title: Self-assembling systems based on quaternized derivatives of 1,4-diazabicyclo[2.2.2]octane in nutrient broth as antimicrobial agents and carriers for hydrophobic drugs.
abstract: Aggregation properties of mono (mono-CS) and dicationic (di-CS) surfactants, namely quaternised derivatives of 1,4-diazabicyclo[2.2.2]octane (DABCO), have been evaluated in water and in nutrient broths of different pH, i.e. in Hottinger broth (рН=7.2) and Sabouraud dextrose broth (рН=5.6). Aggregation capacity of surfactants was shown to be responsible for the solubilization properties of a complex composed of a hydrophobic probe (Sudan I) and a selected drug (quercetin), contributing to the antimicrobial activity of this surfactant system. The effect of N-methyl-d-glucamine (NmDg) additive on the antimicrobial activity of mono-CS, and its aggregation and solubilization parameters, has also been evaluated. A substantial decrease in critical micelle concentration (CMC) of cationic surfactants in nutrient broths (up to 60 times) has been reported. Twofold dilution of monocationic surfactant by NmDg slightly changed the CMC of surfactant; however, it provided a remarkable increase in solubilization capacity (∼by 4 times) and decrease in its toxicity. The data anticipate the potential use of DABCO quaternized derivatives as innovative non-toxic delivery systems for hydrophobic drugs.
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
authors: Tatiana N
authors: TN
authors: Pashirova
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
authors: Svetlana S
authors: SS
authors: Lukashenko
authors: Kazan State Technological University, ul. Karla Marksa 68, Kazan, 420015, Russian Federation.
authors: Sergey V
authors: SV
authors: Zakharov
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
authors: Alexandra D
authors: AD
authors: Voloshina
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
authors: Elena P
authors: EP
authors: Zhiltsova
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation.
authors: Vladimir V
authors: VV
authors: Zobov
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Center for Neuroscience and Cell Biology (CNC), Faculty of Medicine, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal. Electronic address: ebsouto@ff.uc.pt.
authors: Eliana B
authors: EB
authors: Souto
authors: A.E Arbuzov Institute of Organic and Physical Chemistry, Kazan Scientific Center, Russian Academy of Sciences, 8, ul. Arbuzov, 420088 Kazan, Russian Federation; Kazan State Technological University, ul. Karla Marksa 68, Kazan, 420015, Russian Federation.
authors: Lucia Ya
authors: LY
authors: Zakharova
mesh_terms: D016880:Anisotropy; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology; D002176:Candida albicans / Q000187:drug effects; D002412:Cations; D003470:Culture Media; D004337:Drug Carriers; D005453:Fluorescence; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D057446:Hydrodynamics; D057927:Hydrophobic and Hydrophilic Interactions; D008823:Micelles; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D011794:Quercetin / Q000737:chemistry; D012996:Solutions; D013211:Staphylococcus aureus / Q000187:drug effects; D013500:Surface Tension; D013501:Surface-Active Agents / Q000737:chemistry; D013696:Temperature
chemical_list: D000890:Anti-Infective Agents; D002412:Cations; D003470:Culture Media; D004337:Drug Carriers; D008823:Micelles; D004364:Pharmaceutical Preparations; D010879:Piperazines; D012996:Solutions; D013501:Surface-Active Agents; D011794:Quercetin; C007306:triethylenediamine
keywords: 1,4-diazabicyclo[2.2.2]octane; Drug delivery systems; N-methyl-d-glucamine; Surfactants; Toxicity; quercetin