Formulation and characterization of Flurbiprofen nanoparticles loaded microneedles

Abstract

Flurbiprofen (FBP) is a NSAID used in treatment of inflammation, migraine, rheumatic diseases, sore throat and primary dysmenorrhea. FBP is 99% protein bound with rapid oxidative metabolism .The elimination is mainly through urine and the elimination half-life about 3.5 hours. Due to its poor solubility, FBP is a great candidate for formulation of nanoparticles. Poor bioavailability results in frequent dosing and poor patient compliance. Hence an approach has been made to develop FBP nanoparticles loaded microneedle patch for transdermal delivery with faster release and patient compliance.FBP nanoparticles were prepared by using nanoprecipitation method. The particles sizes and zeta potential was measured using zeta potential analyzer. The particles morphology was also determined using SEM. The in-vitro release of FBP from the nanoparticles was carried out in phosphate buffer PH (7.4) containing 10% ethanol to simulate in vivo release in the skin. Microneedle patch of PVA and PVP was prepared using Polydimethylsiloxane (PDMS) micromolds. The ratio of PVA to PVP of matrix solution was optimized to attained maximum needle strength. The optimized strip was evaluated for ex-vivo skin permeation.FBP nanoparticles particle size was in nano size ranged from (9.9 to 158 nm) with positive zeta potential. The drug entrapment efficiency was varied with the drug polymer ratio from 53% -85%. The SEM showed uniform shape and regular distribution of particle sizes. The in-vitro drug release study of nanoparticles exhibited an immediate release of FBP. The outcomes shown that as the ratio of PVP-K30 increased in the polymeric solution blend the needle fraction force decrease. The histopathological study of treated skin showed almost comparable cellular integrity as related to skin treated with PBS (pH 7.4) as control. In addition the skin permeation study show the microneedles permeate more efficiently than simple ordinary patches of the drug through the skin by 4.1 folds.The microneedle patches loaded with FBP nanoparticles were successfully prepared and evaluated .