Publications (30) View all
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Article: Dry powder inhalers of gentamicin and leucine: formulation parameters, aerosol performance and in vitro toxicity on CuFi1 cells.
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ABSTRACT: The high hygroscopicity of gentamicin (G) as raw material hampers the production of respirable particles during aerosol generation and prevents its direct use as powder for inhalation in patients suffering from cystic fibrosis (CF). Therefore, this research aimed to design a new dry powder formulation of G studying dispersibility properties of an aminoacid, L-leucine (leu), and appropriate process conditions. Spray-dried powders were characterized as to water uptake, particle size distribution, morphology and stability, in correlation with process parameters. Aerodynamic properties were analyzed both by Single Stage Glass Impinger and Andersen Cascade Impactor. Moreover, the potential cytotoxicity on bronchial epithelial cells bearing a CFTR F508/F508 mutant genotype (CuFi1) were tested. Results indicated that leu may improve the aerosol performance of G-dried powders. The maximum fine particle fraction (FPF) of about 58.3% was obtained when water/isopropyl alcohol 7:3 system and 15-20% (w/w) of leu were used, compared to a FPF value of 13.4% for neat G-dried powders. The enhancement of aerosol efficiency was credited both to the improvement of the powder flowability, caused by the dispersibility enhancer (aminoacid), and to the modification of the particle surface due to the influence of the organic co-solvent on drying process. No significant degradation of the dry powder was observed up to 6 months of storage. Moreover, particle engineering did not affect either the cell viability or cell proliferation of CuFi1 over a 24 h period.International journal of pharmaceutics 04/2012; 426(1-2):100-7. · 2.96 Impact Factor -
Article: In vitro phytotoxicity and antioxidant activity of selected flavonoids.
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ABSTRACT: The knowledge of flavonoids involved in plant-plant interactions and their mechanisms of action are poor and, moreover, the structural characteristics required for these biological activities are scarcely known. The objective of this work was to study the possible in vitro phytotoxic effects of 27 flavonoids on the germination and early radical growth of Raphanus sativus L. and Lepidium sativum L., with the aim to evaluate the possible structure/activity relationship. Moreover, the antioxidant activity of the same compounds was also evaluated. Generally, in response to various tested flavonoids, germination was only slightly affected, whereas significant differences were observed in the activity of the various tested flavonoids against radical elongation. DPPH test confirms the antioxidant activity of luteolin, quercetin, catechol, morin, and catechin. The biological activity recorded is discussed in relation to the structure of compounds and their capability to interact with cell structures and physiology. No correlation was found between phytotoxic and antioxidant activities.International Journal of Molecular Sciences 01/2012; 13(5):5406-19. · 2.60 Impact Factor -
Article: R.P. Aquino, L. Prota, G. Auriemma, A. Santoro, T. Mencherini, G. Colombo, P. Russo. Dry powder inhalers of gentamicin and leucine: formulation parameters, aerosol performance and in vitro toxicity on CuFi1 cells .
Int. J. Pharm. 01/2012; -
Article: Maltodextrin/pectin microparticles by spray drying as carrier for nutraceutical extracts
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ABSTRACT: a b s t r a c t Functional extracts from Fadogia ancylantha, Melissa officinalis and Tussilago farfara posses excellent anti-oxidant and good antimicrobial properties. The unprocessed extracts occur as sticky and low-water-sol-uble materials with penetrating smell. The loading onto maltodextrins matrix, widely used by food and cosmetic industries, is often unsatisfying. The industrial products are not always enough stable to pre-serve the functional properties of natural compounds, also giving practical difficulties for the manufac-turing. This paper reports on the plant extracts encapsulation by spray-drying in a maltodextrin/apple-pectin based matrix. Physicochemical and technological characteristics, organoleptic and antioxidant properties of the resulting powders, were examined and compared to both unprocessed extracts and industrial products. The selected carrier and process conditions led to stable and handling microencap-sulated powder forms with improved water dissolution rate. The made up powder also masked the extracts unpleasant smell making them suitable for successive manufacturing to produce functional com-ponents for foods or nutraceuticals purposes.Journal of Food Engineering 04/2011; · 2.41 Impact Factor -
Article: Non-steroidal anti-inflammatory drug for pulmonary administration: design and investigation of ketoprofen lysinate fine dry powders.
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ABSTRACT: Pulmonary inflammation is an important therapeutic target in cystic fibrosis (CF) patients, aiming to limit and delay the lung damage. The purpose of the present research was to produce respirable engineered particles of ketoprofen lysinate, a non-steroidal anti-inflammatory drug able to fight lung inflammatory status by direct administration to the site of action. Micronized drug powders containing leucine as dispersibility enhancer were prepared by co-spray drying the active compound and the excipient from water or hydro-alcoholic feeds. Microparticles were fully characterized in terms of process yield, particle size distribution, morphology and drug content. The ability of the drug to reach the deepest airways after aerosolization of spray-dried formulations was evaluated by Andersen Cascade Impactor, using the monodose DPI as device. In order to investigate the behaviour of the drug once in contact with lung fluid, an artificial CF mucus was prepared. Drug permeation properties were evaluated interposing the mucus layer between the drug and a synthetic membrane mounted in Franz-type diffusion cells. Finally, the effect of the engineered particles on vitality of human airway epithelial cells of patients homozygous for ΔF 508 CF (CuFi1) was studied and compared to that of raw active compound. Results indicated that powders engineering changed the diameter and shape of the particles, making them suitable for inhalation. The mucus layer in the donor compartment of vertical diffusion cells slowed down drug dissolution and permeation, leucine having no influence. Cell proliferation studies evidenced that the spray drying process together with the addition of leucine reduced the cytotoxic effect of ketoprofen lysine salt as raw material, making the ketoprofen lysinate DPI a very promising product for the inflammation control in CF patients.International journal of pharmaceutics 03/2013; · 2.96 Impact Factor
