Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Abstract

Abstract:The objective of this study was to prepare a suitable formulation for dermal delivery of diflucortolone valerate (DFV) that would maintain the localization in skin layers without any penetration and to optimize efficiency of DFV. Drug-loaded lecithin/chitosan nanoparticles with high entrapment efficiency (86.8%), were successfully prepared by ionic interaction technique. Sustained release of DFV was achieved without any initial burst release. Nanoparticles were also incorporated into chitosan gel at different ratios for preparing a more suitable formulation for topical drug delivery with adequate viscosity. In ex-vivo permeation studies, nanoparticles increased the accumulation of DFV especially in the stratum corneum + epidermis of rat skin without any significant permeation. Retention of DFV from nanoparticle in chitosan gel formulation (0.01%) was twofold higher than commercial cream, although it contained ten times less DFV. Nanoparticles in gel formulations produced significantly higher edema inhibition in rats compared with commercial cream in in-vivo studies. Skin blanching assay using a chromameter showed vasoconstriction similar to that of the commercial product. There were no barrier function changes upon application of nanoparticles. In-vitro and in-vivo results demonstrated that lecithin/chitosan nanoparticles in chitosan gel may be a promising carrier for dermal delivery of DFV in various skin disorders.

Effective topical delivery systems for corticosteroids: dermatological and histological evaluations

“…The values were found closely related to commercial cream even it contains 10 times less API. The ex-vivo permeation results of current study and in our previous study with nanoparticle in gel formulations showed a better accumulation in stratum corneum + epidermis layer, which is fitted to the results of those produced by Chroma Meter measurements (Ozcan et al, 2013b). A good correlation was also reported between the steroidal drug concentration in skin and the degree of skin blanching (Ishii et al, 2012).…”

“…In our previous work, similar in-vitro results were obtained with lecithin/chitosan nanoparticles in gel formulations (Ozcan et al, 2013b). Pharmacodynamic and treatment efficacies of formulations were investigated with male albino Wistar rats as in-vivo studies.…”

“…Thus, they were incorporated into the chitosan gel as an adequate vehicle, to obtain semi-solid consistency while preserving their original structure (Pavelic et al, 2005). Nanocarrier in chitosan gel system (10%) showed adequate viscosity ($13 000 cps) and spreadability for topical application as shown in our previous study (Ozcan et al, 2013b). In the current study, viscosity values were measured as 13 156-13 200 cps for BMV-and DFV-loaded liposomes or nanopartcile containing gels, at the end of 3 months.…”

“…The EE of nanoparticles was found higher than the EE of liposomes. It was considered that BMV or DFV, due to their lipophilic structure, was located in lipid core of lecithin/chitosan nanoparticles whose lipid composition has been modified by the presence of isopropyl myristate (Ozcan et al, 2013b).…”

Self-assembled lecithin/chitosan nanoparticles for oral insulin delivery: preparation and functional evaluation

“…Several recent studies have investigated the efficiency of this novel nanocarrier in delivering various model drugs via different routes, including oral and transmucosal administration. [18][19][20][21] However, it is believed that only hydrophobic molecules such as progesterone and natamycin can be entrapped into this self-assembled nanocarrier with high entrapment efficiency, whereas poor drug loading (DL) was observed for hydrophilic drugs. 22 Insulin is a large, highly hydrophilic protein that cannot be loaded directly into chitosan-lecithin nanocarriers.…”