Abstract
Liposomes loaded with drug–cyclodextrin complexes are widely used as drug delivery systems, especially for species with low aqueous solubility and stability. Investigation of the intimate interactions of macrocycles with liposomes are essential for formulation of efficient and stable drug-in-cyclodextrin-in-liposome carriers. In this work, we reported the preparation of unilamellar vesicles of 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC) embedded with native β-cyclodextrin and two synthetic derivatives: heptakis(2,3,6-tri-O-methyl)-β-cyclodextrin (TMCD) and heptakis(2,3-di-O-acetyl)-β-cyclodextrin (DACD). We then studied the effect of these macrocycles on the liposomal size, membrane viscosity, and liposomal stability at different temperatures and concentrations. We observed that TMCD and DACD affected vesicle size and the change of size was related to CD concentration. Irrespective of its nature, the macrocycle established interactions with the phospholipidic head groups, preventing cyclodextrins to diffuse into the lipid bilayer, as confirmed by molecular dynamics simulations. Such supramolecular structuring improves liposome stability making these colloid systems promising carriers for biologically active compounds.
Highlights
Nanocarriers are able to change the physicochemical properties of the incorporated molecules, affect the pharmacokinetic profiles of embedded drugs, as well as allow the incorporated molecules to overcome biological barriers
On addition of CDs the size of liposomes slightly increases.ofThis to break and solubilize liposomes has beentodemonstrated for concentrations
Functionalized CDs were embedded into POPC liposomes at different concentrations and the obtained colloidal systems were characterized from various points of view
Summary
Nanocarriers are able to change the physicochemical properties of the incorporated molecules, affect the pharmacokinetic profiles of embedded drugs, as well as allow the incorporated molecules to overcome biological barriers. Liposomes are spherical lipid vesicles formed in aqueous solution by phospholipid molecules organized in bilayers enclosing an aqueous compartment These aggregates are useful in biological, biomedical, and biotechnological applications as drug delivery systems due to their extraordinary capacity to encapsulate hydrophilic drugs in the aqueous core and to trap lipophilic compounds within the membrane [2]. Molecules 2019, 24, 1387 to overcome this problem, in 1994, McCormack and Gregoriadis engineered, for the first time, the possibility of forming a combined system of cyclodextrins (CDs) and liposomes called drug-in-cyclodextrin-in-liposomes (DCLs) [3]. The comprehensive experimental and theoretical results allowed us to clarify the behavior of DLCs and tune and optimize the DCLs formulation
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