Formulation, characterization and in vitro–in vivo evaluation of flurbiprofen-loaded nanostructured lipid carriers for transdermal delivery

Abstract

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.

Keywords::

• Nanostructured lipid carriers
• flurbiprofen
• solubility
• transdermal
• differential scanning calorimetry
• pharmacokinetics
• bioavailability
• anti-inflammatory
• stability

Acknowledgments

The authors are grateful to Sun Pharmaceutical Industries Ltd., Ahmednagar, India for providing flurbiprofen as a gift sample, All India Institute of Medical Sciences (AIIMS), New Delhi, India for carrying out TEM studies and Indian Institute of Technology (IIT), New Delhi, India for DSC studies.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.