INVESTIGADORES
CHIARAMONI Nadia Silvia
artículos
Título:
Lipid-Polymer Membranes as Carriers for L-tryptophan: Molecular and metabolic Properties
Autor/es:
FERNÁNDEZ RUOCCO, MARÍA JULIETA; SIRI, MACARENA; IGARTÚA, DANIELA; PRIETO, MARIA JIMENA; ALONSO, SILVIA DEL VALLE; CHIARAMONI, NADIA SILVIA
Revista:
Open Journal of Medicinal Chemistry
Editorial:
Scientific Research Publishing (SCIRP)
Referencias:
Lugar: Delaware, USA; Año: 2013 vol. 3 p. 31 - 39
ISSN:
2164-3121
Resumen:
Polymerized liposomes
encapsulating L-tryptophan were studied with the aim to characterize them as
drug delivery systems for the treatment of several metabolic diseases that need
an increased systemic L-tryptophan concentration. polymerized liposomes were
obtained by UV irradiation of vesicles containing
1,2-bis(10,12-tricosadiynoyl)-sn-glycero-3-phosphocholine (DC8,9PC) and
1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC) in a 1:1 molar ratio, in the
presence of 10 and 50 mol% of L-tryptophan (respect to total lipid
concentration). Polymerization efficiency was studied spectrophotometrically. Also, bilayer packing at
the polar head region was followed with the Merocyanine 540 (MC540) and
specific interactions in the lipopolymers were studied by FTIR. High L-tryptophan
concentrations (50 mol% respect to total lipid concentration) induced a higher
amount of six- and nine-unit polymers. This phenomenon was induced because the
L-tryptophan located outside the lipid membrane was included in it during the
polymerization process and was thus responsible for the better accommodate of
the polar head region. This was not possible with the lower amount of L-tryptophan
(10 mol%). The stability of lipopolymers with different amounts of L-tryptophan
was studied through release profiles. Polymerized liposomes with 50 mol% of
L-tryptophan were able to retain around 80% of the amino acid after 24 hours, whereas
those with 10 mol % of the amino acid were able to retain 20%. The metabolic activity of the
Caco-2 cell line was also studied. Cytotoxic effects were low in the presence
of polymerized liposomes,
rendering a maximum percentage of cell death of 30%. In summary, this work
stresses the relevance of nonspecific drug-polymerized membrane binding on
L-tryptophan pharmacological interaction with possible pharmaceutical
applications in liposomal drug delivery. Moreover, the absence of significant
cytotoxic effects allows the system proposed to be applied in human health.