NDDS Research Laboratory, Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, University of Delhi, New Delhi, India.
Drug Dev Ind Pharm. 2013 Apr;39(4):569-78. doi: 10.3109/03639045.2012.686509. Epub 2012 May 29.
Flurbiprofen is used in the treatment of arthritis. However, its multiple dosing due to short elimination half life is a concern for such treatment. This work aims to develop nanostructured lipid carriers (NLCs) of flurbiprofen and evaluate their potential for transdermal delivery. The NLCs were prepared by the optimized o/w emulsification-homogenization-sonication technique using coconut oil (liquid lipid). The NLCs were found to be spherical with uniform size (214 nm). The entrapment efficiency and zeta potential were 92.58% and -30.70 mV, respectively. Differential scanning calorimetry (DSC) showed the amorphous state of flurbiprofen encapsulated in NLCs. The percentage cumulative drug release through the excised rat skin from NLCs was biphasic and significantly prolonged compared with the commercial gel. DSC of the treated skin indicated that the NLCs penetrate into follicles of the skin and accumulate in the dermis. The bioavailability of flurbiprofen from NLCs was more than 1.7-fold that of the commercial gel. The NLCs showed a quick onset and sustained anti-inflammatory effect over period of 24 h for carrageenan-induced rat paw edema than the commercial gel. The stability data revealed that the NLCs were more stable when stored at 5°C. In conclusion, prepared NLCs have potential for skin targeting and sustained drug release.
氟比洛芬用于治疗关节炎。然而，由于其消除半衰期短，需要多次给药，这对这种治疗方法是一个关注。本工作旨在开发氟比洛芬的纳米结构脂质载体（NLCs）并评估其经皮给药的潜力。NLCs 通过优化的 o/w 乳化-均化-超声技术使用椰子油（液体脂质）制备。NLCs 呈球形且粒径均匀（214nm）。包封效率和 zeta 电位分别为 92.58%和-30.70mV。差示扫描量热法（DSC）显示氟比洛芬在 NLCs 中呈无定形态。与商业凝胶相比，NLCs 中药物的累积释放百分比呈双相且显著延长。处理皮肤的 DSC 表明 NLCs 渗透到皮肤的毛囊中并在真皮中积累。NLCs 的氟比洛芬生物利用度超过商业凝胶的 1.7 倍。NLCs 对卡拉胶诱导的大鼠足肿胀的抗炎作用起效迅速且可持续 24 小时，优于商业凝胶。稳定性数据表明，NLCs 在 5°C 下储存时更稳定。总之，所制备的 NLCs 具有皮肤靶向和持续药物释放的潜力。
