Enhanced transdermal delivery of carvedilol using nanoemulsion as a vehicle

Abstract

The aim of the present study was to develop nanoemulsion as a possible vehicle for enhanced transdermal penetration of carvedilol (CVD). For screening of nanoemulsion components, solubility of CVD in oils, surfactants and co-surfactants was determined. Various surfactants and co-surfactants were screened for their ability to nanoemulsify the selected oily phases. The obtained results indicated that Acconon CC6Õ had shown good nanoemulsification efficiency (minimum surfactant required S min ¼ 46.52% w/w) among the selected surfactants and further improved in presence of Õ (S min ¼ 37.11% w/w). The ranges of nanoemulsion existence were delineated through the construction of the pseudo-ternary phase diagram at different ratio of surfactant mixture (S/ CoS), and various nanoemulsions were selected from phase diagram of S/CoS ratio 1 : 1. The effect of content of oil and S/CoS (1 : 1) on the skin permeation of CVD was evaluated through an excised wistar rat skin using Franz diffusion cell. All the nanoemulsions showed a high skin permeation rate (92.251-161.53 mg/ cm 2 /h), good enhancement ratio (3.5-6.2) and high permeability coefficient in comparison to control groups. The optimised nanoemulsion formulation with the highest skin permeation rate (161.53 mg/cm 2 /h) consisted of 0.25% w/w CVD, 12.5% w/w Miglyol 810 Õ , 50% w/w Acconon CC6 Õ /CO-20 Õ (1 : 1) and water. The above formulation had the smallest mean globules size (9.28 nm). The superior transdermal flux of CVD may be due to nanorange size of oil globules that lead to intimate contact with the skin layer. These studies suggest that the nanoemulsion system is a promising vehicle for the transdermal delivery of CVD.

Development, Optimization, and Characterization of Solid Self-Nanoemulsifying Drug Delivery Systems of Valsartan Using Porous Carriers

“…In a comparative study between the selected cosurfactants, Tween 20 showed larger self-emulsification region than PEG 600, due its hydrophilic nature. Higher hydrophilicity property favors faster emulsification of the oil-surfactant mixture in contact with water (28). Based on the various combinations, Capmul MCM, Labrasol, and Tween 20 (1:1) were selected for formulation development, as the above S mix ratio showed highest area for nanoemulsion formation.…”

Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect

“…In the last few years, several transdermal patches have been developed for the delivery of carvedilol through the skin. Carvedilol has been delivered through various transdermal delivery systems, such as nanoemulsions [ 9 ], lipid based nanoparticles [ 10 ], and matrix based systems [ 11 ]. A matrix based transdermal patch showed enhanced bioavailability of carvedilol by 72%, as compared to the oral route [ 11 ].…”

The formulation of ginger oil nanoemulsions of three varieties of ginger (Zingiber officinale Rosc.) as natural antioxidant

“…According to Figure 2, it was known that ethanol was the best cosurfactant in producing ginger oil nanoemulsion due to its translucent visualization and highest percentage transmittance. Furthermore, the higher the percentage transmittance, the smaller the particle size [31][32]. Combination of tween 80 and propylene glycol resulted a turbid nanoemulsion with percentage transmittance less than 90%.…”