Lipid nanoparticles for transdermal delivery of flurbiprofen: formulation, in vitro, ex vivo and in vivo studies

Abstract

The aim of the study is to prepare aqueous dispersions of lipid nanoparticles – flurbiprofen solid lipid nanoparticles (FLUSLN) and flurbiprofen nanostructured lipid carriers (FLUNLC) by hot homogenization followed by sonication technique and then incorporated into the freshly prepared hydrogels for transdermal delivery. They are characterized for particle size, for all the formulations, more than 50% of the particles were below 300 nm after 90 days of storage at RT. DSC analyses were performed to characterize the state of drug and lipid modification. Shape and surface morphology were determined by TEM which revealed fairly spherical shape of the formulations. Further they were evaluated for in vitro drug release characteristics, rheological behaviour, pharmacokinetic and pharmacodynamic studies. The pharmacokinetics of flurbiprofen in rats following application of SLN gel (A1) and NLC gel (B1) for 24 h were evaluated. The Cmax of the B1 formulation was 38.67 ± 2.77 μg/ml, which was significantly higher than the A1 formulation (Cmax = 21.79 ± 2.96 μg/ml). The Cmax and AUC of the B1 formulation were 1.8 and 2.5 times higher than the A1 gel formulation respectively. The bioavailability of flurbiprofen with reference to oral administration was found to increase by 4.4 times when gel formulations were applied. Anti-inflammatory effect in the Carrageenan-induced paw edema in rat was significantly higher for B1 and A1 formulation than the orally administered flurbiprofen. Both the SLN and NLC dispersions and gels enriched with SLN and NLC possessed a sustained drug release over period of 24 h but the sustained effect was more pronounced with the SLN and NLC gel

The Impact of Variables on Particle Size of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers; A Comparative Literature Review

“…36 Bhaskar et al carried out the same research with Nitrendipene-loaded SLN and NLC dispersion incorporated into hydrogels. 25,37 They reported the same conclusion indicating the stability of nanoparticles in the point of size and PDI after 90 days of storage at room temperature. In the case of gelforming polymers with very polar groups like Chitosan, possible interactions between the negative surface charge of the lipid nanoparticles and the polar groups of this polymer must be considered as well.…”

“…23 The greatest advantage of SLNs is the opportunity for industrial scale fabrication. [24][25][26] To improve the capability of SLNs for drug delivery purposes, second generation lipid nanoparticles (NLC) were developed. 27 In NLC, solid lipids are mixed with fluid lipids so that the final particle is solid at room temperature.…”

A Correlative Model to Predict In Vivo AUC for Nanosystem Drug Delivery with Release Rate-Limited Absorption

“…The name of drugs and the relevant references are given in Table 1 (9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27). As seen in the table the data includes several kind of nanosystems intended for administration via different routes.…”

Enhanced in Vitro Anti-Tumor Activity of 5-Azacytidine by Entrapment into Solid Lipid Nanoparticles

“…26,31 The greatest benefit of SLNs is the possibility of their industrial scale production. [32][33][34] The present study aimed to formulate 5-azacytidineloaded SLNs for the first time to a) overcome 5-azacytidine instability, and b) increase its anti-tumor performance. The stability of 5-azacytidine was studied via high performance liquid chromatography (HPLC).…”