LIPOSOMAL ACETYLCYSTEINE FORMULATION: PREPARATION AND ANALYSIS

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DOI: https://doi.org/None
Issue: 
4
Year: 
2016

O.A. Kulikov, MD; V.P. Ageev; Professor V.I. Inchina, MD; O.V. Minaeva, MD; E.A. Repina, MD N.P. Ogarev Mordovian State University; 68, Bolshevistskaya St., Saransk 43005, Russian Federation

Background. Liposomal acetylcysteine is recommended for the protection of lung tissue from different pathogenic exposures. Objective: to design a liposomal acetylcysteine (ACC) formulation and to carry out its quantitative analysis using two methods. Material and methods. Liposomes were obtained by the lecithin-cholesterol phase inversion method. ACC was encapsulated by the passive loading technique. Spectrophotometry was used to measure the content of ACC in the liposomes. The size of liposomal vesicles was determined by dynamic light scattering by means of a NANO-flex nanosizer. A dialysis method was applied to purify liposomal dispersion from liposomal unencapsulated ACC. Results. The finished drug Fluimucil was employed to prepare a liposomal ACC formulation. The efficiency of liposomal ACC encapsulation was quantified by two methods using spectrophotometry. The encapsulation efficiency was 13.7325±0.392%. Conclusion. The liposomal ACC composition was chosen, in which the efficiency of liposomal ACC encapsulation was 13.7325±0.392% and the ratio of encapsulated ACC to lecithin was 0.412.
Keywords: 
liposomes
acetylcysteine
concentration
spectrophotometry
References: 
  1. Mitsopoulos P., Suntres Z. E. Protective Effects of Liposomal N-Acetylcysteine against Paraquat-Induced Cytotoxicity and Gene Expression. Journal of Toxicology, 2011; 2011: 1–14.
  2. Suntres Z. E. Role of antioxidants in paraquat toxicity. Toxicology, 2002; 180(1): 65–77.
  3. Stone W.L., Smith M. Therapeutic Uses of Antioxidant Liposomes. Molecular Biotechnology, 2004; 27 (3): 217–30.
  4. Hoesel L.M., Flierl M.A., Niederbichler A. D. Ability of antioxidant liposomes to prevent acute and progressive pulmonary injury. Antioxidants & Redox Signaling, 2008; 10(5): 973–81.
  5. Bailey M.M., Berkland C.J. Nanoparticle formulations in pulmonary drug delivery. Medicinal Research Reviews, 2009; 29(1):196–212.
  6. Mitsopoulos R., Omric A., Alipourc M., Vermeulena N., Smithd M.G., Suntresa Z.E. Effectiveness of liposomal-N-acetylcysteine against LPS-induced lung injuries in rodents. International Journal of Pharmaceutics, 2008; 363 (1–2): 106–11.