Formulation Development, Characterization and in-vitro Evaluation of Nano-Lipid Carriers of Ropinirole HCl for Persistent Parkinsonian Management

Abstract

According to a report of World Health Organization (WHO) 2014, Parkinson's Disease (PD) is the second-most neurodegenerative dysfunction of the central nervous system (CNS) of human being effecting 7–10 million people worldwide. It is primarily due to the death of dopamine-generating cells in the substantia-nigra of midbrain. It is symptomatized by tremor, rigidity, bradykinesia, dementia, depression and falls or emerges with the progression of the disease. Ropinirole HCl is a low molecular weight, highly water soluble active pharmaceutical agent (API) which is rapidly absorbed from the gastro intestinal tract (GIT) and mean peak plasma concentrations have been achieved within 1.5h after oral doses. The oral bioavailability of Ropinirole HCl is less than 50% due to extensive first pass metabolism by the liver. Its mean plasma half-life is 5–6h. The present study tries to enlighten the prior art related to Parkinson's treatment and to prepare Ropinirole HCl loaded nano-structured lipid carriers (NLCs) that may overcome the problem of bio-availability and bypass the blood–brain barrier by preparing the intra-nasal drug delivery targeted to the brain thereby decreasing the dosing frequency and increasing patient compliance. Ropinirole HCl was characterized using various techniques such as melting point determination, Fourier-Transform Infrared (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and U-V scan analysis. A total of eight formulations (RNH1–RNH8) were designed using half factorial design 2³ model by using two different lipids i.e., Isopropyl myristate and Glyceryl monostearate and Pluronic F-68 as surfactant. Ropinirole HCl loaded NLCs were fabricated by hot homogenization method. The optimized NLC formulations were characterized for their % Entrapment efficiency, particle size, zeta potential, transmission electron microscopy (TEM), in-vitro drug release studies and different types of release kinetics models (First order, zero order, Higuchi etc.) were applied. On the basis of evaluation parameters, formulation RNH6 was found to be better as compared to others. The promising results of optimized formulation suggested a practical approach for achieving better therapeutic efficacy by being able to target the CNS.

Keywords: Parkinson's disease, CNS targeting, nano-structured lipid carriers (NLC), nanotechnology.

Cite this Article

Katual MK, Singh G, HariKumar SL. Formulation Development, Characterization and in-vitro Evaluation of Nano-Lipid Carriers of Ropinirole HCl for Persistent Parkinsonian Management. Trends in Drug Delivery. 2019; 6(1): 14–23p.