Design and Development of a novel transmucosal patch Embedded with Diclofenac Diethylamine loaded solid lipid nanoparticles

Objective: Diclofenac diethylamine (DDEA) loaded solid lipid nanoparticles (SLN) were developed and incorporated in to transmucosal patch (TP) for application in dental surgeries. Methods: DDEA-SLNs were prepared by solvent emulsion evaporation method with compritol 888 ATO as lipid and soya lecithin, Pluronic F68 as surfactants and optimized by a 3-factor 3-level central composite design for its impact on particle size (PS) and entrapment efficiency (EE). SLN was incorporated into a bilayer TP prepared with hydroxypropyl cellulose – LF and polycarbophil along with Labrafac as plasticizer. TP was characterized for tensile and mucoadhesive strength, FTIR, DSC, XRD, SEM, in vitro and ex vivo release. Results: PS, EE, in vitro and ex vivo release of the optimized SLN batch D6 were found to be 178.88 ± 1.3 nm, 54.14 ± 1.6%, 98.26 ± 3.4% and 96.28 ± 3.5% at 24 h respectively. TP showed 99.22 ± 0.7% of in vitro release and 99.53 ± 0.9% permeation through porcine mucosa at 24 h with satisfactory tensile strength and mucoadhesive properties. Conclusion: The designed once a day TP loaded with DDEA-SLN applied at the gingival site, immediately after dental surgery has the potential to produce therapeutic relief locally which is prolonged for 24 h, with the added advantage of overcoming first pass metabolism and gastric irritation, in addition to decreasing the frequency of administration of Diclofenac.

Key words: Ex-vivo permeation, Statistical optimization, Diclofenac SLN, Transmucosal patch.