DSPC Liposomes Improve Transport of L-cysteine and Reduce Metabolic Activity

RAMIRO M. PERROTTA; SILVIA DEL VALLE ALONSO; NADIA S. CHIARAMONI; M. JIMENA PRIETO

British Biotechnology Journal

SCIENCEDOMAIN international

Año: 2016 vol. 12 p. 1 - 11

Aims: In this work, we developed and characterized liposomal formulations that encapsulate Lcysteineto study their further application in drug delivery and amino acid supplementation. Thelipids used were 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), 1,2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC).Methodology: Encapsulation efficiency and amino acid release were determined. For biophysicalcharacterization of the three formulations, the size, surface charge and surface packing were alsostudied. Cell viability was analyzed with MTT reagent after treatments with formulations ir order tostudy efficiency of these systems in induce changes in metabolism.Results: Results showed that L-cysteine interacts at the polar head level and that this interactionstabilizes the surface charge and prevents aggregation. We also determined the influence on cellmetabolism in all formulations. The presence of L-cysteine in the DSPC formulation induced deeperchanges in metabolism, evidencing that this formulation provides better transport of this aminoacid.Conclusion: Liposomes developed herein are well suited for the application in the delivery ofL-cysteine. Particularly, they can encapsulate nearly all the L-cysteine and can retain it for 6 hours.Also, L-cysteine stabilized liposomes, preventing their aggregation. L-cysteine encapsulated in theDSPC formulation induced deeper changes in cell metabolism, causing a decrease in metabolicactivity; this was probably due to a higher entry, thus a better liposome-mediated transport.Considering that the smaller the particle, the better the circulation, we believe that the stabilizationof the vesicle by L-cysteine may allow these transporters to have higher circulation times. Based onthe above, we conclude that the DSPC formulation is the best suited for further application inL-cysteine delivery.