High efficiency entrapment of superoxide dismutase into mucoadhesive chitosan-coated liposomes

Superoxide dismutase (SOD), antioxidative enzyme and potential anti-inflammatory agent, was encapsulated into mucoadhesive chitosan-coated liposomes in order to increase its releasing time and to facilitate its cellular penetration. Positively, neutrally and negatively charged liposomes were prepared using soybean lecithin, stearylamine, phosphatidyl glycerol and cholesterol. The effects of liposomal lipid composition and protein to lipid ratio on the encapsulation parameters were studied in three preparation methods: dehydration-rehydration, hydration and proliposome methods. The highest efficiency of SOD entrapment, 39-65%, was achieved by the proliposome method. Vesicles prepared by the hydration method entrapped 1-13% and vesicles prepared by dehydration-rehydration entrapped 2-3% of SOD. Stability tests for SOD-loaded liposomes prepared by the proliposome method showed no significant loss of the enzyme activity within 1 month at 4degreesC or within 2 days at 37 degreesC. Positively, neutrally and negatively charged liposomes, prepared by the proliposome method, were successfully coated with two types of low and medium molecular weight chitosans. Both types of chitosan coating increased the mucoadhesive characteristics of all three types of vesicles. Using the proliposome method and subsequent chitosan coating, highly efficient SOD-loaded vesicles for drug targeting on mucosal tissues could be produced. (C) 2002 Elsevier Science B.V. All rights reserved.