Evaluation of the use of ascorbyl derivatives as membrane liposomes stabilizers.

BENEDINI, L.; ANTOLLINI, S.S.

Córdoba

Congreso; 3era Reunión Internacional de Ciencias Farmacéuticas; 2014

The aim of this work was to compare the biophysical properties of liposomes of DMPC containing Asc16 with those containing Asc10 and also to predict by DLVO theory their properties when other drugs are added to the membrane. Results The ascorbyl derivatives up to 30% did not disturb the membrane order of DMPC liposomes, as evaluated by the calculation of the Generalized Polarization (GP) using the fluorescence probe Laurdan, neither did they modify the DMPC liposome size (~ 150 nm), as calculated by DLVO theory. Thus, all the studied liposomes were stable. Their presence conducted to more negative zeta potential (ζ) values: Asc16 developed a lower ζ than Asc10 (-16.7 mV and - 9.98 mV respectively). Considering the calculated DLVO potential, the stabilization of DMPC liposomes by addition of Asc10 is predictably lower than Asc16, and hence, more Asc10 will be needed to stabilize the membrane. Conclusions The addition of Asc10 or Asc16 to liposomes of DMPC does not disturb the phases of the membrane. However, the stabilization of DMPC liposomes by addition of Asc10 is lower than Asc16. It is important to consider that under experimental conditions (pH ~ 6), both derivatives were negatively charged. Thus, it is expected that if a positively charged drug is inserted into the liposome membrane, a less negative ζ will occur and, consequently, the destabilization of the system will be higher. Therefore, we suggest that the incorporation of active molecules that could reduce the DLVO potential of DMPC liposomes could be accompanied by either Asc10 or Asc16. However, considering these results, the Asc16 will be better than Asc10 to stabilize the liposome membrane.