Felbinac 3% gel

Abstract Background It is important to design an effective formulation to enhance the skin penetration, and nanotechnologies have been used in dermal and transdermal drug delivery. In this study, we prepared formulations (gels) containing l-menthol and felbinac (FEL) solid nanoparticles (FEL-NP gel) for topical application, and investigated the local and systemic absorption of the prepared FEL-NP gel. Methods FEL solid nanoparticles were obtained by bead milling of FEL powder (microparticles), and a topical formulation (FEL-NP gel) consisting of 1.5% FEL solid nanoparticles), 2% carboxypolymethylene, 2% l-menthol, 0.5% methylcellulose, and 5% 2-hydroxypropyl-β-cyclodextrin (w/w %) were prepared. Results The particle size of FEL nanoparticles was 20–200 nm. The released FEL concentration from FEL-NP gel was significantly higher than that from FEL gel without bead mill treatment (carboxypolymethylene gel in which FEL microparticles (MPs) instead of FEL nanoparticles were incorporated, FEL-MP gel), and FEL was released as nanoparticles from the gel. Moreover, both transdermal penetration and percutaneous absorption of FEL-NP gel were significantly increased compared with those of FEL-MP gel, and the area under the FEL concentration-time curve (AUC) of FEL-NP gels was 1.52- and 1.38-fold of commercially available FEL ointment and FEL-MP gel, respectively. In addition, after 24 h of treatment, the FEL content in rat skin treated with FEL-NP gels was 1.38- and 2.54-fold higher than that when treated with commercially available FEL ointment and FEL-MP gel, respectively. Moreover, the enhanced skin penetration of FEL-NP gels was significantly attenuated by inhibition of energy-dependent endocytosis, such as clathrin-mediated endocytosis. Conclusions We successfully prepared a topically applied carboxypolymethylene gel containing FEL nanoparticles. In addition, we observed that the endocytosis pathway was mainly related to the high skin penetration of FEL nanoparticles, and FEL-NP gel application resulted in high local tissue concentration and systemic absorption of FEL. These findings provide useful information for the design of topically applied nanoformulations against inflammation by providing local and systemic effects.

Abstract licence: CC BY 4.0

Abstract The purpose of this study was to design a novel felbinac cataplasm with higher permeability than commercial product SELTOUCH® through using chemical enhancer strategy to reduce the times of administration and improve the compliance of patients. The novel felbinac cataplasm with high adhesion and good biocompatibility was prepared by calendar coating method. On the basis of previous research, the high-performance liquid chromatography (HPLC) analytical method of felbinac was established. According to 2020 Chinese pharmacopoeia (Ch. P), the paddle plate method was used to study the in vitro dissolution. The results showed the release of drug from self-made felbinac cataplasm could reach 90%. Subsequently, the effects of different kinds of penetration enhancers (N-methylpyrrolidone (NMP), isopropyl myristate (IPM) and propylene glycol (PG)) with the same percentage on the penetration of felbinac cataplasm were investigated. Propylene glycol (PG) was proved to be the most effective permeation enhancer among them. After screening different percentages of PG, 1% was added as the amount of permeation enhancer and the 12 h cumulative permeation amount was 189.03 µg/cm2 which was two times of the reference cataplasm (94.44 µg/cm2). The self-made felbinac cataplasm also had good stable permeability after placing at room temperature for 4 months. Finally, the tissue distribution study showed no matter in plasma, skin or muscle, the drug concentration of self-made cataplasm group was higher than reference cataplasm group. These data indicated that the self-made cataplasm provided a new reference for the development of felbinac dosage forms and promising alternative strategy for arthritis therapy.

Abstract licence: CC BY 4.0