通过扫描电子显微镜（SEM），傅立叶变换红外光谱（FTIR）和差示扫描量热法（DSC）对优化的薄膜进行表征，以评估薄膜的形态，化学结构和物理性能。优化膜的机械性能用桑塔姆仪器测量。通过Franz扩散池研究离体渗透，而大鼠颊粘膜用作模型膜。掺有AVgel粉作为天然渗透促进剂的优化膜可在100分钟内通过大鼠颊黏膜转运73.22％的PRH和96.11％RB，组织病理学评估后未显示颊黏膜损伤。总体而言，优化的薄膜可能是有效治疗偏头痛的潜在候选者。

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