Nanotechnology Based Drug Delivery System Of Rivastigmine For The Treatment Of Alzheimer’s Disease

Abstract

Rivastigmine is the important drug used in the treatment of Alzheimer’s disease and it is a reversible cholinesterase inhibitor [1]. Rivastigmine is very poor bioavailability through oral route, to overcome these problems Rivastigmine nanoparticles were prepared and administered through route of intranasal passage. Nasal drug delivery systems are having many advantages like rapid onset of action, less side effects to cross the blood-brain barrier Nano formulations plays an important role and great potential to analyse the limitations of the neurodegenerative diseases and many other diseases. Novel Nano formulations used in this method were developed and successfully optimized with many parameters for the treatment of Alzheimer’s disease [2]. At a specific concentration of 1% P80 mixed with chitosan, drug was dissolved within this study. There is no toxic effect for this formulation. Rivastigmine-loaded chitosan nanoparticles were successfully optimized using at a specific concentration of 1% P80 mixed with chitosan. Optimization was done by taking formulation variables such as taking various concentrations of polymer, drug, cross linking agent, surfactant, cross linking time, stirring speed. Coated nanoparticles showed particle size is less than 200nm and rivastigmine permeation is more in invitro drug permeation indicating nasal sheep. Rivastigmine nanoparticles are prepared to avoid the poor bioavailability and to increase the bioavailability, safety and efficacy

Chitosan is very important in its nature as polycation [3] and its charge density depends on the degree of acetylation and pH of the media. acetylation degree and molecular weight decides the polymer solubility. EUDRAGIT NE 30 D is the aqueous dispersion of a neutral polymer based on ethyl acrylate and methyl methacrylate. Important features to choose EUDRAGIT NE 30 D is no need to add plasticizer, highly flexible and Suitable for matrix structure. Eudragit NE 30 D contains α-(4-nonylphenyl) ω-hydroxypoly-(oxy-1, 2-ethanediyl), namely nonoxynol 100 (1.5%). Talc addition is required to avoid tackiness and agglomeration of the coated pellets. Melting point (~ 60°C) is high, due to this nature leads to increase in drug release. Due to the excellent mucoadhesive properties [4] of EUDRAGIT NE 30 D extends the contact time between drug and mucus layer, disruption of tight junctions, permeation increases and prolong the duration of action, respectively. Current studies are investigating to develop mucoadhesive rivastigmine loaded in chitosan and coated with EUDRAGIT NE 30 D for intranasal delivery, which is useful for the first-pass metabolism of drugs, help to achieve a sustained drug release over a prolonged period. Based on the review of literature this is the first study by coating with EUDRAGIT NE 30 D where rivastigmine was loaded with chitosan. By taking many different types of formulation and parameters, method was optimized to obtain chitosan nanoparticles with achieving the quality. other polymer also used for nose to brain delivery is poly (lactic -co-glycolic acid)

These developed Nano formulations showed significant difference when compared with free drug. This novel method of approach has enhanced the Nano formulations. stability. Finally, these formulations may hold the potential to contribute to develop an effective treatment of AD [5]. If intranasally administered, drugs survive the mucociliary clearance in the vestibular region, move to the posterior regions of nasal cavity and contact with respiratory epithelium in the respiratory region. Some of them are absorbed through the epithelium into the blood or the lymphatic system, being subsequently transported into the systemic circulation.[6].