2 results
Production and characterization of hypromellose phthalate nanoparticles containing levofloxacin for ophthalmic applications
- P. Paradiso, M.A. Rodrigues, R. Colaço, B. Saramago, A.P. Serro
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- Journal:
- Microscopy and Microanalysis / Volume 19 / Issue S4 / August 2013
- Published online by Cambridge University Press:
- 06 August 2013, pp. 151-152
- Print publication:
- August 2013
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Although eyedrops are nowadays the most used administration form of ophthalmic drugs, they present several problems: they imply repeated applications, lead to significant drug losses, and may cause undesirable side effects, as a result of the rapid drug absorption into the blood stream. Several attempts have been made to develop new drug delivery systems, which increase the residence time of the drugs in the eye and improve its bioavailability. Therapeutic soft contact lenses (SCLs) seem to constitute a promising alternative due to the prolonged contact with the eye. Although drug soaked contact lenses have demonstrated to be more efficient than eyedrops, they still present limitations: maximum drug load is limited and diffusion is the only resistance to drug transport across the gel, which may lead to short release times. Designing an effective system for the treatment of ocular diseases is a challenging task, to which nanotechnologies may give a valuable contribution. The incorporation of drug-loaded nanostructures in the SCLs materials may help to control the drug release rates and to maintain drug therapeutic levels for longer periods of time.
The main objective of this work is to produce hypromellose phthalate (HPP 50) nanoparticles (NPs) containing levofloxacin (LOF) to incorporate in hydrogels for SCLs. LOF is an antibiotic which offers a broad spectrum against ocular infections and is used both in prophylaxis and treatment. The NPs were produced using a supercritical atomization process developed by the research team - Supercritical Enhanced Atomization (SEA) and were engineered in order to improve the release rate of LOF. Different working pressures, LOF concentrations and polymer+antibiotic starting solution concentrations were tested. The morphology and size of the obtained particles were analysed by scanning electron microscopy (SEM) (Figure 1). The release profiles of the drug were determined using a standard dissolution tester. The quantification of the drug in the supernatant was done by high performance liquid chromatography (HPLC). The particles which presented the best release rate were SEA 15 (Figure 2), containing 10% w/w of LOF and produced at 20 MPa with a concentration of polymer+antibiotic of 5 mg/mL. These particles were further characterized by dynamic light scattering (DLS) (Figure 3), which confirmed the wide size dispersion of the particles, and by zeta potential measurements, which gave a slightly negative potential, -10 mV.
Future work may involve both the optimization of the experimental conditions to decrease the size dispersion of the particles and their eventual coating with polyelectrolytes in order to extend the drug release time.
This study was financially supported by the project PEst- OE/QUI/UI0100/2011. Patrizia Paradiso acknowledges grant from the project SFRH/BD/71990/2010.
A microscopic perspective of a microreactor
- F. Carvalho, P. Paradiso, P. Fernandes
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- Journal:
- Microscopy and Microanalysis / Volume 19 / Issue S4 / August 2013
- Published online by Cambridge University Press:
- 06 August 2013, pp. 33-34
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- August 2013
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The use of microreactors in (bio)chemical processes has been gaining relevance in the last decade. The low consumption of reagents, the possibility of continuous operation and the faster translation from lab- to production scale are some of the several advantages of these devices. The whole results in cost reductions in process development. Enzyme catalyzed reactions have proved to be an excellent alternative to the use of chemicals due to its ability to catalyze the most complex chemical processes under benign experimental and environmental conditions. In this way, enzymes may be crucial to the implementation of a much more sustainable chemical industry.
The present work is within such scope, using as model system the immobilization of invertase in glass (silica) microchannels, for the production of fructose syrups through sucrose hydrolysis. The immobilization of the enzyme was achieved through treatment of the substrate with a sequence of coatings (Figure 1). Activation of the inner surface of the microchannels with 3-aminopropyltriethoxysilane (APTES) was followed by the introduction of a spacer, glutaraldehyde. Lastly the enzyme solution was introduced in the presence of sodium cyanoborohydride, in order to enhance the stability of the support-enzyme binding.
The characterization of the coatings at each stage of the immobilization protocol was carried out to confirm the change of the microchannel surface. Such studies were performed using Atomic Force Microscopy (AFM) and Scanning Electron Microscopy (SEM) analysis (Figure 1).
The results obtained, namely the shifts on the surface roughness corroborate that the several coatings were successfully applied and the enzyme immobilized. Moreover, the immobilization approach used proved to be highly effective, resulting on successful continuous use of the microreactor for a period of 30 days with roughly constant full conversion of a sucrose solution of 50g/l, at a flow rate of 7µl/minute (Figure 2).
Future work will involve a more extensive characterization of the several coatings by Quartz Crystal Microbalance which will be decisive to achieve a better comprehension of the coating phenomena and hence optimize the immobilization process.
The authors would like to thank Fundação para a Ciência e a Tecnologia, Portugal, for financial support through contracts under the program Ciência 2007 awarded to P. Fernandes, for the doctoral grant SFRH/BD/74818/2010 awarded to F. Carvalho and for the doctoral grant SFRH/BD/71990 /2010 awarded to Patrizia Paradiso.