Hulambukie Eileen, Abdeltawab Hani, Duarah Sanjukta, Svirskis Darren, Sharma Manisha
School of Pharmacy, Faculty of Medical and Health Sciences, The University of Auckland, Auckland 1142, New Zealand.
Gels. 2022 Feb 12;8(2):114. doi: 10.3390/gels8020114.
Nicotine replacement therapy (NRT) is widely used to limit the withdrawal symptoms associated with cigarette smoking cessation. However, the available NRT formulations are limited by their short release profiles, requiring frequent administrations along with local side effects. Thus, the objective of this study is to develop an NRT formulation that offers prolonged, sustained nicotine release. Thermoresponsive in situ gelling systems containing nicotine were prepared using poloxamer 407 (P407) and poloxamer 188 (P188). The system was optimized using a three-factor, two-level full factorial design (2). A formulation composed of P407 (20% ), P188 (5% ), and loaded with nicotine (0.5% ) exhibited sol-to-gel transition at a suitable temperature close to physiological temperature (30 °C). The rheological analysis demonstrated a Newtonian-like flow at room temperature, suggesting ease of administration via injection, and semisolid gel status at physiological temperature. The optimized formulation successfully sustained nicotine in vitro release over 5 days following single administration. The findings suggest that poloxamer based in situ gelling systems are promising platforms to sustain the release of nicotine.
尼古丁替代疗法（NRT）被广泛用于减轻与戒烟相关的戒断症状。然而，现有的NRT制剂受其短释放曲线的限制，需要频繁给药且伴有局部副作用。因此，本研究的目的是开发一种能实现尼古丁延长、持续释放的NRT制剂。使用泊洛沙姆407（P407）和泊洛沙姆188（P188）制备了含尼古丁的热响应原位凝胶系统。该系统采用三因素、两水平全因子设计进行优化。由20%的P407、5%的P188和0.5%的尼古丁组成的制剂在接近生理温度（30℃）的合适温度下表现出溶胶-凝胶转变。流变学分析表明，该制剂在室温下呈类牛顿流体流动，表明易于通过注射给药，在生理温度下呈半固体凝胶状态。优化后的制剂单次给药后在体外成功维持尼古丁释放5天。研究结果表明，基于泊洛沙姆的原位凝胶系统是维持尼古丁释放的有前景的平台。
