Bio-flexy film formulation for delivery of tiagabine via oro trans-soft palatal route and its in-vitro stability study approach

Asian Journal of Nanoscience and Materials Pub Date : 2019-07-01 DOI:10.26655/AJNANOMAT.2019.2.3.7

S. Varshney, N. Madhav

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引用次数: 2

Abstract

The aim of research work was to formulate bio-flexy films using a novel biopolymer isolated from Rosa polyanthapetals containing tiagabine as a model drug. The soft palate drug delivery helps bypass first-pass metabolism in the liver and pre-systemic elimination in the gastrointestinal tract gets avoided. Tiagabine, anticonvulsant drug possesses t1/2:7-9 hours (low); protein binding: 96%; water solubility: 22mg/L enhances acts as selective GABA reuptake inhibitor. Side effects include abdominal pain, pharyngitis, suicidal thoughts and sudden unexpected death. Rosa polyantha biopolymer used as bio-excipient due to its biodegradability, biocompatibility, non-toxicity, non-reactiveness on soft palatal surface. Physicochemical characterization of biopolymer displayed inbuilt filmability, mucoadhesivity properties. Bio-flexy films were prepared by solvent casting technique. Formulations containing different ratios of nanosized Tiagabine: Rosa polyantha biopolymer (1:0.5, 1:1; 1:3, 1:5, 1:6, 1:10) (FRT1-FRT6) were prepared and compared with nanosized Tiagabine loaded Sodium CMC standard flexy films (FET1-FET6). The percentage yield of Rosa polyantha biopolymer was found to be 2.24±0.01%. Evaluation parameters for formulations revealed Thickness of nanosized Tiagabine loaded bio-flexy films containing Rosa polyantha biopolymer (FRT1-FRT6): 0.027 mm±0.005 to 0.039±0.004 mm, Folding Endurance: 83-130, Surface pH: 7.00±0.04 to 7.00±0.01, Weight Uniformity: 0.008±0.05 to 0.044±0.03, Drug Content Uniformity: 85.6%±0.48 to 94.8%±0.37, Swelling Percentage: 66%±0.2 to 75%±0.1, Percentage Moisture Uptake (PTU): 2.5%±0.14 to 3.8%±0.10. Mucoadhesivity: 90-1440 mins, Mucoretentivity: 110-240 mins. Drug release pattern for formulations FRT1-FRT6 containing Rosa polyantha biopolymer based on the T50% and T80% was found to be FRT5 (1:6) > FRT4 (1:5) > FRT6 (1:10) > FRT1 (1:0.5)> FRT3 (1:3) > FRT2 (1:1). Based on all above mentioned evaluation parameters, FRT5 (containing Tiagabine: Rosa polyantha biopolymer (1:6)) bio-flexy film having R2= 0.9295, Higuchi Matrix as best fit model, follows Fickian Diffusion (Higuchi Matrix) release mechanism, T50%: 7hrs., T80%: 30 hrs. using BITS Software 1.12 was found to be Best formulation.

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经软腭给药替加滨的生物弹性膜配方及其体外稳定性研究方法

研究工作的目的是利用从蔷薇花多花中分离的一种新型生物聚合物，以替加滨为模型药物，制备生物柔韧薄膜。软腭给药有助于绕过肝脏的第一关代谢，避免了胃肠道的全身前清除。抗惊厥药物替加滨1/2:7-9小时(低);蛋白结合率:96%;水溶性:22mg/L增强作为选择性GABA再摄取抑制剂。副作用包括腹痛、咽炎、自杀念头和突然意外死亡。多花蔷薇生物聚合物因其可生物降解性、生物相容性、无毒性、在软腭表面无反应性而被用作生物赋形剂。生物聚合物的理化性质显示出内在的成膜性、黏附性。采用溶剂铸造技术制备了生物弹性薄膜。含有不同比例纳米Tiagabine的配方:玫瑰多花生物聚合物(1:0.5,1:1;制备了1:3,1:5,1:6,1:10)(FRT1-FRT6)薄膜，并与纳米Tiagabine负载钠CMC标准柔性薄膜(FET1-FET6)进行了比较。玫瑰多花生物聚合物的产率为2.24±0.01%。配方的评价参数为:纳米级钛加滨生物弹性膜(含玫瑰多刺生物聚合物)的厚度为0.027 mm±0.005 ~ 0.039±0.004 mm，折叠耐久性为83 ~ 130，表面pH为7.00±0.04 ~ 7.00±0.01，重量均匀度为0.008±0.05 ~ 0.044±0.03，药物含量均匀度为85.6%±0.48 ~ 94.8%±0.37，溶膨胀率为66%±0.2 ~ 75%±0.1，吸湿率为2.5%±0.14 ~ 3.8%±0.10。黏附性:90-1440分钟，黏附性:110-240分钟。基于T50%和T80%，发现含有蔷薇多花生物聚合物的FRT1-FRT6制剂的药物释放模式为FRT5 (1:6) > FRT4 (1:5) > FRT6 (1:10) > FRT1 (1:0.5)> FRT3 (1:3) > FRT2(1:1)。综合上述评价参数，FRT5(含Tiagabine: Rosa polyantha生物聚合物(1:6))生物柔韧膜R2= 0.9295, Higuchi Matrix为最佳拟合模型，遵循Fickian Diffusion (Higuchi Matrix)释放机制，T50%: 7hrs。， T80%: 30小时。采用BITS软件1.12为最佳配方。

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Asian Journal of Nanoscience and Materials

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