Pandit Ashlesha P, Pol Vaibhav V, Kulkarni Vinit S
Department of Pharmaceutics, JSPM's Rajarshi Shahu College of Pharmacy & Research, Pune-Mumbai Bypass Highway, Tathawade, Pune, Maharashtra 411033, India.
J Pharm (Cairo). 2016;2016:3054321. doi: 10.1155/2016/3054321. Epub 2016 Jan 28.
The present study was aimed at formulating thermoreversible in situ gel of local anesthetic by using xyloglucan based mucoadhesive tamarind seed polysaccharide (TSP) into periodontal pocket. Temperature-sensitive in situ gel of lidocaine hydrochloride (LH) (2% w/v) was formulated by cold method. A full 3(2) factorial design was employed to study the effect of independent variables concentrations of Lutrol F127 and TSP to optimize in situ gel. The dependent variables evaluated were gelation temperature (Y 1) and drug release (Y 2). The results revealed the surface pH of 6.8, similar to the pH of saliva. Viscosity study showed the marked increase in the viscosity of gel at 37°C due to sol-gel conversion. TSP was found to act as good mucoadhesive component to retain gel at the site of application in dental pocket. Gelation of formulation occurred near to body temperature. In vitro study depicted the fast onset of drug action but lasting the release (90%) till 2 h. Formulation F7 was considered as optimized batch, containing 18% Lutrol F127 and 1% tamarind seed polysaccharide. Thus, lidocaine hydrochloride thermoreversible in situ gel offered an alternative to painful injection therapy of anesthesia during dental surgery, with fast onset of anesthetic action lasting throughout the dental procedure.
本研究旨在通过将基于木葡聚糖的粘膜粘附性罗望子种子多糖(TSP)制成局部麻醉剂的热可逆原位凝胶,并将其注入牙周袋。采用冷法制备了盐酸利多卡因(LH)(2% w/v)的温度敏感原位凝胶。采用全3(2)析因设计研究了自变量 Lutrol F127 和 TSP 的浓度对优化原位凝胶的影响。评估的因变量为凝胶化温度(Y1)和药物释放(Y2)。结果显示表面pH值为6.8,与唾液pH值相似。粘度研究表明,由于溶胶-凝胶转变,凝胶在37°C时粘度显著增加。发现TSP作为良好的粘膜粘附成分,可将凝胶保留在牙袋中的应用部位。制剂在接近体温时发生凝胶化。体外研究表明药物作用起效快,但可持续释放(90%)直至2小时。制剂F7被认为是优化批次,含有18% Lutrol F127和1%罗望子种子多糖。因此,盐酸利多卡因热可逆原位凝胶为牙科手术中痛苦的注射麻醉治疗提供了一种替代方法,麻醉作用起效快,可贯穿整个牙科手术过程。