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pH-responsive lyotropic liquid crystals for controlled drug delivery.

Renata Negrini1, Raffaele Mezzenga

  • 1Food and Soft Materials Science, Institute of Food, Nutrition and Health, Eidgenössische Technische Hochschule Zürich, Schmelzbergstrasse 9, CH-8092 Zürich, Switzerland.

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This pH-responsive food-grade liquid crystal system transitions between cubic and hexagonal phases. It enables controlled drug release, with faster release in the cubic phase at neutral pH for targeted intestinal delivery.

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Area of Science:

  • Materials Science
  • Biomedical Engineering
  • Physical Chemistry

Background:

  • Lyotropic liquid crystals offer tunable properties for drug delivery.
  • pH-responsive materials are crucial for targeted oral administration.
  • Understanding phase transitions is key to controlling release kinetics.

Purpose of the Study:

  • To develop a food-grade lyotropic liquid crystal system responsive to pH changes.
  • To investigate the reversible structural and property switches induced by pH variations.
  • To evaluate the system's efficacy as a controlled-release vehicle for hydrophilic drugs.

Main Methods:

  • Formulation of a monolinolein and linoleic acid system in water.
  • Induction of phase transitions (Im3m to H(II)) by altering pH from 7 to 2.
  • Controlled release studies of phloroglucinol using UV-Vis spectroscopy.
  • Analysis of critical packing parameter (CPP) changes due to pH-induced protonation of linoleic acid.

Main Results:

  • The system reversibly switched from Im3m cubic to H(II) hexagonal phase upon pH change.
  • Linoleic acid's protonation state modulated the CPP, driving the phase transition.
  • Phloroglucinol release was approximately four times faster from the Im3m cubic phase (pH 7) than the H(II) phase (pH 2).

Conclusions:

  • The developed lyotropic liquid crystal system demonstrates effective pH-triggered structural changes.
  • The system shows potential as a controlled-release vehicle for oral drug delivery.
  • Targeted delivery to the intestine or colon is feasible due to differential release rates at varying pH.