Study of liposomes stability containing soy phosphatidyleholine and hydrogenated soy phosphatydylcholine adding or not cholesterol by turbidity method

Study of Liposomes Stability Containing Soy Phosphatidyleholine and Hydrogenated Soy Phosphatydylcholine Adding or Not Cholesterol by Turbidity Method. Liposomes are structures composed by phospholipids as soy phosphatidylcholine (PC) and hydrogenated soy phosphatydylcholine (PCH). Among the methods used to prove liposomes stability, turbidity method is widely used. The objective of this work was to study the liposomes stability containing PC or PCH with and without cholesterol (CHOL) by turbidity method. Liposomes were stored a 30 degrees C during 90 days and periodically absorbance readings at 410 nm were made to verify possible turbidity alterations. Increases in the turbidity with time occurred for PC liposomes. In the presence of CHOL higher turbidity was obtained probably reflecting the increase in the size of liposomes. For PCH liposomes the presence of CHOL did not affect the turbidity suggesting higher physical stability of the structures.

Study of the diclofenac/phospholipid interactions with liposomes and monolayers

The interaction of diclofenae sodium (SD) with soya phosphatidylcholine (SPC) has been studied with floating Langmuir monolayers and liposomes. SD was either introduced into the subphase of SPC monolayers or co-spread with SPC on an aqueous subphase. In both cases, SD caused the surface pressure isotherm to become more expanded, thus demonstrating the affinity between SD and SPC. The incorporation of SD caused SPC liposomes to have a decreased diameter according to light scattering experiments. When SPC liposomes were injected into an aqueous subphase, their destruction yielding surface-active monomers could be monitored by changes in surface pressure. SD-loaded liposomes displayed a much faster kinetics when the surface density of surface-active monomers was plotted against time, with rate constants increasing significantly with the SD concentration. The kinetic profile can be quantitatively analyzed by plotting In[1 - (Gamma/Gamma(infinity))] versus t(1/2) (C) 2004 Elsevier B.V. All rights reserved.

Structure and viscoelastic behavior of pharmaceutical biocompatible anionic microemulsions containing the antitumoral drug compound doxorubicin

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Structural Properties Induced by the Composition of Biocompatible Phospholipid-Based Microemulsion and Amphotericin B Association

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Investigating the effect of different positioning of lysine residues along the peptide chain of mastoparans for their secondary structures and biological activities

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Monitoring the positioning of short polycationic peptides in model lipid bilayers by combining hydrogen/deuterium exchange and electrospray ionization mass spectrometry

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Tertiary structural changes of the alpha-hemolysin from Staphylococcus aureus on association with liposome membranes

The interaction of alpha-hemolysin (also called alpha-toxin) from Staphylococcus aureus with mixed egg-yolk phosphatidylcholine/cholesterol liposomes has been investigated using the intrinsic tryptophan fluorescence emission (ITFE) signal. The ITFE intensity of alpha-hemolysin, which was obtained using a novel purification protocol, showed a triphasic increase on incubation with liposomes at low protein/lipid ratios. The first, rapid phase results in an increase in ITFE of 10%, which reflects rapid conformation changes in the alpha-hemolysin on association with the liposome membrane, the second phase of the ITFE increase is associated with a red shift from 334 to 339 nm in the maximum emission wavelength, suggesting the transition to a partially unfolded intermediate in the oligomerization process. The third phase of the ITFE intensity change demonstrates a temporal correlation with the appearance of SDS-stable oligomers. The results demonstrate the feasibility of identification of intermediate protein conformations in complex membrane-associated processes by manipulation of the liposomal membrane composition. (C) 1998 Academic Press.

The effect of sodium chloride on the formation of W/O microemulsions in soy bean oil/surfactant/water systems and the solubilization of small hydrophilic molecules

Partial pseudoternary phase diagrams were constructed for soy bean oil (SBO)/surfactant/NaCl aqueous solution systems, at 25 degrees C, using the anionic sodium bis(2-ethylhexyl) sulfosuccinate (ACT) and zwiterionic phosphatidylcholine (PC) or mixtures of these surfactants. The isotropic single phase of water-in-oil (W/O) microemulsions (MEs) is shown in the phase diagram and their viscosity reported. ME samples containing small amount of surfactant exhibit slightly higher viscosity than pure SBO, and were used in the solubilization of small water soluble molecules. NaCl enhances the area of the ME phase and MEs with different surfactant composition exhibit different induction time as obtained from tests of oxidative stability, and so are the MEs enriched with ascorbic acid, folic acid and FeSO4, with the latter exhibiting lower stability. The so prepared enriched soy bean oil has potential application in food industry since the surfactants are food grade. (C) 2007 Elsevier B.V. All rights reserved.

Influence of the Bilayer Composition on the Binding and Membrane Disrupting Effect of Polybia-MP1, an Antimicrobial Mastoparan Peptide with Leukemic T-Lymphocyte Cell Selectivity

Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq)

The membranotropic activity of N-terminal peptides from the pore-forming proteins sticholysin I and II is modulated by hydrophobic and electrostatic interactions as well as lipid composition

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Relationship between structural features and in vitro release of doxorubicin from biocompatible anionic microemulsion

In this work structural features of anionic microemulsions, containing the pharmaceutical biocompatible components soya phosphatidylcholine (SPC), eumulgin HRE 40 (EU) and sodium oleate (SO) as surfactant, cholesterol (CHO) as oil phase and aqueous buffer were studied. Microemulsions were formulated with and without the antitumor drug doxorubicin (DOX). The various microstructures characterized in the pseudo-temary phase diagram were analyzed by polarized light microscopy, small-angle X-ray scattering (SAXS) and X-ray diffraction (XRD) as well as by their ability to incorporate and release DOX. The experimental results demonstrated a correlation between the composition, the structural features and drug delivery. It was found that at higher cholesterol contents, the crystallization of CHO polymorph phases changed the mobility of DOX molecules. Droplets were formed with short-range spatial correlation from a microemulsion (ME) with a low surfactant:oil ratio. More ordered structures with lamellar arrangements formed by the increasing of the CHO proportions in the formulation may be due to CHO crystallization. The in vitro release of DOX showed that the presence of a high content of crystalline CHO prolongs the release of DOX from ME. The retention of DOX in the internal oil phase of the ME may modulate the drug release for a prolonged time. These results clearly demonstrate the potential of ME as a drug-delivery system. (c) 2007 Elsevier B.V. All rights reserved.

Oil-in-water lecithin-based microemulsions as a potential delivery system for amphotericin B

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Espectro de gotas de pontas de pulverização com adjuvantes de uso agrícola

O sucesso de uma boa aplicação de produtos fitossanitários depende da sinergia entre fatores como tamanho de gota, tipo de ponta, pressão, volume e composição da calda e características do alvo. Assim, o objetivo deste trabalho foi avaliar o espectro de gotas produzidas por pontas de jato plano defletor (TT 11002) e jato plano defletor com indução de ar (TTI 11002), com diferentes adjuvantes adicionados à calda de pulverização, pela técnica de difração de raio laser. O experimento foi conduzido em delineamento inteiramente casualizado, com quatro repetições, em esquema fatorial 2 x 5, ou seja, duas pontas de aplicação (jato plano defletor e jato plano defletor com indução de ar) e cinco composições de calda (água e água mais quatro adjuvantes: fosfatidilcoline+ácido propiônico, éter poliglicólico de monilfenol, ésteres de ácidos graxos e nonil-fenol etoxilado+óxido de etileno). em ambiente controlado, avaliou-se o espectro de gotas, por meio de um analisador a laser de gotas em tempo real, na pressão de 276 kPa. O efeito dos adjuvantes no espectro de gotas mostrou-se dependente da ponta de pulverização empregada. A adição dos adjuvantes à calda não alterou o risco potencial de deriva, expresso pela porcentagem do volume em gotas com diâmetro inferior a 100 µm, porém o adjuvante fosfatidilcoline+ácido propiônico reduziu o diâmetro da mediana volumétrica das gotas produzidas pela ponta de jato plano defletor com indução de ar, em relação à avaliação feita somente com água.

Anticardiolipin antibodies from syphilis and systemic lupus erythematosus induce leakage in cardiolipin vesicles

Anticardiolipin antibodies from sera of patients with systemic lupus erythematosus or syphilis induced leakage of entrapped carboxyfluorescein (CF) from cardiolipin (CL)/phosphatidylcholine(PC) vesicles prepared by sonication of equimolar mixtures of CL:PC. The sera dilution used here was 1:7500. IgG (5-20 mu g/ml) from the same sera, not containing beta(2)GPI, also produced a concentration-dependent leak. Vesicle leakage was inhibited by salt and was not detected with vesicles prepared exclusively with phosphatidylcholine. The demonstration of antibody-induced vesicle leakage offers a convenient system to investigate the mechanism of antibody-lipid binding as well as a potential diagnostic tool.

Tissue tolerance of diclofenac sodium encapsulated in liposomes after intramuscular administration

In this work the effect of the encapsulation of diclofenac sodium within liposomes on the reduction of the myotoxicity after intramuscular administration in rats was studied. Diclofenac sodium was encapsulated in small unilamellar liposomes obtained from phosphatidylcholine, cholesterol, and a-tocopherol (40:10:0.04 mM), and administered by intramuscular injection in the quadriceps femoral muscle of male Wistar rats. After a single dose of 0.2 mg diclofenac formulations the local tissue damage was assessed by plasma creatine kinase (CPK) activity and histological analysis. It was demonstrated that formulations containing free diclofenac produced a higher increase in CPK activity, while those encapsulated in liposomes exhibited CPK activity similar to the control groups. Histopathological analysis of local muscle tissue performed on the third and seventh days following the injection showed intense cellular damage when free drug solution was used, while encapsulation in liposome protected the tissue against the local tissue inflammation.