■在当前的研究中,开发了负载氯诺昔康的原位凝胶,并评估了它们在眼部炎症中的潜在用途。
■用羟丙基甲基纤维素和泊洛沙姆P407制备的氯诺昔康环糊精复合物由于原位凝胶的低粘度而易于应用。然而,由于加热形成胶凝,因此很难将其从眼表洗涤和除去。
■采用三级析因实验设计来评估泊洛沙姆407浓度的影响,聚合物类型,和聚合物浓度对粘度,pH值,凝胶化能力,凝胶化时间,和凝胶化温度,这被认为是含氯诺昔康制剂的最佳指标。
■作为三级阶乘实验设计的结果,优化的制剂含有15(%w/v)泊洛沙姆407和1(%w/v)羟丙基甲基纤维素。优化配方粘度25°C=504±49cP,粘度35°C=11247±214cP,pH=6.80±0.01,凝胶化温度=35±0.2℃,凝胶化时间=34±0.2s。在体外释放研究中,68%的氯诺昔康在最初的三个小时内释放出爆发效应;然后,释放持续8小时,控制释放。对配方的释放动力学进行了数学建模,发现它与Korsemeyer-Peppas和Weibull模型兼容。在细胞培养研究中,NL6和NL6-CD在100μg/ml时的细胞活力分别为83%和96%,分别。在Draize体内试验中,大鼠未出现阴性情况。
■因此,NL6-CD制剂有可能成为治疗眼部炎症的有利选择。
UNASSIGNED: In the current research, lornoxicam-loaded in situ gels were developed, and their potential usage in ocular inflammation was evaluated.
UNASSIGNED: Lornoxicam cyclodextrin complex prepared with hydroxypropyl methylcellulose and poloxamer P407 because of the low viscosity of in situ gels to provide easy application. However, washing and removing it from the ocular surface becomes difficult due to the gelation formation with heat.
UNASSIGNED: A three-level factorial experimental design was used to evaluate the effects of poloxamer 407 concentration, polymer type, and polymer concentration on viscosity, pH, gelation capacity, gelation time, and gelation temperature, which were considered the optimal indicators of lornoxicam-containing formulations.
UNASSIGNED: As a result of the three-level factorial experimental design, the optimized formulation contained 15 (%w/v) poloxamer 407 and 1 (%w/v) hydroxypropyl methylcellulose. The optimize formulation viscosity 25 °C = 504 ± 49cP, viscosity 35 °C = 11247 ± 214cP, pH = 6.80 ± 0.01, gelation temprature = 35 ± 0.2 °C, and gelation time= 34 ± 0.2 s was obtained. In the in vitro release studies, 68% of lornoxicam was released with a burst effect in the first three hours; then, the release continued for eight hours with controlled release. Release kinetics of the formulations were modeled mathematically, and it was found to be compatible with the Korsemeyer-Peppas and Weibull models. In cell culture studies, cell viability at 100 µg/mL was 83% and 96% for NL6 and NL6-CD, respectively. In Draize\'s in vivo test, no negative conditions occurred in rats.
UNASSIGNED: Therefore, the NL6-CD formulation has the potential to be a favorable option for treating ocular inflammation.