Preparation of Carbopol 934 Based Ketorolac Tromethamine Buccal Mucoadhesive Film: In Vitro, Ex Vivo, and In Vivo Assessments
Preparation of Carbopol 934 Based Ketorolac Tromethamine Buccal Mucoadhesive Film: In Vitro, Ex Vivo, and In Vivo Assessments
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DOI：
10.1155/2021/4786488
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发表时间：
2021-10-11
影响因子：
3.3
通讯作者：
Rahamathulla, Mohamed
中科院分区：
文献类型：
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作者：
Begum, M. Yasmin;Alqahtani, Ali;Rahamathulla, Mohamed
本研究的目的是研制和评价酮咯酸氨丁三醇(KTM)口腔黏膜粘附膜。以PVP K30、HPMCK4M、HPMCK15M、卡波姆934、壳聚糖、海藻酸钠为聚合物，丙二醇为增塑剂，采用溶剂挥发法制备膜。对薄膜的厚度、重量变化、耐折叠性、表面pH值、溶胀指数、体外滞留时间、体外扩散、释放动力学、体外渗透、体内外相关性以及抗炎、镇痛等体内药理活性进行了评价。薄膜的厚度、重量、药物含量和耐折叠性被发现是一致的。表面pH值为6.85+/-0.10，溶胀指数最高(27.27+/-0.37)。F2的体外滞留时间大于5h，体外释药百分率为98.71%。F2膜在5h的抑肿率为55.49%，8h的抑肿率在38.88%以上，5h的最大镇痛反应为17s，8h的最大镇痛反应为11s，与游离药物溶液相比，F2的抗炎镇痛作用最强，且持续时间较长。因此，含有卡波姆934、海藻酸钠和PVP K30的KTM口腔粘附膜可能是一种有效的替代传统疗法的方法，其疗效更佳。
The goal of present investigation was to formulate and evaluate ketorolac tromethamine (KTM) mucoadhesive buccal films. The films were prepared by solvent evaporation method using PVP K30, HPMC K4M, HPMC K15M, carbopol 934, chitosan, and sodium alginate as polymers and propylene glycol as plasticizer. The films were evaluated for thickness, weight variation, folding endurance, surface pH, swelling index, in vitro residence time, in vitro diffusion, release kinetics, ex vivo permeation, in vitro-ex vivo correlation, and in vivo pharmacological activities such as anti-inflammatory and analgesic activity. Thickness, weight, drug content, and folding endurance were found to be uniform for the films. Surface pH was 6.85 +/- 0.10, and swelling index was the highest (27.27 +/- 0.37) for the best film containing carbopol 934 along with sodium alginate and PVP K 30 (formulation code F2). In vitro residence time was greater than 5 h, and in vitro % drug release was 98.71% for F2. It exhibited 55.49% of swelling inhibition at 5 h, and above 38.88% was maintained at even 8 h. The film F2 has shown maximum analgesic response of 17 sec at 5 h, and the response of 11 sec was maintained at even 8 h. The anti-inflammatory and analgesic effect of F2 was found be maximum while sustaining the effect for prolonged period when compared to free drug solution. Thus, KTM mucoadhesive buccal film containing carbopol 934, sodium alginate, and PVP K30 could be an effective alternative for conventional therapy with improved efficacy.