Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity

Abstract

Objective

Ibuprofen is an established non-steroidal anti-inflammatory drug commonly used for general inflammation. However, it causes gastrointestinal troubles when administered orally, thereby decreasing patient compliance. Transdermal application of vesicular formulation of Ibuprofen will provide better patient compliance and efficacy.

Methods

Six different compositions of lipid constituents have been formulated into nanovesicles using thin-film hydration method and dispersed into gel using Carbopol 934. The formulations were characterized based on physicochemical parameters using photon correlation spectroscopy, transmission electron microscopy, in vitro drug release, ex vivo skin permeation using human skin, and in vivo studies.

Results

The formulation, ibuprofen liposomal gel-5 (ILG-5), had nanoliposome of smallest size (159 nm) and polydispersity index (0.331). This formulation showed moderate zeta potential and the highest encapsulation. All the formulations including IG showed a considerable amount of drug release through in vitro synthetic membrane. ILG-5 showed maximum permeation during skin permeation studies. IG showed no permeation in ex vivo settings. ILG-5 has shown the highest C_max and AUC during in vivo permeation study.

Conclusions

The present work clearly shows the superiority of nanoliposome formulation over non-vesicular formulations and that lipid composition containing 7/3/1 molar ratio of phosphatidylcholine, cholesterol, and dicetyl phosphate is optimum for nanoliposome preparations, in the cases where controlled delivery of drug is needed for a sufficient period of time.

Keywords::

• delivery
• entrapment efficiency
• ibuprofen
• permeation
• nanoliposome

Acknowledgements

The authors acknowledge Asoj Soft caps for providing ibuprofen and phosphatidylcholine.

Further, we acknowledge the sophisticated analytical instrumentation facility, AIIMS, New Delhi for TEM analysis and Advanced centre for nanotechnology, National Institute of Pharmaceutical Education & Research for providing facility of Zetasizer nano ZS.

Declaration of interest

The authors report no declarations of interests. The authors solely are responsible for the content and writing of the paper.