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Conjugation of Squalene to Acyclovir Improves the Affinity for Biomembrane Models by Maria Grazia Sarpietro; Dorotea Micieli; Flavio Rocco; Maurizio Ceruti; Francesco Castelli is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

What is Conjugation of Squalene to Acyclovir Improves the Affinity for Biomembrane Models about?

Differential scanning calorimetry was used to study the interaction of acyclovir and its prodrug squalenoyl-acyclovir (obtained by conjugation of 1,1 ,2-tris-nor-squalene acid (squaleneCOOH) with acyclovir) with biomembrane models made of DMPC multilamellar vesicles with the aim to verify whether a stronger interaction of the prodrug with respect to the free drug can be obtained. Multilamellar vesicles were prepared in the presence of increasing molar fractions of acyclovir, squaleneCOOH or prodrug and the effect of the compounds on the thermotropic behavior of vesicles was researched, revealing no effect of acyclovir but a strong effect of squaleneCOOH and prodrug. To evaluate if acyclovir, squaleneCOOH and prodrug can be absorbed by the biomembrane model, an experiment was carried out in which the considered compounds were left in contact with the biomembrane model and their eventual uptake was evaluated analyzing the effect on the thermotropic behavior of the biomembrane model. A very small uptake was revealed for all the compounds. To check the potential use of liposomes as a delivery system for the prodrug, the biomembrane models were incubated with liposomes loaded with the c

Who reads Conjugation of Squalene to Acyclovir Improves the Affinity for Biomembrane Models?

Author

Maria Grazia Sarpietro; Dorotea Micieli; Flavio Rocco; Maurizio Ceruti; Francesco Castelli

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 0378-5173)

Published

2009

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)