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Biomedical subjects

S S Guterres

Publications and source records attributed to S S Guterres.

13 recordsLinked to original sources
PubMed2006

Preparation, characterization, and in vivo anti-ulcer evaluation of pantoprazole-loaded microparticles.

Pantoprazole is an important drug in the treatment of acid-related disorders. This work concerns the preparation and characterization of gastro-resistant pantoprazole-loaded microparticles prepared using an O/O emulsification/solvent evaporation technique. The in vivo activity of the pantoprazole-loaded Eudragit S100 microparticles was carried out in rats. Furthermore, tablets containing the microparticles were also investigated. Microparticles presented spherical and smooth morphologies (SEM) and they remained intact in the inner surface of tablets. DSC and IR analyses showed that pantoprazole was physically and molecularly dispersed in the polymer. In vivo anti-ulcer evaluation showed that the microparticles were able to protect rat stomachs against ulcer formation, while the drug aqueous solution did not present activity. Drug dissolution profiles from tablets demonstrated slower release than untabletted microparticles. Weibull equation was the best model for describing the drug release profiles from microparticles and tablets. As regards the acid protection, tablets showed a satisfactory drug protection in acid medium (61.05 +/- 8.09% after 30 min).

2-Pyridinylmethylsulfinylbenzimidazoles↗
PubMed2005

Semisolid topical formulations containing nimesulide-loaded nanocapsules, nanospheres or nanoemulsion: development and rheological characterization.

The objective of this work was to develop and characterize semisolid topical formulations containing nimesulide-loaded nanospheres, nanocapsules or nanoemulsion. The nanoprecipitation and spontaneous emulsification methods were used to prepare the colloidal suspensions and the nanoemulsion. The hydrodynamic diameters were 282 nm for the nanoemulsion, 293 nm for the nanocapsules and 191 nm for the nanospheres containing nimesulide. The encapsulation efficiencies were close to 99% in all cases and pH values ranged between 5.1 and 5.3. Each drug-loaded nanocarrier formulation was incorporated in Carbopol 940 gels. The semisolid dosage forms showed yellowish, glossy and homogeneous aspect after the incorporation of the colloidal suspensions and nanoemulsion. The recovery of nimesulide and the pH values for the gels containing nanoemulsion, nanospheres or nanocapsules remained constant during storage (120 days). For all formulations, the rheograms exhibited a non-Newtonian behavior presenting pseudoplastic characteristics and shear thinning. The rheograms were adjusted to Ostwald's model showing regression coefficients higher than 0.9900. None thixotropic phenomenon was experimentally detected under the test conditions for all formulations.

Algorithms↗
PubMed2004

Protective properties of melatonin-loaded nanoparticles against lipid peroxidation.

The aim of this study was to prepare melatonin-loaded nanoparticles (nanocapsules and nanospheres) by nanoprecipitation, using Eudragit S100 as polymer. The potential of these systems to protect lipids against peroxidation was evaluated in comparison to melatonin in aqueous solution and nanoemulsion. Liposomes and microsomes were used as model of a lipid membrane and lipid peroxidation was induced by free radical ascorbyl. Nanocapsule and nanosphere suspensions presented total recoveries of melatonin near 100% and associated drug around 55%. The zeta potential values were negative and the hydrodynamic diameter of particles were lower than 255 nm. The results demonstrate that the lipids were protected against peroxidation from 8 to 51% due to the presence of the melatonin and that this effect depended on the drug dose, the type of the lipid substrate and the type of colloid, in which melatonin was incorporated. Nanocapsules and nanospheres provided an important increase in the antioxidant effect of melatonin against lipid peroxidation.

Dosage Forms↗
PubMed2004

Microdialysis for evaluating the entrapment and release of a lipophilic drug from nanoparticles.

The aim of the study was to evaluate the microdialysis (MD) as a tool to determine entrapment efficiency and drug release of a lipophilic drug model, diclofenac (DIC), from nanocapsules, nanospheres, and nanoemulsions. Factors that could interfere with the MD probe recovery were investigated: perfusion fluid composition, concentration and form of the drug in the perfusate, and recovery method. DIC entrapment efficiency to nanoparticles and the drug release in phosphate buffer pH 7.4 after different dilutions were evaluated by MD and ultrafiltration/centrifugation (UC). DIC recovery for the 5 microL/min flux was concentration and pH dependent. DIC sodium was used for the recoveries determination since it did not differ from the DIC acid recovery for the same media. DIC entrapment efficiency determined applying both techniques were equivalent and close to 100% for all nanoparticles. In pH 7.4 DIC release from the nanoparticles was partial for the dilution rate 1:1 (v/v), around 50-60%. A complete release was observed from 1:10 (v/v) dilution. Only nanocapsules presented a incomplete release for 1:5 (v/v) dilution, around 86%. MD and UC techniques were equivalent for the evaluation of DIC entrapment efficiency and drug release from the nanoparticles.

Colloids↗
PubMed2004

Nanoparticle-coated microparticles: preparation and characterization.

The objective of the present work was to design and prepare new nanoparticle-coated drug-loaded inorganic microparticles by spray-drying using diclofenac as drug model. Previous works presented the process to dry drug-loaded polymeric nanoparticles using silicon dioxide as adjuvant, otherwise in the present proposition the drug is associated with the silicon dioxide and unloaded polymeric nanocapsule or nanosphere suspensions were used as organic coating. Eudragit S100 was chosen because of its gastric resistance. The potential application of polymeric colloidal suspensions as nanocoating for microparticles were evaluated in terms of process yields, encapsulation efficiencies, morphologic analyses and in vitro drug release profiles in buffered media (pH 1.2; 5.0 and 7.4). The results showed the technological feasibility of preparing controlled nanoparticle-coated drug-loaded inorganic microparticles. When the diclofenac was employed as a hydrophilic model, in this salt form, the powders prepared in two steps (core previously prepared) showed an adequate gastroresistance by the use of Eudragit S100. The use of diclofenac as a hydrophobic model (acid form) conducted to powders presenting good gastroresistance when the nanocapsules and triacetin were employed.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2003

Hydrophilic gel containing nanocapsules of diclofenac: development, stability study and physico-chemical characterization.

The purpose of this work was to develop and to characterize hydrophilic gels containing nanocapsules (NC) of diclofenac (DIC). Nanocapsules suspension of poly-epsilon-caprolactone containing free acid diclofenac were prepared by nanoprecipitation. The pH value of the nanocapsules suspension was 5.70 +/- 0.03 and the mean sizes of the NC were in the sub 300 nm range. Drug incorporated into the nanocapsules was close to 100% and the encapsulation efficiency was 104.1% +/- 3.5%. Diclofenac nanocapsules suspension (1 mg/mL) was incorporated in a Carbopol gel matrix fournishing a formulation with 0.5 mg of DIC/g. The gel stability was evaluated in terms of the macroscopic and microscopic aspect, rheological properties, pH and drug recoveries. As a result, we obtained a suitable formulation for topical use presenting a non-Newtonian behaviour with plastic properties and with intact nanostructures in the gel matrix after 3 months storage atroom temperature (freeze-fracture electron microscopy).

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2001

Ofloxacin/beta-cyclodextrin complexation.

Ofloxacin (OFX) is a fluorquinolone characterized by photochemical instability. With the goal to improve its photostability in aqueous solutions, the complexation of ofloxacin with beta-cyclodextrin was investigated. The complexes showed a water solubility enhancement of approximately 2.6 times; nevertheless, the photodegradation of ofloxacin was not reduced. The complexes obtained were characterized by thermal and 1H nuclear magnetic resonance (NMR) analysis, which revealed an interaction between ofloxacin and beta-cyclodextrin. The last analysis indicated that only partial inclusion of the N-methylpiperazinyl moiety occurred, which can explain the fact that photostabilization was not improved. This partial inclusion phenomenon could be explained also by computer-aided molecular modeling.

Anti-Infective Agents↗
PubMed2001

Spray-dried diclofenac-loaded poly(epsilon-caprolactone) nanocapsules and nanospheres. Preparation and physicochemical characterization.

The aims of the present study were to prepare spray-dried polymeric nanocapsules (NC) and nanospheres (NS) from poly(epsilon-caprolactone) (P epsilon C) suspensions containing diclofenac (DIC) and to determine the physicochemical properties of the formulations. NC or NS suspensions were prepared by interfacial deposition of the polymer. DSC-thermograms of raw materials and NC or NS suspensions (evaporated or spray-dried) were obtained using a PL-DSC. Spray-dried powders were prepared by addition of 3% (w/v) Aerosil 200 into suspensions of NC or NS. These mixtures were fed into a spray-dryer. DIC was assayed by HPLC. NC and NS spray-dried powders were examined under SEM (Jeol Scanning Microscope, JSM-5800). NC and NS suspensions had acceptable diameter, 340 and 247 nm respectively. The yields of NC and NS spray-dried powders were 80% and 75% and the recovery of the DIC was 99% and 93%, respectively. The melting peak of P epsilon C in NC and NS was observed at a temperature about 10 degrees C lower than in the raw material. In the NC thermograms the maximum of the oil (Miglyol 810) melting peak (+1.6 degrees C) was lowered about 7 degrees C. For spray-dried NC formulations, the SEM analyses of powders showed spherical microparticles of silicon dioxide, covered by nanoparticles (300 nm), while for spray-dried NS formulations the microparticles presented a rugged surface at the same magnification.

Anti-Inflammatory Agents, Non-Steroidal↗
PubMed2000

Preparation and characterization of spray-dried polymeric nanocapsules.

Recently, much interest has been generated by colloidal drug delivery systems such as nanocapsules because of the possibilities for controlled release, increased drug efficacy, and reduced toxicity after parenteral administration. Nanocapsules of poly-epsilon-caprolactone and Eudragit S90 were prepared. However, these systems present physicochemical instability. To dry these nanocapsule suspensions with the view of obtaining a solid form, the spray-drying process was used. Spray-dried powders of nanocapsules of poly-sigma-caprolactone and Eudragit S90 were prepared by atomization in a Büchi 190 Mini-spray dryer using colloidal silicon dioxide as a technological carrier. The morphological analysis of the surface at the powders showed that nanocapsules remain intact, and no change in particle size was detected after the spray-drying process. These results suggest that this method can be an interesting alternative to dry nanocapsule suspensions.

Chemistry, Pharmaceutical↗
PubMed2000

Poly(rac-lactide) nanocapsules containing diclofenac: protection against muscular damage in rats.

The aim of this work was to determine whether encapsulation of a non steroidal antiinflammatory agent within nanocapsules could reduce local toxicity after intramuscular injection. Diclofenac-loaded nanocapsules were prepared by deposition of poly(rac-lactic acid) polymer, and administered intramuscularly to male Wistar rats. Plasma creatine phosphokinase (CPK) activity and histological examination were used to assess local tissue damage. Following a single intramuscular injection of diclofenac (0.8 mg), CPK activity was shown to depend on both the type of dosage form and, in the case of nanocapsules, on the chemical nature of the central oily core. Lower CPK activity was observed with nanocapsules prepared from Miglyol 810, a caprylic/capric triglyceride, while nanocapsules prepared from benzyl benzoate, either empty or containing diclofenac, exhibited the same CPK activity as the drug solution. Histopathological examination performed three days after administration of free diclofenac or nanocapsules containing diclofenac prepared from Miglyol 810 revealed that a much more intense inflammation was obtained with the solution than with nanocapsules. In conclusion, when appropriately formulated, nanocapsules can considerably reduce the muscular damage caused by diclofenac.

Animals↗
PubMed2000

Polymeric colloidal systems containing ethionamide: preparation and physico-chemical characterization.

The association of ethionamide with different colloidal systems was evaluated. Nanocapsules (NC), nanospheres (NS), and nanoemulsions (NE) were prepared by interfacial deposition and spontaneous emulsification techniques. Ethionamide was incorporated before (B) and after (A) preparation of nanoparticles. Ethionamide was assayed by HPLC, the particle size was determined using a Nanosizer, and the zeta potential using a Zetasizer 4. Free ethionamide was determined using a combined ultrafiltration-centrifugation technique. The drug release was determined by direct dilution of the nanoparticle dispersion in phosphate-buffer pH 7. All preparations retained acceptable particle size distribution (+/- 300 nm), except the NE. The zeta potential of all formulations was between -36.6 mV and -46.1 mV. Percentages of ethionamide associated were: NC (B: 62.4%, A: 56.2%), NS (B: 53.0%, A: 43.2%), and NE (B: 38.5%). After 45 days, the percentage of drug association with NC increased (B: 66.8%, A: 60.6%). The release profiles demonstrated that associated ethionamide was more readily released from the NC and NS prepared by procedure A rather than B. The ethionamide amount not released (B) was greater in NS than NC. The drug is mainly adsorbed onto the surface of nanoparticles. However, approximately 10% of ethionamide is encapsulated into NC and 20% entrapped into NS, respectively.

Antitubercular Agents↗
PubMedDate not supplied

Influence of benzyl benzoate as oil core on the physicochemical properties of spray-dried powders from polymeric nanocapsules containing indomethacin.

To prepare spray-dried powders of poly(D,L-lactic acid) (PLA) or poly-epsilon-caprolactone (P epsilonC) from colloidal suspensions containing indomethacin (IND) using benzyl benzoate (BnB), nanocapsules (NC) were prepared by nanoprecipitation. To select the best NC formulations, increasing drug concentrations were tested (1.0, 1.5, or 2.0 mg/mL). The particle size was measured by Nanosizer. Spray-dried powders (SDP) were prepared by addition of Aerosil 200 into suspensions of NC. IND was assayed by HPLC. Free IND was determined using an Ultrafree. NC-SPD were examined under SEM. The particle sizes of all formulations are in the sub-300 nm range and are IND-associated, with drug recovery close to 100%. After 1 month, the formulations with highest drug content (2.0 mg/mL) showed a decline of total quantity of IND. After spray-drying, IND recovery for SDP presented values above 100%, indicating that the drug was concentrated from loss of mass during the process. To verify the relationship of oil phase with this loss of mass, similar NC (IND 1.5 mg/mL) prepared with Miglyol 810 (MI) were spray-dried, and SEM analysis showed nanostructures adsorbed onto SiO2. Similar nano-structures were not visualized for NC samples prepared with BnB. A swelling experiment showed the complete dissolution of both polymer by the BnB, whereas for MI the polymer masses remained unchanged. In conclusion, BnB is a solvent for PLA and P epsilonC and this ester is entrained during spray-drying. Despite the use of BnB in formulations of NC, PLA, or P epsilonC, colloidal suspensions prepared with BnB could be micelles instead of nanocapsules.

Benzoates↗