Formulation and Optimization of Ethosomes for Transdermal Delivery of Ropinirole Hydrochloride

Abstract

The present study focuses on the formulation of ethosomal gel of ropinirole hydrochloride (ropinirole HCl), an anti-Parkinsonian drug, for delivery as a carrier for transdermal application. The ethosomes were prepared using different concentrations of phospholipids (2-5 % w/v), ethanol (20-50 % w/v), ropinirole HCl (5 % w/v) and water. They were optimized using 3(2) full factorial designs to study the effect of independent variables, concentrations of ethanol and lecithin on dependent variables, entrapment efficiency and in-vitro drug release at 24 hrs. The drug release profile exhibited Higuchi's and zero order kinetics. From the regression analysis, it was observed that independent variables had significant effect on response variables. Formulations were optimized using contour plot and response surface plot. The optimized formulation was found to be RS10 containing 30 % w/v ethanol and 4% w/v lecithin. The optimized formulation was evaluated for assay, particle characteristics, zeta potential, skin retention and stability. Ethosomal gel was prepared by incorporation of optimized ethosomal suspension into gel base. The ethosomal gel was characterized for physical appearance, pH, content uniformity, rheological behaviour, skin-retention, in-vitro and in-vivo drug release and stability. From the results it can fairly be concluded that ethosomes are capable of delivering ropinirole hydrochloride into systemic circulation by transdermal route. The amounts thus delivered are also equitable to those delivered orally and are delivered at a rate slow enough to achieve longer blood levels.

Ethosomes for Coenzyme Q10 Cutaneous Administration: From Design to 3D Skin Tissue Evaluation

“…Furthermore, comparing the images with those of untreated cells, it is noteworthy that the ultrastructural morphology of fibroblasts was not affected by the presence of ETHO 0.9 . These findings corroborate previous studies conducted by many authors, indicating that the malleable ETHO vesicles can penetrate cellular membrane, releasing the loaded molecule within cells [ 22 , 24 , 51 , 52 , 53 , 54 ].…”

“…ETHO are vesicular systems whose composition is mainly based on phospholipids (e.g., phosphatidylcholine, PC), ethanol, and water [ 21 , 22 ]. ETHO can be defined as the second generation of liposome, in which the relatively high percentage of ethanol (20–45%) makes the vesicles more stable and enables them to achieve higher drug entrapment efficiency with respect to classic liposomes [ 21 , 22 , 23 , 24 ]. Notably, in vitro and in vivo studies have demonstrated that ETHO possess a transdermal potential, making them suitable for enhancing absorption and bioavailability of different drugs [ 25 , 26 , 27 , 28 , 29 ].…”

“…The transdermal effect has been attributed to the synergistic properties of PC and ethanol, acting both as penetration enhancers. Indeed, on one hand ethanol makes the vesicle structure softer than conventional liposomes, on the other PC and ethanol exert a penetration enhancement effect [ 23 , 24 , 25 , 26 , 27 ]. Particularly, PC itself can promote skin permeation of actives in reason of its chemical similarity with skin lipids [ 30 ], while ethanol opens spaces within the stratum corneum, facilitating the delivery of therapeutic and cosmetic agents through the skin [ 31 ].…”

DOE Optimization of Nano-based Carrier of Pregabalin as Hydrogel: New Therapeutic & Chemometric Approaches for Controlled Drug Delivery Systems

“…The best fit with the highest correlation coefficient (r 2 ) was shown with Higuchi model (0.987–0.993) for control hydrogels and (0.991–0.993) for niosomal hydrogels ( Table 7 and Fig. 7b ) as the release kinetics of some drugs from different hydrogels in the literature followed the Higuchi diffusion model 54 55 . In addition, release data were analyzed using Peppas and Korsmeyer equation 56 .…”

The New Frontiers in Neurodegenerative Diseases Treatment: Liposomal-Based Strategies

“…For instance, Ropinirole hydrochloride is commonly used in Parkinson disease. With the aim to evaluate the possibility to administrate Ropinirole hydrochloride via transdermal route, Mishra et al (2013) synthetized different ethosomal carriers, varying ethanol and lecithin concentrations. The experimental in vivo study showed that RHC encapsulated in ethosomes (30 and 4% w/v of ethanol and lecithin, respectively) increased their blood circulation time, becoming comparable to the oral administration case.…”