Improved skin-permeated diclofenac-loaded lyotropic liquid crystal nanoparticles: QbD-driven industrial feasible process and assessment of skin deposition

ABSTRACT

The purpose of the present study was to optimise diclofenac diethylamine-loaded liquid crystal nanoparticles (LCNPs) using the principles of quality by design. Based on risk assessment, the effect of various formulation variables on the critical quality attributes was investigated. A three-level Box-Behnken design with 14 runs was utilised for optimisation. The LCNPs were evaluated for size, polydispersity index, zeta potential, entrapment efficiency, morphology, solid-state characterisation, and drug release. The LCNPs were found to show prolonged drug release up to 12 h as compared to the free drug which showed a 100% release in less than 3 h. The optimised formulation was further investigated for scale-up studies, incorporated into carbopol gel and characterised for rheological parameters, skin permeation, and skin accumulation. Ex-vivo skin permeation studies revealed 1.55 times more permeation as compared to the marketed formulation. The designed gel had the potential to prolong the drug release, improve the permeation of drug through the skin layers, and industrial feasibility.

Graphical abstract

KEYWORDS:

• Diclofenac diethylamine
• liquid crystal nanoparticles
• permeation
• quality by design
• skin deposition

Acknowledgments

Authors are very thankful to Sun Pharmaceutical Pvt Ltd, India for providing a generous gift sample of Diclofenac diethylamine. We are thankful to Mohini Organics Pvt. Ltd. for providing us Glyceryl monooleate (Monegyl-O100) as a gift sample for this research study. We acknowledge the research support of BASF (India) for providing gift sample of Lutrol® F 127 (Polaxomer 407). We are grateful to Lubrizol for providing Carbopol® 980P NF as a free sample for our studies.

Disclosure statement

The authors report no conflict of interest.

Additional information

Funding

The study is not funded by any agency.