A novel transdermal nanoethosomal gel of betahistine dihydrochloride for weight gain control: in-vitro and in-vivo characterization

Abstract

BackgroundBetahistine dihydrochloride (BDH) is a histamine analog used to control weight gain, with short elimination half-life and gastric irritation as side effects.ObjectiveThe aim of the current investigation is to formulate and optimize a topical BDH ethosomal gel for weight gain control.Materials and methodsBox–Behnken design was applied to study the effect of independent variables: phosphatidylcholine (PC), propylene glycol (PG), and ethanol on vesicle size; entrapment efficiency; % drug release; and flux. The morphology and zeta potential of the optimized formulation were evaluated. The % drug release, flux, and pharmacodynamics of the optimized formulation gel were studied.ResultsThe size and entrapment efficiency percent had a direct positive relationship with the concentration of PC and negative relationship with ethanol and PG. The % drug release and flux decreased with increasing PC and PG, while ethanol enhanced both responses. Regression modeling indicated a good correlation between dependent and independent variables, where F16 was chosen as the optimized formulation. F16 showed well-defined spherical vesicles and zeta potential of −24 mV, and % release from the gel exceeded 99.5% over 16 h with the flux of 0.28 mg/cm2/h. Food intake and weight gain of rats were significantly decreased after transdermal application of the BDH ethosomal gel when compared with control, placebo, and BDH gel. The histopathological findings proved the absence of inflammation and decrease in adipose tissue.ConclusionResults obtained showed a significant, sustained transdermal absorption of BDH ethosomal gel and, consequently, a decrease in food intake and weight gain.

Formulation of Sodium Valproate Nanospanlastics as a Promising Approach for Drug Repurposing in the Treatment of Androgenic Alopecia

“…The in vitro release of SV-loaded nanospanlastics was implemented using the membrane diffusion technique using a glass cylinder which is attached to the USP dissolution apparatus shaft (USP apparatus II, Erweka DT-720, Germany) [ 20 , 25 ]. Firstly, the semi-permeable cellulose membrane was hydrated using phosphate buffer (pH = 7.4) for 24 h at room temperature.…”

“…The comparative ex vivo permeation study of the optimized SV-loaded SNVs was done using the membrane diffusion technique previously described except for the use of the pre-soaked rat skin instead of the dialysis membrane [ 20 , 25 ]. The pre-soaked rat skin was mounted carefully at the cylinder base with the SC side facing the donor chamber.…”

Tailoring of Retinyl Palmitate-Based Ethosomal Hydrogel as a Novel Nanoplatform for Acne Vulgaris Management: Fabrication, Optimization, and Clinical Evaluation Employing a Split-Face Comparative Study

“…The ethosomal particle size increased with increasing the concentration of PC Phospholipids are the main component of the ethosomal wall and therefore expected to increase wall thickness and therefore increase particle size. 45 It is worth noting that propylene glycol and ethanol concentration had an antagonistic effect on the mean ethosomes' size; 46,47 this can be interpreted to the negative charge gained by both ethanol and PG, which causes electrostatic repulsion and prevention of vesicle aggregation. 48 Furthermore, the reduction in membrane thickness resulted from the interaction of ethanol and PG with the lipid bilayer.…”

Development of Provesicular Nanodelivery System of Curcumin as a Safe and Effective Antiviral Agent: Statistical Optimization, In Vitro Characterization, and Antiviral Effectiveness

“…The in vitro release study of Curcumin-loaded proniosomes was demonstrated by the dialysis method using a glass cylinder which is attached to the dissolution apparatus shaft (USP apparatus II, Erweka DT-720, Kreuzau, Germany) [17,35,36]. Initially, the semi-permeable cellulose membrane was hydrated using a phosphate buffer solution of pH = 7.4 [10] at 25 • C for 24 h. To maintain the sink condition, 0.5% (w/v) SLS was added to phosphate buffer, pH = 7.4, and used as the dissolution medium [37].…”