CENTRAL COMPOSITE DESIGNED APREMILAST LOADED NANOSTRUCTURED LIPID CARRIERS FOR PSORIASIS TREATMENT

<p>Psoriasis is an inflammatory autoimmune disorder of the skin possesses reddened plaques and silvery-scaley patches. Apremilast is phosphodiesterase-4 inhibitor used for psoriasis and psoriasis arthritis. There are solubility constraints which limits its therapeutic effect such as Apremilast cannot be absorbed easily or nor does it dissolve well in water. It’s solubility and bioavailability are quite low. To solve this problem NLCs have been prepared by Glyceryl monostearate solid lipid, Oleic acid liquid lipid, Pluronic F-127 as a surfactant using melt emulsification with probe sonication method. Central Composite Design has been used for optimization of critical formulation variables. Effect of two independent variables such as Glyceryl monostearate and Pluronic F-127 was studied on particle size and entrapment efficiency. The particle size was ranged between 179.3 and 242.1 nm while entrapment efficiency ranged from 74.21% to 86%. Two optimized formulations were selected; NLC7 for high entrapment efficiency and NLC8 smaller particle size. FTIR confirmed drug-excipient compatibility and DSC showed drug was well encapsulated in lipid matrix. Zeta potential of both optimized formulation was found to be –16.5mV and be –19.7mV and indicate good stability of the nanostructured lipid carriers due to sufficient repulsive forces preventing aggregation. In vitro drug release in pH 6.8 buffer for 24 hr showed sustained release NLC7- 86%, NLC8- 87%, respectively represented prolonged drug availability. For estimation of mechanism of drug release data was fitted to various kinetic models and revealed Higuchi model (r² 0.9915) indicating diffusion-controlled release of drug from NLCs. TEM images showed smooth surface spherical particles with no aggregation. Overall, Optimized NLCs stable, nanosized and promising for topical delivery of Apremilast in psoriasis treatment.</p>