Formulation and evaluation of lipid nanoparticles enriched gel for transdermal delivery of Aspirin

Abstract

Background: ASP is reported to have antithrombotic, analgesic and anti-inflammatory newlineaction. Gastrointestinal adverse effects due to frequent dosing, shorter half life with poor newlineoral bioavailability leads to limitation to use of ASP in conventional dosage forms. newlineThe main obstacle to develop a transdermal dosage form of ASP is the property of drug newlineto undergo hydrolysis. The basic structure of NLC protects ASP from hydrolysis by newlinekeeping the drug intact in a lipid core. newlineObjective: To develop a novel dosage form of ASP using lipid nanoparticulate approach newlineusing SLNs and NLCs enriched gel for investigating transdermal potential of ASP using newlineskin permeation, pharmacokinetic and pharmacodynamic studies. newlineMethodology: Design and optimization of SLNs and NLCs dispersions were performed newlineby formulating nine formulations of each, with factorial design approach (Design Expert newline8.0.7.1 STATEASE, USA INC.) By varying the concentrations of solid lipid, liquid lipid newlineand surfactant using microemulsion method. SLNs and NLCs dispersions were newlinecharacterized for particle size, zeta potential, polydispersity index, in vitro drug release newlineand SEM studies. On basis of Obtained results SLN5 and NLC7 was found to be an newlineoptimized dispersions and it was suitably gelled by carbopol preparation. Formulated newlineASP-SLNs and ASP-NLCs enriched gel were characterized with respect to pH, newlinespreadability, rheology and consistency index also it was assessed for skin permeation, newlinepharmacokinetic and pharmacodynamic studies. newlineResults: Results of skin permeation studies revealed that formulated ASP-SLNs (150.95 newlineµg/cm newline2 newline/hr) and ASP-NLCs (169.76 µg/cm newline2 newlineXXI newline newline newlineAbstract newline/hr) enriched gel gives more prominent newlinepermeation profile compared with normal ASP gel (100 µg/cm newline2 newline/hr) in rat skin without newline newlineskin irritation. Formulated ASP-SLNs and ASP-NLCs enriched gel showed no platelet newlineagg