RESUMO
Drug controlled release technologies (DCRTs) represent an opportunity for designing new therapies. Main objectives are dose number optimization and secondary effects reduction to improve the level of patient/client acceptance. The present work studies DCRTs based in blended polymeric implants for single dose and long-term therapies of florfenicol (FF), a broad spectrum antibiotic. Polymers used were PLGA and Eudragit E100/S100 types. Eudragit/PLGA and FF/PLGA ratios were the main studied factors in terms of encapsulation efficiencies (EEs) and drug release profiles. In addition, morphological and physicochemical characterization were carried out. EEs were of 50-100% depending on formulation composition, and the FF releasing rate was increased or diminished when E100 or S100 were added, respectively. PLGA hydrolytic cleavage products possibly affect Eudragit solubility and matrix stability. Different mathematical models were used for better understanding and simulating release processes. Implants maintained the antimicrobial activity against Pseudomonas aeruginosa up to 12 days on agar plates. The developed DCRTs represents a suitable alternative for florfenicol long-term therapies.
Assuntos
Ácidos Polimetacrílicos , Tianfenicol , Preparações de Ação Retardada , Humanos , Solubilidade , Tianfenicol/análogos & derivadosRESUMO
Progesterone (PGT) is a natural hormone that stimulates and regulates various important functions, such as the preparation of the female body for conception and pregnancy. Due to its low water solubility, it is administered in a micronized form and/or in vehicles with specific solvents requirements. In order to improve the drug solubility, inclusion complexes of PGT and ß-cyclodextrins were obtained by the freeze-drying method. Two ß-cyclodextrins (native and methylated) in two solvents (water and water:ethanol) and different molar ratio of the reagents were the variables tested for the selection of the best condition for the preparation of the complexes. The PGT/randomly methylated-ß-cyclodextrin complexes were incorporated into chitosan thermosensitive hydrogels, as an alternative formulation for the vaginal administration of PGT. Neither the micro and macroscopic characteristics of the gels nor the transition time from solution to gel were modified after the complexes incorporation. In addition, chitosan gels with complexes resisted better the degradation in simulated vaginal fluid in comparison to commercial gel (Crinone®). The chitosan gel with inclusion complexes and Crinone® were tested in vitro in a diffusion assay to evaluate the delivery of the hormone and its diffusion through porcine epithelial mucosa obtained from vaginal tissue. Chitosan gel presented sustained diffusion similar to the exhibited by commercial gel. The use of chitosan gels with inclusion complexes based on cyclodextrins would be a viable alternative for vaginal administration of PGT.
RESUMO
Polylactic and glycolic acid nanoparticles (PLGA-NPs), coated with L-ferritin, are exploited for the simultaneous delivery of paclitaxel and an amphiphilic Gd based MRI contrast agent into breast cancer cells (MCF7). L-ferritin has been covalently conjugated to the external surface of PLGA-NPs exploiting NHS activated carboxylic groups. The results confirmed that nanoparticles decorated with L-ferritin have many advantages with respect to both albumin-decorated and nondecorated particles. Ferritin moieties endow PLGA-NPs with targeting capability, exploiting SCARA5 receptors overexpressed by these tumor cells, that results in an increased paclitaxel cytotoxicity. Moreover, protein coating increased nanoparticle stability, thus reducing the fast and aspecific drug release before reaching the target. The theranostic potential of the nanoparticles has been demonstrated by evaluating the signal intensity enhancement on T1-weighted MRI images of labeled MCF7 cells. The results were compared with that obtained with MDA cells used as negative control due to their lower SCARA5 expression.
Assuntos
Portadores de Fármacos/química , Ferritinas/química , Nanopartículas/química , Paclitaxel/administração & dosagem , Ácido Poliglicólico/química , Antineoplásicos Fitogênicos/administração & dosagem , Neoplasias da Mama/diagnóstico por imagem , Neoplasias da Mama/tratamento farmacológico , Neoplasias da Mama/patologia , Meios de Contraste/administração & dosagem , Meios de Contraste/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Humanos , Células MCF-7 , Imageamento por Ressonância Magnética , Nanopartículas/uso terapêutico , Paclitaxel/farmacocinética , Receptores Depuradores Classe ARESUMO
One possibility to obtain a higher dose of drug in a lower formulation volume can be by using of saturated quantity of drug in one of the phases of an emulsion. These formulations are called suspoemulsions (S/O/W). When a hydrophobic polymer is added to the organic phase of suspoemulsions, these formulations can be used to entrap the drug inside microspheres after in situ precipitation of the polymer-drug-excipients mix. In this work, performance and stability of progesterone suspensions in triacetin as organic phase of suspoemulsions were evaluated. These formulations were compared with O/W emulsions. Mathematical models were used to study in vitro release profiles. The results confirmed that S/O/W systems could be an attractive alternative to O/W formulations for the entrapment of progesterone inside poly(d,l-lactide-co-glycolide) microspheres. Diffusive-based models fit the in vitro release of progesterone from in situ-formed microspheres. For longer release periods, a time-dependent diffusion coefficient was successfully estimated.
Assuntos
Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos , Microesferas , Progesterona/administração & dosagem , Química Farmacêutica , Difusão , Portadores de Fármacos , Emulsões , Excipientes , Ácido Láctico/química , Modelos Teóricos , Poloxâmero/química , Ácido Poliglicólico/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Polímeros/química , Polissorbatos/química , Progesterona/química , Triacetina/químicaRESUMO
The aims of the present study were to analyze the genetic variability of Cercospora kikuchii isolates and the in vitro cercosporin production, of these isolates obtained from soybean at the central-northern region of Santa Fe province (Argentina). Also the relationship between RAPD profiles and toxin production was also assessed. The strain C. kikuchii NBRC 6711 and 13 soybean isolates with symptoms of leaf blight were tested. Cercosporin production was analyzed by growing the fungus on Potato Dextrose Agar, extracting the toxin in alkaline medium and determining its concentration by spectrophotometry. The population of C. kikuchii studied showed variability, both genotypically, nine different groups were encountered, and have the ability to produce cercosporin. No relationship was found between toxin production and the RAPD profiles.