ABSTRACT
Background: The present work focuses on the development of ultra-small solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) encapsulating cyclosporine and calcipotriol, further incorporated into gel, increasing their penetration through the skin.
Research design and methods: Developed SLN and NLC were characterized regarding particle size, zeta potential, %entrapment efficiency and dispersed into carbopol 934P-NF gel. Gel was further characterized for rheological behavior and spreadability. Ex vivo dermatokinetic by tape stripping method, in vitro efficacy on HaCaT cell lines and in vivo efficacy on imiquimod induced psoriatic model in mice were evaluated.
Results: Ultra-small (size<100 nm) particles were formed with high entrapment efficiency and spherical morphology. Ex vivo dermatokinetic studies revealed deeper and confined drug penetration of lipid formulation gel in epidermal layers as compared to free drug. In vitro study on HaCaT cell lines depicted higher uptake and high efficacy owing to decrease in cell viability for NLC. The anti-psoriatic efficacy in BALB/c mice (evaluated on basis of cytokine levels and skin morphology) highlighted potential of drug-loaded NLC significantly higher as compared to drug loaded SLN and marketed formulation Betagel.
Conclusions: The study demonstrated that NLC gel had higher efficacy in psoriatic management and hold promise for further exploration.
Acknowledgments
The authors wish to acknowledge Department of Pharmaceuticals, Ministry of Chemicals and Fertilizers, Govt. of India for providing fellowship. Authors also want to express their thanks to Director, NIPER S.A.S. Nagar for providing necessary facilities and infrastructure. V Kushwah is thankful to CSIR, Govt. of India for providing fellowship.
Supplemental meterial
Supplemental data for this article can be accessed here.
Declaration of interest
The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.