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Research Article

L-cysteine encapsulation in liposomes: Effect of phospholipids nature on entrapment efficiency and stability

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Pages 399-413 | Received 16 Jan 2008, Accepted 21 Feb 2008, Published online: 08 Oct 2008
 

Abstract

Liposomal entrapment of L-cysteine (L-CySH) could be a solution to enhance its oxidative stability and its intracellular bioavailability for glutathione (GSH) synthesis. This study addresses the influence of different factors (i.e. pH value (6.3 vs 7.4), antioxidant agents (EDTA or tocopherol (TO))) and nature of phosphatidylcholine (PC) (Soybean PC (SPC) vs hydrogenated SPC (HSPC)) to formulate and optimize Large Unilamellar Vesicles (LUVs) of L-CySH composed of PC/Cholesterol/Phosphatidylglycerol (6 : 3 : 1). pH decrease (p = 0.0002) and substitution of SPC by HSPC (p < 0.001) reduced L-CySH oxidation. EE% (entrapment efficiency) varied from 0.98% ± 0.54 (SPC, pH 7.4) to 6.46% ± 1.37 (HSPC, pH 6.3) and was improved by decreasing pH (p = 0.011) and using HSPC (p < 0.0001). An immediate release of L-CySH was observed with SPC. On the contrary, with HSPC at pH 6.3, 42.0% ± 1.2 and 73.0% ± 1.7 remained encapsulated after 24 h at 25°C and 4°C, respectively. In conclusion, HSPC offering both stronger rigidity and lesser propensity for peroxidation led to optimize L-CySH liposomal stability.

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