Influence of phosphated cross-linked high amylose on in vitro release of different drugs

The influence of structural characteristics of high amylose cross-linked at different degrees on the release of drugs with important molecular differences, namely sodium diclophenac (SD) and nicotinamide (NI), was assessed in vitro from non-compacted systems. The release profiles were related with classical kinetic mathematical models for better understanding of the release mechanism. An increase in polymer cross-linking degree resulted in longer release time for both drugs, although SD generally was released slower than NI. SD release from samples cross-linked at 2% of basis was driven mainly by Fickian diffusion, while from samples cross-linked at 4% of basis follows anomalous mechanism. Inversely, anomalous mechanism was responsible for NI release from 2% samples and Fickian diffusion from 4% samples. Results suggest that the performance of cross-linked high amylose as excipient for controlled drug release not only depends on cross-linking degree but also is highly influenced by structural characteristics of the drug. (C) 2009 Elsevier Ltd. All rights reserved.

Controlled Drug Release from Ureasil-Polyether Hybrid Materials

Flexible, transparent, and insoluble urea-cross-linked polyether-siloxane hybrids presenting a tunable drug delivery pattern were prepared using the sol-gel method from PEO (poly(ethylene oxide)) and PPO (poly(propylene oxide)) functionalized at both chain ends with triethoxysilane. Different polyether chain lengths were used to control the urea/siloxane (named ureasil) node density, flexibility, and swellability of the hybrid network. We herein demonstrate that the drug release from swellable hydrophilic ureasil-PEO hybrids can be sustained for some days, whereas that from the unswellable ureasil-PPO hybrids can be sustained for some weeks. This outstanding feature conjugated with the biomedically safe formulation of the ureasil cross-linked polyether-siloxane hybrid widens their scope of application to include the domain of soft and implantable drug delivery devices.

LC Evaluation of In Vitro Release of AZT from Microemulsions

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Thermal analysis of biodegradable microparticles containing ciprofloxacin hydrochloride obtained by spray drying technique

Thermal analysis has been extensively used to obtain information about drug-polymer interactions and to perform pre-formulation studies of pharmaceutical dosage forms. In this work, biodegradable microparticles of poly(D,L-lactide-co-glycolide) (PLGA) containing ciprofloxacin hydrochloride (CP) in various drug:polymer ratios were obtained by spray drying. The main purpose of this study was to investigate the effect of the spray drying process on the drug-polymer interactions and on the stability of microparticles using differential scanning calorimetry (DSC), thermogravimetry (TG) and derivative thermogravimetry (DTG) and infrared spectroscopy (IR). The results showed that the high levels of encapsulation efficiency were dependant on drug:polymer ratio. DSC and TG/DTG analyses showed that for physical mixtures of the microparticles components the thermal profiles were different from those signals obtained with the pure substances. Thermal analysis data disclosed that physical interaction between CP and PLGA in high temperatures had occurred. The DSC and TG profiles for drug-loaded microparticles were very similar to the physical mixtures of components and it was possible to characterize the thermal properties of microparticles according to drug content. These data indicated that the spray dryer technique does not affect the physicochemical properties of the microparticles. In addition, the results are in agreement with IR data analysis demonstrating that no significant chemical interaction occurs between CP and PLGA in both physical mixtures and microparticles. In conclusion, we have found that the spray drying procedure used in this work can be a secure methodology to produce CP-loaded microparticles. (C) 2007 Elsevier B.V. All rights reserved.

Modeling a system of phosphated cross-linked high amylose for controlled drug release. Part 1: Synthesis and polymer characterization

High amylose was cross-linked with sodium trimetaphosphate (STMP) using 2% and 4% solutions of NaOH at room temperature with reaction contact times of 0.5, 1, 2 and 4 h. The different polymers obtained were analyzed by FT IR, C-13 and P-31 solid state NMR, SEM and C, H and P elemental analysis. The results were used to propose a two-stage mechanism for phosphate incorporation, the first being kinetically controlled. (C) 2008 Elsevier Ltd. All rights reserved.

Development and In Vitro Evaluation of Surfactant Systems for Controlled Release of Zidovudine

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)

Development and validation of a dissolution test for diltiazem hydrochloride in immediate release capsules

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

Effects of chronic stress on nicotine-induced locomotor activity and corticosterone release in adult and adolescent rats

We examined nicotine-induced locomotion and increase in corticosterone plasma levels in adolescent and adult animals exposed to chronic restraint stress. Adolescent [postnatal day (P) 28-37] and adult (P60-67) rats were restrained for 2 hours once daily for 7 days. Three days after the last exposure to stress, the animals were challenged with saline or nicotine (0.4 mg/kg subcutaneously). Nicotine-induced locomotion was recorded in an activity cage. Trunk blood samples were collected in a subset of adolescent and adult rats and plasma corticosterone levels were determined by radioimmunoassay. Exposure to stress did not affect the nicotine-induced locomotor- or corticosterone-activating effects in both ages.

Metronidazole release using natural rubber latex as matrix

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

Effect of the addition of soy lecithin and Yucca schidigera extract on the properties of gelatin and glycerol based biodegradable films

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

Desenvolvendo e gerenciando compostagem de resíduos sólidos urbanos: para geração de renda e repasse de tecnologia à acrevi

Nowadays, as well as in the past decades, the dumping of biodegradable organic waste in landfill is common practice in Brazil, as well as in most parts of the world. Nevertheless due to its rapid decomposition and release of odors, this practice hamper’s the operation and implementation of a recycling system. These facts encouraged our research to find an efficient system for the management of organic waste, not only for the use of official workers responsible for managing these wastes, but also for non-governmental institutions. The Recycling for Life Community Association – ACREVI (Associação Comunitária Reciclando para a Vida), together with the municipal authorities of Mossoró-RN, Brazil, have assumed the social role of collecting and recycling solid waste produced by most of the local population. However, it was observed that the organic waste it collected was not receiving any treatment. This present work aims to make compost with mixed waste (green waste and organic household), and then do chemical analysis of the material in view to use the waste as organic fertilizer. The objective being: to share the knowledge acquired by putting it into a very simple language accessible to people with little education. The experiment was conducted at ACREVI, Mossoró (RN), and the compost was obtained following the method "windrow", forming three cells (I, II, III) with conical shape, dimensions of 1.6 meters and 2.0 meters in diameter for cells I and II, and 1.0 meters high and 2.0 meters in diameter for cell III. The process was accompanied by analysis: CHN elemental, a variation of cell temperature, humidity, pH, TKN, bulk density, nutrients and heavy metals. Stabilized organic compounds reached the C/N ratio of 10.4/1 cell I and 10.4/1 in the cell II in the cell, showing how good soil conditions, with potential to improve the physical properties of any soil and pH acid soils, has presented the cell III at the end of the process the C/N 26/1, is a high ratio may be associated with the stack size III, thus changing the optimal conditions for the occurrence of the process. The levels of heavy metals in the analyzed compounds were lower than those established by the SDA normative instruction, Nº 27, of 5 June, 2006. The use of pruning trees and grass are used in small-scale composting, while generating a quality compost in the final process, it also created an important condition for a correct sizing of the composting piles. Under the studied conditions it is not advisable to use cells with a height of 1.00 m in height and 2.00 m in diameter, as these do not prevent the rapid dissipation of heat and thus can not be a good product at the end of composting. The composting process in the shed of the association and the preparation of the primer enabled the development of an alternative technology to generate income for members of ACREVI.

Biocompatibilidade e biodegradabilidade de micropartículas de poli-lactato-co-glicolato na ceratite infecciosa em coelhos

Avaliaram-se a biocompatibilidade e a biodegradabilidade do sistema de liberação controlada de poli-lactato-co-glicolato (PLGA) no tratamento com ciprofloxacina das ceratites por Staphylococcus aureus em coelhos. Foram utilizados 20 coelhos, distribuídos em quatro grupos (G). Os animais dos G1, G3 e G4 foram inoculados com 2,5µL da bactéria - 108UFC, no estroma corneano. Os do G2 não receberam a aplicação do inóculo. O tratamento foi realizado com solução salina básica para os animais do G1, micropartículas de PLGA contendo ciprofloxacina nos animais dos G2 e G4 e colírio de ciprofloxacina naqueles do G3. Suabe e biópsia da superfície ocular foram coletados para cultura. Apenas um animal do G1 apresentou cultura positiva para S. aureus. Exame histológico revelou a presença bacteriana em todos os animais do G1 e em dois animais do G3. Também foi constatada reação inflamatória no local da aplicação do sistema de liberação controlada. O tratamento com micropartículas de PLGA foi eficiente no tratamento de ceratites bacterianas, ao eliminar por completo a presença do S. aureus, mas entretanto não foi completamente biocompatível e biodegradável após cinco dias.

Mineral trioxide aggregate stimulates macrophages and mast cells to release neutrophil chemotactic factors: role of IL-1 beta, MIP-2 and LTB4

Objective. In the present study, the role of macrophages and mast cells in mineral trioxide aggregate (MTA)-induced release of neutrophil chemotactic factor was investigated.Study design. MTA suspension (50 mg/mL) was plated over inserts on macrophages or mast cells for 90 minutes. Untreated cells served as controls. Cells were washed and cultured for 90 minutes in RPMI without the stimuli. Macrophages and mast cell supernatants were injected intraperitoneally (0.5 mL/cavity), and neutrophil migration was assessed 6 hours later. In some experiments, cells were incubated for 30 minutes with dexamethasone (DEX, 10 mu M/well), BWA4C (BW, 100 mu M/well) or U75302 (U75, 10 mu M/well). The concentration of Leukotriene B-4 (LTB4) in the cell-free supernatant from mast cells and macrophage culture was measured by ELISA.Results. Supernatants from MTA-stimulated macrophages and mast cells caused neutrophil migration. The release of neutrophil chemotactic factor by macrophages and mast cells was significantly inhibited by DEX, BW, or U75. Macrophages and mast cells expressed mRNA for interleukin-1 (IL-1)beta and macrophage inflammatory protein-2 (MIP-2) and the pretreatment of macrophages and mast cells with DEX, BW, or U75 significantly altered IL-1 beta and MIP-2 mRNA expression. LTB4 was detected in the MTA-stimulated macrophage supernatant but not mast cells.Conclusions. MTA-induces the release of neutrophil chemotactic factor substances from macrophages and mast cells with participation of IL-1 beta, MIP-2, and LTB4. (Oral Surg Oral Med Oral Pathol Oral Radiol Endod 2010; 109: e135-e142)