International Journal of Pharmaceutical Investigation, 2020, 10, 4, 553-558.
DOI: 10.5530/ijpi.2020.4.96
Published: December 2020
Type: Original Article
Authors:
Srinivas Hebbar
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Mangaluru, Karnataka, INDIA.
Manasa Poonja
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Mangaluru, Karnataka, INDIA.
Amitha Shetty
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Mangaluru, Karnataka, INDIA.
Akhilesh Dubey
Department of Pharmaceutics, NGSM Institute of Pharmaceutical Sciences, NITTE (Deemed to be University), Mangaluru, Karnataka, INDIA.
ABSTRACT
Objectives: The main objective of the present investigation was to develop and compared conventional, chitosan-coated and electrosteric stealth liposomes of Rivastigmine Tartrate for the treatment of Alzheimer’s Disease. Methods: The solvent evaporation method was employed to prepare liposomes and optimized by the Design of Experiment approach. The effect of various process parameters was investigated and optimized on for particle size and percentage entrapment efficiency. The compatibility studies were carried out using Fourier Transform Infrared Spectroscopy. The optimized formulations were also characterized by Transmission Electron Microscopy and Atomic Force Microscopy for their surface morphology and in vitro percentage drug release study by comparing it with a standard solution of Rivastigmine Tartrate. The compatibility of drug and excipient mixtures was confirmed by Fourier Transform Infrared Spectroscopy. Results: The optimized formulation of conventional, chitosan-coated, stealth liposome of Rivastigmine Tartrate showed vesicle size of 111.8, 153.3, 136.3 nm respectively and entrapment efficiency of 75.27±0.8 %, 80.33±0.4 % 78.2±0.2 respectively. Clear surface morphology was observed through surface morphological images. The in vitro drug release studies showed a significant difference in percentage cumulative drug release pattern of chitosan-coated and stealth liposomes (81±0.3 % and 76±1.2 %) when compared with the conventional liposomes (69±0.8 %), after 24 h. On subjecting it to stability studies, the liposome preparations did not show any significant changes in particle size and entrapment efficiency. Conclusion: The developed formulations (chitosan-coated and stealth liposomes) can deliver the active moiety on the target site for the treatment of AD.
Keywords: Alzheimer’s disease, Rivastigmine tartrate, Liposome, Chitosan, Stealth.