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      Cubic and Hexagonal Liquid Crystals as Drug Delivery Systems

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          Abstract

          Lipids have been widely used as main constituents in various drug delivery systems, such as liposomes, solid lipid nanoparticles, nanostructured lipid carriers, and lipid-based lyotropic liquid crystals. Among them, lipid-based lyotropic liquid crystals have highly ordered, thermodynamically stable internal nanostructure, thereby offering the potential as a sustained drug release matrix. The intricate nanostructures of the cubic phase and hexagonal phase have been shown to provide diffusion controlled release of active pharmaceutical ingredients with a wide range of molecular weights and polarities. In addition, the biodegradable and biocompatible nature of lipids demonstrates the minimum toxicity and thus they are used for various routes of administration. Therefore, the research on lipid-based lyotropic liquid crystalline phases has attracted a lot of attention in recent years. This review will provide an overview of the lipids used to prepare cubic phase and hexagonal phase at physiological temperature, as well as the influencing factors on the phase transition of liquid crystals. In particular, the most current research progresses on cubic and hexagonal phases as drug delivery systems will be discussed.

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          Cubic lipid-water phases: structures and biomembrane aspects

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            Surfactant self-assembly objects as novel drug delivery vehicles

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              pH-responsive lyotropic liquid crystals for controlled drug delivery.

              We present a food-grade lyotropic liquid crystal system, capable of responding to pH variations with a reversible switch in both the structure and physical properties. The system, which is composed by monolinolein and linoleic acid (97:3 wt % ratio) in the presence of excess water at 37 °C and 150 mM ionic strength, is specifically designed to reversibly change from a Im3m reverse bicontinuous cubic phase to a H(II) reverse columnar hexagonal phase, when changing the pH from neutral (pH 7) to acidic (pH 2) conditions, to simulate intestine and stomach conditions, respectively. The pH responsiveness is provided by the linoleic acid, which, being a weak acid (pK(a) ≈ 5), is essentially in the deprotonated charged state at pH 7 and mainly protonated and neutral at pH 2, imposing changes in the critical packing parameter (CPP) of the lyotropic liquid crystal. The use of this system as an efficient controlled-release delivery vehicle is demonstrated on the model hydrophilic drug phloroglucinol, by both release and diffusion studies at different pH, as followed by ultraviolet-visible (UV-vis) spectroscopy. The Im3m cubic phase at pH 7 is shown to release 4 times faster than the H(II) phase at pH 2, making this system an ideal candidate for oral administration of drugs for targeted delivery in intestine or colon tracts.
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                Author and article information

                Journal
                Biomed Res Int
                Biomed Res Int
                BMRI
                BioMed Research International
                Hindawi Publishing Corporation
                2314-6133
                2314-6141
                2014
                5 June 2014
                : 2014
                : 815981
                Affiliations
                1Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, Hefei, Anhui 230031, China
                2Global Pharmaceutical Research and Development, Hospira Inc., 1776 North Centennial Drive, McPherson, KS 67460, USA
                3Anhui Key Laboratory of Modern Chinese Medicine & Materia, Hefei, Anhui 230031, China
                4Anhui “115” Xin'an Traditional Chinese Medicine Research & Development Innovation Team, Hefei, Anhui 230031, China
                Author notes

                Academic Editor: Sergio Murgia

                Article
                10.1155/2014/815981
                4068036
                24995330
                918fbd63-2ba9-40bd-9d35-699ee3770181
                Copyright © 2014 Yulin Chen et al.

                This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

                History
                : 27 February 2014
                : 22 May 2014
                Funding
                Funded by: http://dx.doi.org/10.13039/501100001809 National Natural Science Foundation of China
                Award ID: 81274099
                Funded by: Natural Science Foundation of Anhui Province
                Award ID: 11040606M219
                Funded by: Natural Science Foundation of the Anhui Higher Education Institutions of China
                Award ID: KJ2012A184
                Funded by: Foundation of Anhui University of Chinese Medicine
                Award ID: 201303
                Categories
                Review Article

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