Preparation and Characterization of Rivastigmine Loaded Human Serum Albumin (HSA) Nanoparticles

Amelia   M.   Avachat; Yogesh   M.   Oswal; Kishor   N.   Gujar; Rohit   D.   Shah

doi:10.2174/15672018113109990050

Abstract

The aim of the present study was to develop and characterize rivastigmine loaded Human Serum Albumin (HSA) nanoparticles (NPs) for sustained release. Rivastigmine tartrate (RT) is a short acting cholinesterase inhibitor (ChEI) used for Alzheimer’s disease (AD). In the present study sustained release nanoparticulate formulation of RT was prepared, optimized (using 32 factorial design) and characterized (using biodegradable polymer HSA as a carrier). HSA NPs were prepared by desolvation-crosslinking technique using ethanol with variable drug/polymer ratios (1:1, 1:2, 1:3, and 1:5) and using glutaraldehyde as a crosslinking agent. All prepared nanoparticles were coated with polysorbate-80 to facilitate brain targeting via endocytosis. Effect of key formulation variables on particle size (PS) and percentage drug entrapment (PDE) of NPs was studied by using 32 factorial design. Among different ratios studied, 1:2 showed minimum PS of 83.71 ± 4.2 nm with highest PDE of 81.46 ± 0.76 %. FTIR interpretation showed that there is no interaction between the drug and excipients used, DSC thermograms indicated that RT was dispersed as an amorphous state in HSA NPs. SEM studies indicated that the drug was completely entrapped in HSA NPs. In vitro studies showed 55.59 ± 3.80% release of drug from HSA NPs in 12 h. The experimental results showed the suitability of HSA nanoparticles as a potential carrier for providing sustained delivery of RT.

Keywords: Desolvation-Crosslinking, Factorial design, Human Serum Albumin (HSA) nanoparticles, Rivastigmine Tartrate, Sustained release.

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