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Self-microemulsifying drug delivery system as nanosystems for bioavailability enhancement of flavonoids in vitro
e u r o p e a n j o u r n a l o f p h a r m a c e u t i c a l s c i e n c e s 3 4 S ( 2 0 0 8 ) S25–S29
NANO- AND MICROTECHNOLOGY IN PHARMACY
S29
toluene, anisole and acetone, are suitable spray solvents in DAPPI.
O14 Opportunities for digitally encoded microcarriers in pharmacy and cell-based assays
doi:10.1016/j.ejps.2008.02.074
Farzaneh Fayazpour, B. Lucas, N. Huyghebaert, K. Braeckmans, S. Derveaux, R. Vandenbroucke, J.P. Remon, J. Demeester, C. Vervaet, S. De Smedt
Self-microemulsifying drug delivery system as nanosystems for bioavailability enhancement of flavonoids in vitro
O16
Alexander Shikov, O. Pozharitskaya, M. Karlina, V. Makarov Department of Pharmaceutics, Ghent University, Belgium St-Petersburg Institute of Pharmacy, Russia Counterfeiting of drugs is a real threat to public health. “In-drug labelling” would be a major step forward to combat counterfeiters. We recommend digitally encoded microparticles, known as memobeads, for this purpose. We also use these encoded microcarriers as a “non-positional cell array”: each of these encoded microcarriers can accommodate one cell type or certain substance. This might be a powerful tool for analysis of drug targets or toxicity markers or even as a delivery system for genetic materials. We found that entrapping the memobeads in starch-based granules protects them from deformation during tabletting; even when high compression forces were applied the code in the beads did not deform. Different cell lines can grow on the beads and these cells did not hamper the decoding of the beads. Furthermore, we have proposed a method of immobilizing adenoviral vectors on encoded microcarriers, while maintaining their ability to infect cells (reversed transfection). doi:10.1016/j.ejps.2008.02.073
The goals of the present investigations are to develop and characterize self-microemulsifying drug delivery systems (SMEDDS) with different flavonoids (rutin, quercetin and dihydroquercetin), and to evaluate their bioavailability. A water-in-oil microemulsion containing 2% flavonoids, oil phase, water, surfactant, and cosurfactant were prepared. The in vitro self-microemulsification properties and droplet size analysis of these formulations upon their addition to water under mild agitation conditions were studied. Pseudo-ternary phase diagrams were constructed identifying the efficient self-micro emulsification region. The efficiency of microemulsification was good when the surfactant–cosurfactant (6:1) concentration was 20–50%. The release of flavonoids from SMEDDS form resulted in about two- to fivefold increase in bioavailability compared with the powder formulation in vitro. SMEDDS have improved the bioavailability of all tested flavonoids significantly. The data suggest the potential use of SMEDDS to provide an efficient way of improving oral absorption of lipophilic drugs–flavonoids.
O15 Desorption atmospheric pressure spectrometry in drug analysis a, ¨ Luosujarvi
Laura Saarela c , S. Kauppila b
Arvola b ,
V. Franssila c , R.
photoionization-mass
doi:10.1016/j.ejps.2008.02.075 O17
Haapala b ,
M. Kostiainen b , T.
´ b, Pol
J. V. Kotiaho a,b , T.J.
Modulation of lipidic nanostructures by designer short peptide surfactants Anan Yaghmur a , P. Laggner a , S. Zhang b , M. Rappolt a
a
Laboratory of Analytical Chemistry, Department of Chemistry, Faculty of Science, University of Helsinki, Finland b Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, Finland c Department of Micro and Nanosciences, Faculty of Electronics, Communications and Automation, Helsinki University of Technology, Finland Desorption atmospheric pressure photoionization (DAPPI) is a new ambient ionization technique for mass spectrometry. DAPPI is based on thermal desorption of the analytes and gas phase dopant-assisted photoionization. Depending on the analyte and spray solvent (dopant), DAPPI produces [M+H]+ , [M−H]− , M+• , or M−• ions. The sample is either applied to a sample plate as liquid droplet, or the compounds can be analyzed directly from e.g. tablet or plant surface. In this study the ionization process in DAPPI and the effect of the ion source configuration were studied. In addition, DAPPI was applied to drug analysis. Several sample plate materials and spray solvents were tested and compared. Polymer sample plates were found to be most suitable for DAPPI since their low thermal conductivity enables local heating of the sample spot. Organic solvents with low ionization energy, such as
a
Institute of Biophysics and Nanosystems Research (IBN), Austrian Academy of Sciences, Graz, Austria b Center for Biomedical Engineering, Massachusetts Institute of Technology, Cambridge, MA, USA The present contribution focuses on the influences of four different charged designer lipid-like short anionic and cationic peptide surfactants on the fully hydrated monoolein (MO)-based cubic Pn3m phase. The studied peptide surfactants comprise seven amino acid residues, namely A6 D, DA6 , A6 K, and KA6 . D (aspartic acid) bears two negative charges, K (lysine) bears one positive charge, and A (alanine) constitutes the hydrophobic tail. To elucidate the impact of these peptide surfactants, the ternary MO/peptide/water system has been investigated using small-angle X-ray scattering (SAXS). We demonstrate that these peptides can be (i) used to tune the pore size in the cubic phase, and (ii) can be applied to stabilize over a wide temperature and concentration regime the inverted hexagonal phase (H2). Thus, in the near future the amphiphilic designer peptides may play a key role in improving functionalization and drug loading capacities of new drug nanocarriers based on cubosomes and hexosomes. doi:10.1016/j.ejps.2008.02.076
NANO- AND MICROTECHNOLOGY IN PHARMACY
S29
toluene, anisole and acetone, are suitable spray solvents in DAPPI.
O14 Opportunities for digitally encoded microcarriers in pharmacy and cell-based assays
doi:10.1016/j.ejps.2008.02.074
Farzaneh Fayazpour, B. Lucas, N. Huyghebaert, K. Braeckmans, S. Derveaux, R. Vandenbroucke, J.P. Remon, J. Demeester, C. Vervaet, S. De Smedt
Self-microemulsifying drug delivery system as nanosystems for bioavailability enhancement of flavonoids in vitro
O16
Alexander Shikov, O. Pozharitskaya, M. Karlina, V. Makarov Department of Pharmaceutics, Ghent University, Belgium St-Petersburg Institute of Pharmacy, Russia Counterfeiting of drugs is a real threat to public health. “In-drug labelling” would be a major step forward to combat counterfeiters. We recommend digitally encoded microparticles, known as memobeads, for this purpose. We also use these encoded microcarriers as a “non-positional cell array”: each of these encoded microcarriers can accommodate one cell type or certain substance. This might be a powerful tool for analysis of drug targets or toxicity markers or even as a delivery system for genetic materials. We found that entrapping the memobeads in starch-based granules protects them from deformation during tabletting; even when high compression forces were applied the code in the beads did not deform. Different cell lines can grow on the beads and these cells did not hamper the decoding of the beads. Furthermore, we have proposed a method of immobilizing adenoviral vectors on encoded microcarriers, while maintaining their ability to infect cells (reversed transfection). doi:10.1016/j.ejps.2008.02.073
The goals of the present investigations are to develop and characterize self-microemulsifying drug delivery systems (SMEDDS) with different flavonoids (rutin, quercetin and dihydroquercetin), and to evaluate their bioavailability. A water-in-oil microemulsion containing 2% flavonoids, oil phase, water, surfactant, and cosurfactant were prepared. The in vitro self-microemulsification properties and droplet size analysis of these formulations upon their addition to water under mild agitation conditions were studied. Pseudo-ternary phase diagrams were constructed identifying the efficient self-micro emulsification region. The efficiency of microemulsification was good when the surfactant–cosurfactant (6:1) concentration was 20–50%. The release of flavonoids from SMEDDS form resulted in about two- to fivefold increase in bioavailability compared with the powder formulation in vitro. SMEDDS have improved the bioavailability of all tested flavonoids significantly. The data suggest the potential use of SMEDDS to provide an efficient way of improving oral absorption of lipophilic drugs–flavonoids.
O15 Desorption atmospheric pressure spectrometry in drug analysis a, ¨ Luosujarvi
Laura Saarela c , S. Kauppila b
Arvola b ,
V. Franssila c , R.
photoionization-mass
doi:10.1016/j.ejps.2008.02.075 O17
Haapala b ,
M. Kostiainen b , T.
´ b, Pol
J. V. Kotiaho a,b , T.J.
Modulation of lipidic nanostructures by designer short peptide surfactants Anan Yaghmur a , P. Laggner a , S. Zhang b , M. Rappolt a
a
Laboratory of Analytical Chemistry, Department of Chemistry, Faculty of Science, University of Helsinki, Finland b Division of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Helsinki, Finland c Department of Micro and Nanosciences, Faculty of Electronics, Communications and Automation, Helsinki University of Technology, Finland Desorption atmospheric pressure photoionization (DAPPI) is a new ambient ionization technique for mass spectrometry. DAPPI is based on thermal desorption of the analytes and gas phase dopant-assisted photoionization. Depending on the analyte and spray solvent (dopant), DAPPI produces [M+H]+ , [M−H]− , M+• , or M−• ions. The sample is either applied to a sample plate as liquid droplet, or the compounds can be analyzed directly from e.g. tablet or plant surface. In this study the ionization process in DAPPI and the effect of the ion source configuration were studied. In addition, DAPPI was applied to drug analysis. Several sample plate materials and spray solvents were tested and compared. Polymer sample plates were found to be most suitable for DAPPI since their low thermal conductivity enables local heating of the sample spot. Organic solvents with low ionization energy, such as
a
Institute of Biophysics and Nanosystems Research (IBN), Austrian Academy of Sciences, Graz, Austria b Center for Biomedical Engineering, Massachusetts Institute of Technology, Cambridge, MA, USA The present contribution focuses on the influences of four different charged designer lipid-like short anionic and cationic peptide surfactants on the fully hydrated monoolein (MO)-based cubic Pn3m phase. The studied peptide surfactants comprise seven amino acid residues, namely A6 D, DA6 , A6 K, and KA6 . D (aspartic acid) bears two negative charges, K (lysine) bears one positive charge, and A (alanine) constitutes the hydrophobic tail. To elucidate the impact of these peptide surfactants, the ternary MO/peptide/water system has been investigated using small-angle X-ray scattering (SAXS). We demonstrate that these peptides can be (i) used to tune the pore size in the cubic phase, and (ii) can be applied to stabilize over a wide temperature and concentration regime the inverted hexagonal phase (H2). Thus, in the near future the amphiphilic designer peptides may play a key role in improving functionalization and drug loading capacities of new drug nanocarriers based on cubosomes and hexosomes. doi:10.1016/j.ejps.2008.02.076