Colloidal Soft Nanocarrier for Transdermal Delivery of Dopamine Agonist: <I>Ex</I> <I>Vivo</I> and <I>In</I> <I>Vivo</I> Evaluation

Abstract

Ropinirole, an antiparkinsoism dopamine agonist, is used to treat Restless Legs Syndrome. However, orally it undergoes degradation in gastrointestinal tract and extensive first pass metabolism, resulting in its poor and variable bioavailability of the commercially available oral tablets. In the present investigation, soft nanocarriers, viz., microemulsion of ropinirole with the globule size of 160 2 ± 3 87 nm and zeta potential of −4.24 mV was explored for transdermal application. Transdermal drug delivery offers benefits such as sustained therapeutic plasma levels of drugs, avoidance of first pass effect, and improved patient compliance. In comparison to the hydrogel, the developed microemulsion enhanced the drug permeation across the rat skin and porcine ear skin by 3.5 and 2 folds, respectively. Further, the developed microemulsion antagonized the catalepsy in the haloperidol-induced catalepsy rat model by 10 folds as compared to the marketed tablets. Additionally, in rotenone induced Parkinsonism rat model, the microemulsion showed improvement in the motor function by 76% whereas the oral tablet showed only 5% restoration of the normal function. Besides this, the developed formulation successfully restored the catalase and superoxide dismutase levels which were significantly reduced by rotenone administration. Overall, the in vivo studies suggested the potential of the developed transdermal microemulsion of Ropinirole as a viable alternative to marketed formulations.

Application of neurotoxin- and pesticide-induced animal models of Parkinson’s disease in the evaluation of new drug delivery systems

“…Patel et al (39) have developed nanocarriers (microemulsions, ME) of RP for transdermal application which are considered highly efficient as colloidal soft nanocarriers in dermal and transdermal drug delivery systems. In this study and in order to achieve sustained and controlled permeation of RP through the skin, ME was converted into a ME-based gel (MEG) using a biocompatible gelling agent.…”

Effect of Free and Nanoencapsulated Copaiba Oil on Monocrotaline-induced Pulmonary Arterial Hypertension

“…Through nanoemulsions, it is possible to improve the chemical stability of substances, prolong the duration of activity, and delineate the site of action. 6,7 The bioavailability of many drugs is limited. To solve this problem, many approaches have been developed, such as incorporation the drug into micro-or nanoparticles.…”