Abstract
Background: The effect of different concentrations of the absorption enhancer Trimethyl Chitosan (TMC) to the physicochemical properties of Large Unilamellar Vesicles (LUV) comprised of L-a-Phospahtidyl Choline (PC) were investigated in the current study. Methods: The Degree of Quartenization (DQ) of trimethylchitosan was assessed with nuclear magnetic resonance (1H NMR). The vesicles were characterized by means of Dynamic Light Scattering (DLS), ζ-potential, Differential Scanning Calorimetry (DSC) and Contact Angle Goniometry (CAG) measurements. Results: The data showed that the surface charge of the PC liposomes was significantly altered as a function of the TMC concentration, giving evidence of presence of the polyelectrolyte to the liposome’s membrane. Varying the concentration of TMC affected the phase Transition Temperature (Tm) of the lipid, verifying the miscibility of the polyelectrolyte with the lipid bilayer. The association of the polymer with the liposomes was related to the amount of the polyelectrolyte present, reflecting changes to the wettability of the dispersion as measured by CAG. Conclusion: The results demonstrated that presence of TMC significantly modified the physical properties of liposomes. Such systems might have a potential use for mucosal delivery (e.g. nasal route of administration).
Highlights
The use of colloidal drug delivery systems, such as nanoparticles and liposomes, has been shown to increase the bioavailability of administered drugs (REF)
The vesicles were characterized by means of Dynamic Light Scattering (DLS), ζ-potential, Differential Scanning Calorimetry (DSC) and Contact Angle Goniometry (CAG) measurements
The data showed that the surface charge of the Phospahtidyl Choline (PC) liposomes was significantly altered as a function of the Trimethyl Chitosan (TMC) concentration, giving evidence of presence of the polyelectrolyte to the liposome’s membrane
Summary
The use of colloidal drug delivery systems, such as nanoparticles and liposomes, has been shown to increase the bioavailability of administered drugs (REF). Liposomes, which are vesicles, composed of one or more phospholipid bilayers can carry a variety of molecules with therapeutic potential and offer different advantages for many routes of administration [1]. Liposomes decorated with polyelectrolytes, alter their properties, are extensively used as drug carriers [2, 3] and have been shown to increase their therapeutic activity and circulation lifetime in a biological milieu [4]. A solid polymeric vesicle, namely palmitoyl glycol chitosan, was entrapped within a liposomal formulation to control the release profiles of a model compound [8]. The results showed that the polymeric vesicle phospholipid in vesicle system released 28% of the entrapped model compound compared to 62% from the polymeric vesicles over the duration of 4 hours [8]. The effect of different concentrations of the absorption enhancer Trimethyl Chitosan (TMC) to the physicochemical properties of Large Unilamellar Vesicles (LUV) comprised of L-a-Phospahtidyl Choline (PC) were investigated in the current study
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