title: Influence of serum albumin on intracellular delivery of drug-loaded hyaluronan polymeric micelles.
abstract: Polymeric micelles are attractive drug delivery systems for intravenously administered nonpolar drugs. Although physical parameters like size, shape and loading capacity are considered as the most important for their efficiency, here we demonstrate that the effects of serum protein interaction and characteristics of loaded compound cannot be neglected during the micelle development and design of experimental set up. Polymeric micelles prepared from amphiphilic hyaluronic acid grafted with short (hexanoic) and long fatty acids (oleic) were tested after loading with two different hydrophobic models, Nile red and curcumin. The composition of micelles affected mainly the loading capacity. Both encapsulated compounds behaved differently in the in vitro cell uptake, which was also influenced by serum concentration, where serum albumin was found to be the primary destabilizing component. This destabilization was found to be influenced by polymeric micelle concentration. Thus, the chemical structure of micelle, the properties of non-covalently loaded substance and serum albumin/polymeric micelle ratio modulate the in vitro intracellular uptake of drugs loaded in nanocarriers.
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic; Department of Experimental biology, Faculty of Sciences, Masaryk University, Kotláſská 267/2, 611 37 Brno, Czech Republic.
authors.forename: Kristina
authors.initials: K
authors.lastname: Nešporová
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic.
authors.forename: Jana
authors.initials: J
authors.lastname: Šógorková
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic. Electronic address: daniela.smejkalova@contipro.com.
authors.forename: Daniela
authors.initials: D
authors.lastname: Šmejkalová
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic.
authors.forename: Jaromír
authors.initials: J
authors.lastname: Kulhánek
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic.
authors.forename: Gloria
authors.initials: G
authors.lastname: Huerta-Angeles
authors.affiliation: Department of Experimental biology, Faculty of Sciences, Masaryk University, Kotláſská 267/2, 611 37 Brno, Czech Republic; Institute of Biophysics, Academy of Sciences of the Czech Republic, Královopolská 135, 612 65 Brno, Czech Republic; International Clinical Research Center, St. Anne⿿s University Hospital, Pekaſská 53, 656 91 Brno, Czech Republic.
authors.forename: Lukáš
authors.initials: L
authors.lastname: Kubala
authors.affiliation: Contipro a.s., Dolní DobrouĿ 401, 561 02 Dolní DobrouĿ, Czech Republic.
authors.forename: Vladimír
authors.initials: V
authors.lastname: Velebný
mesh_terms: D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D004337:Drug Carriers / Q000008:administration & dosage / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods; D045325:HCT116 Cells; D019073:HT29 Cells; D006801:Humans; D006820:Hyaluronic Acid / Q000008:administration & dosage / Q000378:metabolism*; D007424:Intracellular Fluid / Q000187:drug effects / Q000378:metabolism*; D008823:Micelles; D011108:Polymers / Q000008:administration & dosage / Q000378:metabolism*; D011485:Protein Binding / Q000502:physiology; D012709:Serum Albumin / Q000008:administration & dosage / Q000378:metabolism*
chemical_list: D004337:Drug Carriers; D008823:Micelles; D011108:Polymers; D012709:Serum Albumin; D006820:Hyaluronic Acid
keywords: Albumin; Cell uptake; Fatty acid; Hyaluronan; Polymeric micelle; Stability