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Lipid-based supramolecular systems for topical application: A preformulatory study

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Abstract

This article describes the production and characterization of monoglyceride-based supramolecular systems by a simple processing technique, avoiding time-consuming procedures, high energy input, and the use of organic solvents. A preformulatory study was performed to study the influence of the experimental parameters on the production of monoglyceride-based disperse systems. In particular the effects of (1) stirring speed, (2) type and concentration of monoglyceride mixture, and (3) type and concentration of surfactant were investigated on the recovery, fraction of larger particles, mean diameter, and shape of smaller particles (so called nanosomes). Dispersions were first characterized by optical microscopy and freeze-fracture electron microscopy. The mean diameter of standard nanosomes, analyzed by photon correlation spectroscopy (PCS) after elimination of larger particles by filtration, was 193.5 nm. Cryotransmission electron microscopy studies, conducted in order to investigate the structure of dispersions, showed the coexistence of vesicles and particles characterized by a cubic organization. X-ray diffraction data revealed the coexistence of 2 different cubic phases, the first being a bicontinuous cubic phase of spatial symmetry Im3m (Q229) and the second belonging to the Pn3m spatial symmetry. A study on the stability of monoglyceride-based dispersions based on macroscopical analysis of organoleptic properties and dimensional analysis by time was performed after elimination of larger particles by filtration. Organoleptic and morphological features do not change by time, appearing free from phase-separation phenomena for almost 1 year from production. PCS studies showed that nanosomes undergo an initial increase in mean diameter within the first month following production; afterwards they generally maintain their dimensions for the next 4 months.

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Authors and Affiliations

  1. Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara, 19, I-44100, Ferrara, Italy

    Elisabetta Esposito, Nadia Eblovi, Enea Menegatti & Rita Cortesi

  2. Institute für Polymere, ETH Zentrum, Zürich, Switzerland

    Silvia Rasi

  3. Macromolecular Chemistry II, University of Bayreuth, Germany

    Markus Drechsler

  4. Dipartimento di Scienze Applicate ai Sistemi Complessi e INFM, Università Politecnica delle Marche, Ancona, Italy

    Giordano M. Di Gregorio

Authors
  1. Elisabetta Esposito
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  2. Nadia Eblovi
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  3. Silvia Rasi
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  4. Markus Drechsler
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  5. Giordano M. Di Gregorio
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  6. Enea Menegatti
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  7. Rita Cortesi
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Correspondence to Elisabetta Esposito.

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Published: November 18, 2003

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Esposito, E., Eblovi, N., Rasi, S. et al. Lipid-based supramolecular systems for topical application: A preformulatory study. AAPS PharmSci 5, 30 (2003). https://doi.org/10.1208/ps050430

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  • DOI: https://doi.org/10.1208/ps050430

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