Biomedical subjects

V Gallardo

Publications and source records attributed to V Gallardo.

At least 19 recordsLinked to original sources

PubMed2006

Ftorafur loading and controlled release from poly(ethyl-2-cyanoacrylate) and poly(butylcyanoacrylate) nanospheres.

In the present work, a method is described to prepare polymeric colloidal nanospheres, consisting of poly(ethyl-2-cyanoacrylate) (PE-2-CA) or poly(butylcyanoacrylate) (PBCA), loaded with the anticancer drug ftorafur. The method is based on the anionic polymerization procedure, often used in the synthesis of poly(alkylcyanoacrylate) nanospheres for drug delivery. A detailed investigation of the capabilities of both polymeric nanoparticles to load this drug is shown. The effect of synthesis residuals and degradation products on the absorbance of supernatants was considered in the loading and release measurement methodologies, because of their potential perturbing influence on the determination of ftorafur concentration in solution. We found the existence of two mechanisms of drug incorporation: absorption or entrapment in the polymeric network, and surface adsorption, detectable by means of zeta potential and spectrophotometric measurements. Among the factors affecting the drug incorporation to the polymer network, the type of polymer, the pH and the drug concentration are the main determining ones. Moreover, the acidity of the medium needs to be controlled in order to avoid the formation of macroaggregates of solids. The optimum loading conditions were used to perform ftorafur release evaluations from polymeric particles, and the influence of the mechanism of drug incorporation, the amount of drug loaded, and the type of polymer on the drug release were studied.

Absorption↗

PubMed2006

Chemical characterization with XPS of the surface of polymer microparticles loaded with morphine.

Hydrophilic matrices are a potentially useful option for the development of oral controlled-release formulations. The porous surface of these particles makes it possible to control or modify release of the active principle after administration. As a result, such formulations can be used in liquid controlled-release pharmaceutical formulations. We investigated a method of spontaneous drug encapsulation to prepare ethylcellulose polymer microparticles (since the polymer is synthetic rather than natural the final suspension is called pseudolatex) filled with morphine hydrochloride. Morphine is incorporated to water during the synthesis process and thus it is microencapsulated inside the micelles that give rise to the final microparticles. X-ray photoelectron spectroscopy (XPS), a technique that can identify elements in a sample without destroying it, was used for the chemical analysis of the surface of these microspheres. The results demonstrated the complete absence of morphine from the microsphere surface, which was taken as evidence that the drug had been completely encapsulated.

Analgesics, Opioid↗

PubMed2006

Preparation and characterization of carbonyl iron/poly(butylcyanoacrylate) core/shell nanoparticles.

In this article a method is described to prepare composite colloidal nanoparticles, consisting of a magnetic core (carbonyl iron) and a biodegradable polymeric shell [poly(butylcyanoacrylate) or PBCA]. The method is based on the so-called anionic polymerization procedure, often used in the synthesis of poly(alkylcyanoacrylate) nanospheres designed for drug delivery. Interest of this investigation is based upon the fact that the heterogeneous structure of the particles can confer them both the possibility to respond to external magnetic fields and to be used as drug carriers. In order to investigate to what extent do the particles participate of this mixed properties, we compare in this work the physical characteristics (structure, chemical composition, specific surface area and surface electrical and thermodynamic properties) of the core/shell particles with those of both the nucleus and the coating material. This preliminary study shows that the mixed particles display an intermediate behavior between that of carbonyl iron and PBCA spheres. Electrophoretic mobility measurements as a function of pH and as a function of KNO3 concentration, show a great similarity between the core/shell and pure polymer nanoparticles. Similarly, a surface thermodynamic study performed on the three types of particles demonstrated that the electron-donor component of the surface free energy of the solids is very sensitive to the surface composition. In fact, a measurable decrease of such component is found for core/shell particles as compared to carbonyl iron. We also analyzed the influence of the relative amounts of polymer and carbonyl iron on the characteristics of the composite particles: data on the coating thickness, the amount of polymer bound to the magnetic nuclei, the redispersibility characteristics of the suspensions and the surface electrical and thermodynamic properties, suggest that the optimal synthesis conditions are obtained for a 4/3 initial monomer/carbonyl iron weight ratio.

Absorbable Implants↗

PubMed2005

An experimental investigation of the stability of ethylcellulose latex: correlation between zeta potential and sedimentation.

This paper aims at explaining the experimental observations of the stability and redispersibility of an aqueous ethylcellulose latex through the electrokinetic characterization of the particles. The surface charge and the electrical double layer thickness play an essential role in the stability of the system, hence the need for a full characterization of the polymeric particles. The effect of both pH and ionic strength of the dispersion medium were investigated. It was found that at acid pH values the latex displays "delayed" or "hindered" sedimentation: in such conditions, the electrophoretic mobility and zeta potential are rather low, indicating a small electrokinetic charge on the particles. At alkaline pH, when the dissociation of ionizable surface groups must be complete, the zeta potential is high and negative. The electrostatic repulsion between polymer particles is responsible for the low sedimentation volume and poor redispersibility of the latex. The effect of NaCl and CaCl(2) concentration on both the zeta potential and stability of the latexes was also investigated: it was found that CaCl(2) has the greatest influence, yielding flocculated, easily re-dispersible systems when its concentration in the dispersion medium is high enough. There qualitative observations were ascertained by means of calculations of the potential energy of interaction between particles. In the case of NaCl solutions, a high and relatively wide potential energy barrier was predicted, that may prevent the particle aggregation. Above 5mM NaCl a shallow minimum in the potential energy curves must lead to the formation of aggregates. Similar results were found with CaCl(2) solutions, although in this case the secondary minima are deeper and appear at lower concentrations.

Calcium Chloride↗

PubMed2005

Formulations of hydrogels and lipogels with vitamin E.

Vitamin E, a topically administered antioxidant, reduces erythema, photoaging, photocarcinogenesis, edema, and skin hypersensitivity associated with exposure to ultraviolet B (UVB) radiation. Virgin olive oil, which also has antioxidant properties, reduces the number of, and delays the onset of skin cancer induced by UVB radiation when used after sunbathing. Topical use after sunbathing of formulations that contain virgin olive oil and vitamin E may therefore reduce the number and delay the onset of UVB-related skin cancer in humans. We designed formulations of gels with olive oil (lipogels) and hydrogels containing 2% tocopherol. The formulations were optimized on the basis of rheological, organoleptic, biopharmaceutical, and cosmetic criteria. Different formulae for hydrogels with vitamin E were ideal for application after exposure to solar radiation because of their good organoleptic properties. Vitamin E lipogels are of potential use in cosmetics such as locally acting anti-aging treatments because of the antioxidant effects of vitamin E.

Journal Article↗

PubMed2004

Electrophoretic properties of acrylic latex suspensions (Kollicoat MAE 30 D) and ibuprofen.

We have compared the electrophoretic properties (measured on the electrical surface) of the commercial latex Kollicoat MAE 30 D and the non-steroidal anti-inflammatory drug (NSAID) ibuprofen in preparation for attempts to develop a suitable vehicle for the NSAID to obtain a modified release formulation. Electrophoretic mobility of the latex and the active principle was measured in solutions containing different concentrations of inorganic electrolytes (NaCl, CaCl2 and AlCl3) at different pH values. This was considered an indispensable first step for further characterization of the substance's electrical properties. Suspensions of both the latex and the drug had negative mobility values throughout the range of pH values studied here. Of the electrolytes, neither NaCl nor CaCl2 led to positive mobility, and no isoelectric point could be determined. However, AlCl3 at a concentration of 10(-3) M led to the greatest reduction in mobility. We therefore found that trivalent cations were more effective than divalent cations, which in turn were more effective than monovalent cations, in reducing mobility.

Acrylates↗

PubMed2004

Physical characteristics of polymer complexes in suspension obtained from cellulosic latexes with ondansetron.

Ondansetron is a carbazol with antiemetic properties. It is used primarily to control nausea and vomiting caused by cytotoxic chemotherapy and radiotherapy, as well as in postoperative vomiting in gynecological surgery. Ondansetron has a half-life of approximately 4 h, hence it is a matter of great interest to determine the ideal conditions for the formation of a drug-polymer complex in order to prolong the duration of the therapeutic action. A stability study of the active drug was first carried out on each of the polymers (Aquateric and Aquacoat). The adsorption of ondansetron on the lattices was determined with respect to time, pH and concentration. The results obtained suggest that both polymers are suitable as drug carriers for the controlled-release formulations obtained. We conclude that an acid pH is evidently fundamental in the adsorption process of this drug in the latexes. Moreover, the Aquateric latex would seem to be the best-suited polymer to use as a vehicle for drug delivery.

Adsorption↗

PubMed2001

Synthesis and characterization of poly(ethyl-2-cyanoacrylate) nanoparticles with a magnetic core.

A method is described to prepare composite colloidal nanoparticles, consisting of a magnetic core (magnetite) and a biodegradable polymeric shell (poly(ethyl-2-cyanoacrylate) or PE-2-CA). The method is based on the so-called anionic polymerization procedure, often used in the synthesis of PE-2-CA nanospheres designed for drug delivery. In the present work, the heterogeneous structure of the particles can confer both magnetic-field responsiveness and potential applicability as a drug carrier. In order to investigate to what extent this target is achieved, we compare the structure, chemical composition, and surface properties of the core/shell particles with those of both the nucleus and the coating material. This preliminary study shows that the synthetic new material displays an intermediate behavior between that of magnetite and PE-2-CA spheres. Thus, electrophoresis measurements as a function of pH and as a function of KNO3 concentration, show great similarity between the core/shell and pure polymer nanoparticles. A similar conclusion is reached when a surface thermodynamic study is performed on the three types of particles: the electron-donor component of the surface free energy of the solids is the quantity that appears to be most sensitive to the surface composition. The fact that PE-2-CA is close to being a non-polar material gives rise to a measurable decrease in the electron-donor component of the surface free energy of core/shell particles as compared to magnetite.

Contrast Media↗

PubMed2001

X-ray diffraction and electron microscopy in the polymorphism study of ondansetron hydrochloride.

Using different techniques, we studied the possible formation of ondansetron polymorphs. Ondansetron is a carbazol antiemetic that acts as a competitive, selective inhibitor of 5-HT3 serotonin receptors. The polymorphs were determined by X-ray diffraction (XRD) and scanning electron microscopy (SEM). The results suggest that the compounds are not true crystallographic polymorphs, but instead are the product of physical structural changes in the drug, which would be of interest pharmaceutically.

Algorithms↗

PubMed2000

The expression and activity of monoamine oxidase A, but not of the serotonin transporter, is decreased in human placenta from pre-eclamptic pregnancies.

Serotonin (5-HT) plays a pivotal role in pregnancy and a hyperserotonomic condition has been documented in pre-eclampsia. We have attempted to elucidate the possible participation of 5-HT as an aetiological factor in pre-eclampsia, by estimating the activity and expression of the 5-HT transporter (SERT) and monoamine oxidase A (MAO-A) in human placenta from full term normal (NG) and severe pre-eclamptic (PES) pregnancies. Uptake of 5-[1,2-3H] hydroxytryptamine binoxalate (specific radioactivity, 30.4 Ci/mmol) was determined in placental brush border vesicles by a rapid filtration technique. 5-HT metabolism in placental homogenate was measured using a HPLC-ECD system. Expression of SERT and MAO-A was determined by Western blot, using specific antibodies against the human SERT and MAO-A in placental tissues obtained from NG and PES. Our results, showed no significant difference in 5-HT uptake between both groups. However, 5-HT metabolism was significantly lower in placental homogenates from PES than in NG placentas, with the pathological preparations showing no MAO-A activity against 5-HT during the first 60 min of incubation (87% and 5% of metabolism of 5-HT initially added, NG and PES respectively). Western blot analysis showed a similar expression of SERT in BBMV from NG and PES. However, unlike for normal pregnancies, the expression of MAO-A in placental homogenates from PES was found to be very low, or almost negligible. These findings confirm our previous results and suggest that the higher plasma free 5-HT levels observed in severe pre-eclampsia could be mainly due to a reduction in placental MAO-A expression and activity and are not limited by the expression and uptake of 5-HT into the placental tissue.

Adult↗

PubMed2000

Interfacial properties of barium sulfate suspensions. Implications in their stability.

A surface characterization of barium sulfate particles in aqueous suspensions was carried out in this work. With the aim of predicting the stability conditions of these widely used suspensions, the electrical surface properties of the particles were first studied by electrophoretic mobility determinations. It was found that both H(+) and OH(-) ions can be considered as potential-determining ions for the barium sulfate/water interface. The same conclusion was reached concerning the lattice ions, Ba(2+) (mainly) and SO(4)(2-). It was also found that increasing the concentration of sodium chloride in the dispersion medium can even change the sign of the zeta (zeta) potential: it is suggested that this behavior is an indirect effect provoked by changes in the solubility of barium sulfate with the ionic strength. To compute the van der Waals (LW) attraction between the particles as well as the acid-base contribution to the total energy of interaction, a thermodynamic characterization of the interface was also carried out by measuring the rate of penetration of selected liquids through plugs of the particles. It was found that barium sulfate particles are essentially monopolar in nature; that is, they show electron-donor character as demonstrated by the essentially zero value of the electron-acceptor component of their surface free energy. Pretreatment of the particles with 10(-2) M solutions of BaCl2 and CaCl2 significantly reduced the electron-donor component, whereas both NaCl and Na(2)SO(4) provoked the opposite effect. This result is explained in terms of the acid-base character of the ions added. These data were used to calculate the interaction energy between the particles. The effect of electrolyte concentration on the stability of the suspensions was analyzed on the basis of the dependence with distance of the interaction energy between the particles. Our results suggest that more stable suspensions of barium sulfate are predicted if moderate amounts of SO(4)(2-) ions are added to the dispersion medium.

Barium Sulfate↗

PubMed2000

Adsorption of omeprazole on latex particles and characterization of the complex.

Omeprazole is an antisecretory drug used against gastric ulcers. It quickly decomposes in an acid medium, however, therefore making it a matter of great interest to protect it in these conditions and determine the ideal adsorption conditions for this drug on latex particles for formulation designs--oral suspensions--containing polymers with the aim of delivering different drugs in a sustained and controlled action. Time, pH, and concentration of the active ingredient for which maximum adsorption occurs, were determined. The findings suggest that adsorption is evidently greatest at an acid pH 4-5, that the adsorption of Omeprazole rises concomitantly with the increase in latex particles, and the time is the least influential factor.

Adsorption↗

PubMed2000

Mechanisms of endothelin-1-induced contraction in isolated placental veins from normal full-term and preterm pregnancies.

This study characterizes the reactivity of human chorionic plate vein in full-term (39.4+/-0.3 weeks of gestation) and preterm (34.4+/-0.6 weeks of gestation) pregnancy to endothelin-1 (ET-1) and attempts to characterize ET-1 receptor subtype, and the contribution of nitric oxide and cyclooxygenase products in these responses. In placental veins from full-term and preterm pregnant women, cumulative addition of ET-1 (10(-10)-10(-6) M) caused marked and long-lasting concentration-dependent contractile responses. The mean EC(50) and E(max) values for ET-1-induced venoconstriction did not differ between the full-term and preterm pregnancy groups. In the veins from preterm placental preparations, the ET(A) receptor-selective antagonist cyclo(D-alpha-aspartyl-L-propyl-D-valyl-L-leucyl-D-tryptophyl (BQ123) reduced the ET-1-induced contraction by 28.6+/-2.4%, compared to a decline in tension of 51.2+/-4.2% in the full-term placental vessels. The ET(B) receptor-selective antagonist, N-[N-[N-[2,6-dimethyl-1piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-D-norleucinemonosodium (BQ788), did not influence ET-1-induced contraction in placental vein from both pregnancy groups in terms of maximal contraction and sensitivity. Pretreatment with the cyclooxygenase inhibitor, indomethacin (1 microM) and the nitric oxide synthase inhibitor N(w)-nitro-L-arginine (NOLA, 100 microM) did not significantly affect either the EC(50) or the maximum contraction to ET-1 in veins from normal full-term and preterm preparations. The results of this study suggest that there is no correlation between ET-1-induced vasoconstriction and gestational age and that this vasoconstriction is mediated predominantly via ET(A) receptor subtype in both groups of pregnant women, independent of NO and eicosanoids.

Endothelin Receptor Antagonists↗

PubMed2000

Adsorption-desorption of ondansetron on latex particles.

Ondansetron is a carbazol with antiemetic properties. It is used primarily to control nausea and vomiting caused by cytotoxic chemotherapy and radiotherapy, as well as for treatment of postoperative vomiting in gynecological surgery. Ondansetron has a shelf life of about 3 hr; hence, it is a matter of great interest to determine the ideal adsorption-desorption conditions for this drug on latex particles for designs of formulations (oral suspensions) containing polymers with the aim of delivering different drugs in a prolonged and controlled fashion. Time, pH, electrolytes, and concentration of the active principal at which maximal adsorption occurred were determined. Desorption of the drug from latex polymer particles was studied in different media. The results obtained suggest that this polymer is suitable as carrier of drug for obtained formulations of controlled release. The findings suggest that pH is the principal factor influencing the release of the ondansetron from Aquateric. The greatest release of drug occurs at acid pH, approximately 70% in the first hour; for the basic medium, the release is about 6%.

Adsorption↗

PubMed2000

Transport and metabolism of serotonin in the human placenta from normal and severely pre-eclamptic pregnancies.

We have attempted to elucidate the possible participation of serotonin as an etiological factor in pre-eclampsia. The transport of serotonin into vesicles from the maternal-facing brush border membrane was measured, as well as the metabolism induced by monoamine oxidase (MAO) in placental homogenate obtained from normal-term and severely pre-eclamptic placentas. Kinetic analysis of serotonin uptake by the placental brush border membrane of the syncytiotrophoblast between normally pregnant and severely pre-eclamptic subjects showed no significant difference (similar Vmax and Km values). However, the metabolism of serotonin was significantly higher in placental homogenate from normal pregnancies than in placentas from severely pre-eclamptic pregnancies. These findings suggest that the higher plasma-free serotonin levels observed in severe pre-eclampsia are mainly due to a reduction in MAO-A activity and not limited by the rate of serotonin uptake into the cells.

Adult↗

PubMed2000

Vascular reactivity to angiotensin II and eicosanoid production in the human placenta from term and preterm pregnancy.

Isolated human placental cotyledons from normal term (37-40 weeks of gestation) and preterm (26-36 weeks of gestation) labor were perfused in vitro, and the effect of angiotensin II (ANG II) and its interaction with prostanoids was measured. In the preterm group, ANG II caused greater maximal increases in perfusion pressure than in normal term pregnancies without affecting sensitivity. Also, preparations from normal term pregnancies showed a marked development of tachyphylaxis compared to placentae from preterm pregnancies. Indomethacin (10(-6) M) increased the maximum pressor response to ANG II by 33.6% in normal term, however, in preterm placentas a 39.2% reduction was observed. Infused ANG II 10(-6) M) decreased the concentrations of thromboxane B(2) and 6-keto-PGF(1alpha) in both pregnancy groups, but this effect was not statistically different from the baseline values. In the current study, we show that the placenta of preterm pregnancies in basal conditions produce 7.6 times as much thromboxane as the normal term placenta (2,800+/-470 vs. 366.5+/-62 pg/min, respectively), without significant change in prostacyclin levels (preterm 88.6+/-11.0 vs. Term 100.6+/-30.7 pg/min). These observations provide evidence that the contribution of basally released thromboxane from placental tissue appears to contribute to abnormalities in the regulation of fetoplacental hemodynamics in premature pregnancies.

6-Ketoprostaglandin F1 alpha↗

PubMed1999

Formation of ondansetron polymorphs.

We used differential scanning calorimetry, infrared spectrophotometry and 1H nuclear magnetic resonance imaging to search for polymorphs of ondansetron. Samples were tested under different conditions of temperature, pulverization and pH, and in different solvents. The factors identified as able to cause the formation of polymorphs were heating to different temperatures for different times, and the use of ethanol and methanol as solvents.

Antiemetics↗

PubMed1999

Development, formulation, and effectiveness testing of a silicone-based barrier-type hand cream.

We report the development, design, and results of effectiveness and acceptability testing of a hydrating, nutritive, barrier-type hand cream designed for severely damaged skin (including skin damaged by dermatological problems). We tested different silicone derivatives and a water-in-oil (W/O) silicone emulsifier to produce organoleptic qualities that would increase consumer acceptance of this type of W/O emulsion. Pharmacotechnical and effectiveness tests were done to check the stability and preservation of the formulas, their usefulness in improving dry skin, and acceptance by users. The results of pharmacotechnical testing were optimal. Although no active principle aimed specifically at dermatological problems was present in the final formulas, users reported notable subjective improvements in cracking and scaling.

Chemistry, Pharmaceutical↗