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A Novel Dual Action Monolithic Thermosetting Hydrogel Loaded With Lidocaine And Metronidazole As a Potential Treatment For Alveolar Osteitis.
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.4 ) Pub Date : 2020-01-27 , DOI: 10.1016/j.ejpb.2020.01.007 Lena Bender 1 , Hannah M Boostrom 1 , Carmine Varricchio 1 , Marika Zuanon 1 , Vildan Celiksoy 2 , Alastair Sloan 3 , Jonathan Cowpe 3 , Charles M Heard 1
European Journal of Pharmaceutics and Biopharmaceutics ( IF 4.4 ) Pub Date : 2020-01-27 , DOI: 10.1016/j.ejpb.2020.01.007 Lena Bender 1 , Hannah M Boostrom 1 , Carmine Varricchio 1 , Marika Zuanon 1 , Vildan Celiksoy 2 , Alastair Sloan 3 , Jonathan Cowpe 3 , Charles M Heard 1
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Alveolar osteitis is a complication that can occur after tooth extraction, whereby exposed bone results in severe throbbing pain for the patient and can be prone to infection. The current treatment options are widely regarded as sub-optimal. The aim of this project was to investigate in vitro the plausibility of a dual-action monolithic drug-loaded thermosensitive hydrogel that undergoes thermal gelation within the tooth socket and releases both anaesthetic and antimicrobial agents. Hydrogels containing different levels of lidocaine HCl and metronidazole were prepared based upon Carbopol 934P NF and Pluronic F-127 blends. Membrane-less drug release was determined from the set hydrogels into phosphate buffered saline (PBS) at 37°C as a function of time, following analysis by HPLC. Gelation characteristics and hydrogel dissolution characteristics were also determined. At 23.38% Pluronic F-127, sol-gel transition commenced at 23 °C and gelation was completely at 37 °C (physiological temperature). Setting times varied with Pluronic content and there was an inverse relationship between drug release and Pluronic content. Sustained and dose dependent release of both drugs was observed at therapeutically relevant levels over 24h, via a combination of diffusion, dissolution and surface erosion processes. Based on the amounts of drugs released, it was determined that hydrogels containing up to 0.5% lidocaine and 0.1% metronidazole exhibited low risk of cytotoxicity to primary human gingival fibroblasts. In an in vivo scenario, the sol-phase formulation would make contact with all inner surfaces of a tooth socket prior to transitioning to monolithic gel-phase and provide sustained release of lidocaine and metronidazole at sub-toxic levels, thereby providing simultaneous pain relief, protection from ingress of debris and potentially pathological bacteria.
中文翻译：
一种新型的双重作用的整体式热固性水凝胶，载有利多卡因和甲硝唑作为一种治疗肺泡性骨炎的潜在方法。
牙槽骨炎是拔牙后可能发生的并发症，裸露的骨头会给患者带来严重的搏动性疼痛，并且容易感染。当前的治疗选择被广泛认为是次优的。该项目的目的是在体外研究载有双作用整体式药物的热敏水凝胶的可行性，该凝胶在牙槽内发生热胶凝并释放麻醉药和抗菌药。基于Carbopol 934P NF和Pluronic F-127共混物制备了含有不同含量的盐酸利多卡因和甲硝唑的水凝胶。通过HPLC分析，在37℃下随时间从无定形水凝胶测定无膜药物释放到磷酸盐缓冲盐水（PBS）中。还确定了胶凝特性和水凝胶溶解特性。在23.38％的Pluronic F-127，溶胶-凝胶转变在23°C开始，凝胶化完全在37°C（生理温度）下进行。凝结时间随Pluronic含量的不同而变化，药物释放与Pluronic含量之间存在反比关系。通过扩散，溶解和表面腐蚀过程的组合，在治疗相关水平上观察到两种药物的持续释放和剂量依赖性释放在24小时内。根据释放的药物量，可以确定含有高达0.5％利多卡因和0.1％甲硝唑的水凝胶对原代人牙龈成纤维细胞的细胞毒性风险较低。在体内情况下，
更新日期：2020-01-30
中文翻译：
一种新型的双重作用的整体式热固性水凝胶，载有利多卡因和甲硝唑作为一种治疗肺泡性骨炎的潜在方法。
牙槽骨炎是拔牙后可能发生的并发症，裸露的骨头会给患者带来严重的搏动性疼痛，并且容易感染。当前的治疗选择被广泛认为是次优的。该项目的目的是在体外研究载有双作用整体式药物的热敏水凝胶的可行性，该凝胶在牙槽内发生热胶凝并释放麻醉药和抗菌药。基于Carbopol 934P NF和Pluronic F-127共混物制备了含有不同含量的盐酸利多卡因和甲硝唑的水凝胶。通过HPLC分析，在37℃下随时间从无定形水凝胶测定无膜药物释放到磷酸盐缓冲盐水（PBS）中。还确定了胶凝特性和水凝胶溶解特性。在23.38％的Pluronic F-127，溶胶-凝胶转变在23°C开始，凝胶化完全在37°C（生理温度）下进行。凝结时间随Pluronic含量的不同而变化，药物释放与Pluronic含量之间存在反比关系。通过扩散，溶解和表面腐蚀过程的组合，在治疗相关水平上观察到两种药物的持续释放和剂量依赖性释放在24小时内。根据释放的药物量，可以确定含有高达0.5％利多卡因和0.1％甲硝唑的水凝胶对原代人牙龈成纤维细胞的细胞毒性风险较低。在体内情况下，
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