References of "Delattre, Luc"
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See detailSolid Lipid Microparticles: Formulation, Preparation, Characterisation, Drug Release and Applications
Jaspart, Séverine ULg; Piel, Géraldine ULg; Delattre, Luc ULg et al

in Expert Opinion on Drug Delivery (2005), 2(1), 75-87

This review details the properties of solid lipid microparticles (SLMs): a promising drug carrier system that has been until now rather unexploited. First, the advantages of SLMs compared with other drug ... [more ▼]

This review details the properties of solid lipid microparticles (SLMs): a promising drug carrier system that has been until now rather unexploited. First, the advantages of SLMs compared with other drug carrier systems are listed. Then an overview of SLM manufacturing compounds and techniques is presented. A detailed discussion of the characteristics of SLMs follows, and includes the determination of particle size distribution, the determination of SLM morphology, the solid-state analysis, the determination of SLM drug loading and the factors influencing it. The in vitro drug release studies that have been carried out so far and the parameters affecting them are also described. Some preliminary in vivo aspects (in vivo drug release studies, biocompatibility studies and in vivo fate) are also considered. [less ▲]

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See detailIn vitro release of salbutamol acetonide from solid lipid nanoparticles
Jaspart, Séverine ULg; Bodson, Cédric; Bertholet, Pascal et al

in Proceedings of 1st Pharmaceutical Sciences Fair and Exhibition (2005)

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See detailEvaluation of the pulmonary inflammation and bronchial hyperresponsiveness in healthy mice induced by inhaled cyclodextrins
Guéders, Maud ULg; Bertholet, P.; Barillaro, Valery et al

in Journal of inclusion Phenomena and Macrocyclic Chesmistry (2005)

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See detailOral bioavailability in pigs of a miconazole/hydroxypropyl-gamma-cyclodextrin/L-tartaric acid inclusion complex produced by supercritical carbon dioxide processing
Barillaro, Valery; Evrard, Brigitte ULg; Delattre, Luc ULg et al

in AAPS Journal (2005), 7(1), 149-155

The objective of this study was to determine the pharmacokinetic parameters of miconazole after oral administration of a miconazole/hydroxypropyl-gamma-cyclodextrin(HPgammaCD)/L-tartaric acid inclusion ... [more ▼]

The objective of this study was to determine the pharmacokinetic parameters of miconazole after oral administration of a miconazole/hydroxypropyl-gamma-cyclodextrin(HPgammaCD)/L-tartaric acid inclusion complex produced by supercritical carbon dioxide processing. The pharmacokinetics of the miconazole ternary complex (CPLX), of the corresponding physical mixture (PHYS), and of miconazole alone (MICO) were compared after oral administration. Six mixed-breed pigs received each formulation as a single dose (10 mg miconazole/kg) in a crossover design. Miconazole plasma concentrations were determined by a high-performance liquid chromatography method. Preliminary in vitro dissolution data showed that CPLX exhibits a faster and higher dissolution rate than either PHYS or MICO. Following CPLX oral administration, mean area under the plasma concentration curve (AUC(0-infinity)) for miconazole was 95.0 +/- 55.8 microg/min/mL, with the peak plasma concentration (C(max) 0.59 +/- 0.39 microg/mL) at 19.30 minutes. The AUC(0-infinity) and C(max) values were significantly higher than those after oral administration of PHYS (AUC(0-infinity) 38.5 +/- 12.7 microg/min/mL and C(max) 0.24 +/- 0.08 microg/mL; P < .1) and of MICO (AUC(0-infinity) 24.1 +/- 14.0 microg/min/mL and C(max) 0.1 +/- 0.05 microg/mL; P < .1). There were also significant differences between PHYS and MICO (P < .1). The results of the study indicate that CPLX shows improved dissolution properties and a higher relative oral bioavailability compared with PHYS and MICO. [less ▲]

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See detailThe Effect of Cyclodextrins on the Aqueous Solubility of a New Mmp Inhibitor: Phase Solubility, 1 H-Nmr Spectroscopy and Molecular Modeling Studies, Preparation and Stability Study of Nebulizable Solutions
Bertholet, Pascal; Guéders, Maud ULg; Dive, Georges ULg et al

in Journal of Pharmacy & Pharmaceutical Sciences : A Publication of the Canadian Society for Pharmaceutical Sciences (2005), 8(2), 164-175

PURPOSE: Ro 28-2653 (RO) is a synthetic inhibitor of matrix metalloproteinases (MMPs), which is potentially effective against bronchial remodeling. Given that this molecule has very poor aqueous ... [more ▼]

PURPOSE: Ro 28-2653 (RO) is a synthetic inhibitor of matrix metalloproteinases (MMPs), which is potentially effective against bronchial remodeling. Given that this molecule has very poor aqueous solubility, different cyclodextrins (CDs) have been tested to increase its solubility. The aim of this study was to prepare and to characterize inclusion complexes between RO and CDs, in order to develop nebulizable solutions. METHODS: The complex formation was investigated by phase solubility studies. (1)H-NMR spectroscopy and molecular modeling studies were carried out to elucidate the structure of the inclusion complex between RO and dimethyl-beta-CD (DIMEB). Nebulizable solutions of RO were developed with CDs and a stability study was performed over 9 months. RESULTS: The phase solubility studies showed that beta-CD and its derivatives form a 1:2 complex with RO, whereas gamma-CD includes RO with a 1:1 stoichiometry and a weak stability constant. T-ROESY spectra showed that DIMEB is able to complex two RO substituents (nitrophenyl and biphenyl groups) with preferential orientations, while molecular modeling demonstrated that the configurations observed with (1)H-NMR are energetically favorable, especially owing to H-bond formation between RO and DIMEB. Two CDs were selected to develop nebulizable solutions of RO and the stability study demonstrated that RO degradation in solution is strongly dependent on the concentration of the 1:2 inclusion complex. CONCLUSIONS: CDs are able to include RO and to improve its aqueous solubility. The beta-CD derivatives can be used to formulate nebulizable solutions of RO, the stability of which depends on the concentration of the 1:2 complex. [less ▲]

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See detailEffect of acidic ternary compounds on the formation of miconazole/cyclodextrin inclusion complexes by means of supercritical carbon dioxide
Barillaro, Valery; Bertholet, Pascal; Henry de Hassonville, Sandrine et al

in Journal of Pharmacy & Pharmaceutical Sciences : A Publication of the Canadian Society for Pharmaceutical Sciences (2004), 7(3), 378-388

PURPOSE: The aim of the study is to evaluate the effect of different acidic compounds on the inclusion of miconazole (MICO) in several cyclodextrins (CDs) using supercritical carbon dioxide (SCCO(2 ... [more ▼]

PURPOSE: The aim of the study is to evaluate the effect of different acidic compounds on the inclusion of miconazole (MICO) in several cyclodextrins (CDs) using supercritical carbon dioxide (SCCO(2) ) processing. METHODS: Physical mixtures were processed by SCCO(2) at 30 MPa, 125 degrees C during 60 minutes in a static mode to produce inclusion complexes. The inclusion complexes were characterized by differential solubility, Fourier transform infrared spectroscopy (FT-IR) and dissolution test. RESULTS: The best inclusion yields were achieved with the combination of MICO base and HPgammaCD with or without acids. Maleic and fumaric acids influenced the MICO inclusion differently in function of their conformation. During the process, a miconazole salt was observed with maleic acid and characterized by thermal analysis and mass spectrometry. The kinetics inclusion followed a saturation-type shape curve. FT-IR confirmed the presence of genuine inclusion complexes. The complexes MICO base/HPgammaCD/(L-tartaric acid) enhanced the dissolution rates of MICO more than the corresponding physical mixtures did. Lastly, the stability study revealed that the complexes were stable. CONCLUSIONS: The formation of stable complexes between MICO and CDs is possible using SCCO(2). Moreover an acidic ternary compound is able to modify the formation of the complex. The inclusion complexes, which show better dissolution profiles than those with the corresponding physical mixtures, could lead to an increase of the oral bioavailability of MICO. [less ▲]

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See detailDevelopment and validation of a high-performance liquid chromatographic method for the determination of cyproterone acetate in human skin
Henry de Hassonville, Sandrine; Chiap, Patrice ULg; Liégeois, Jean-François ULg et al

in Journal of Pharmaceutical & Biomedical Analysis (2004), 36(1), 133-143

In the framework of a preliminary study on the transdermal penetration of cyproterone acetate (CPA), a simple and rapid procedure involving an extraction step coupled to a HPLC-UV determination has been ... [more ▼]

In the framework of a preliminary study on the transdermal penetration of cyproterone acetate (CPA), a simple and rapid procedure involving an extraction step coupled to a HPLC-UV determination has been developed for the separation and quantification of CPA in the two main skin layers-epidermis and dermis-after local application. The separation of epidermis and dermis layers was carefully carried out by means of a sharp spatula after skin immersion in heated water at 65 degrees C. The two skin layers were then treated separately according to the same process: (1) sample homogenization by vibration after freezing with liquid nitrogen in a Mikro-Dismembrator; (2) CPA extraction with methanol after addition of the internal standard (betamethasone dipropionate); (3) centrifugation; (4) evaporation of a supernatant aliquot; (5) dissolution of the dry residue in methanol and addition of water; (6) centrifugation; (7) injection of a supernatant aliquot into the HPLC system. The separation was achieved on octadecylsilica stationary phase using a mobile phase consisting in a mixture of acetonitrile and water (40:60 (v/v)). The method was then validated using a new approach based on accuracy profiles over a CPA concentration range from 33 to 667 ng/ml for each skin layer. Finally, the method was successfully applied to the determination of CPA to several skin samples after topical application of different gel formulations containing CPA. [less ▲]

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See detailModulation of the arachidonic cascade with omega 3 fatty acids or analogues: Potential therapeutic benefits
Roland, Isabelle ULg; de Leval, X.; Evrard, Brigitte ULg et al

in Mini-Reviews in Medicinal Chemistry (2004), 4(6), 659-668

Increasing interest in the role of omega 3 fatty acids has arisen in these latest years since evidence of their implication in the cardioprotective fish based diet of the Inuit has been demonstrated ... [more ▼]

Increasing interest in the role of omega 3 fatty acids has arisen in these latest years since evidence of their implication in the cardioprotective fish based diet of the Inuit has been demonstrated. Furthermore, several in vitro, in vivo and epidemiological studies support the benefit of this fatty acids intake in various pathological states such as in the cardiovascular, cancer, inflammation, psychiatric, paediatric, pulmonary, dermatological and ophthalmologic fields. This review will focus on metabolism and pharmacological implication of w3 fatty acids intake as well as its interest in the prevention or treatment of the above-mentioned pathologies. [less ▲]

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See detailInfluence of methyl-b-cyclodextrin on the relase kinetics of inulin encapsulated in bioadhesive liposomes
Piel, Géraldine ULg; Boulmedarat, Laila; Bochot, Amélie et al

Poster (2004, May)

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See detailEffect of methylated-b-cyclodextrin on the skin and influence on cyproterone acetate percutaneous absorption
Henry de Hassonville, Sandrine; Christiaens, Benoit; Piel, Géraldine ULg et al

Poster (2004, May)

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See detailEvaluation of the pulmonary inflammation and the bronchial hyperresponsiveness in healthy mice induced by inhaled cyclodextrins
Guéders, Maud ULg; Bertholet, Pascal; Barillaro, Valery et al

Conference (2004, May)

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See detailSolid lipid Nanoparticles for administration by inhalation : Optimisation of manufacturing parameters
Jaspart, Séverine ULg; Bodson, Cédric; Bertholet, Pascal et al

Conference (2004)

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See detailPreparation and in vivo toxicity study of solid lipid microparticles as carrier for pulmonary administration
Sanna, V.; Kirschvink, Nathalie; Gustin, Pascal ULg et al

in AAPS PharmScitech (2004), 5(2), 27

The purpose of this research was to investigate the effects of processing conditions on the characteristics of solid lipid microparticles (SLM) with a potential application as carriers for pulmonary ... [more ▼]

The purpose of this research was to investigate the effects of processing conditions on the characteristics of solid lipid microparticles (SLM) with a potential application as carriers for pulmonary administration. Compritol ( 5.0% wt/ wt) SLM dispersions were prepared by rotor-stator homogenization, at different surfactant concentrations and emulsification times. The SLM were characterized, in terms of morphology and size, after lyophilization and sterilization by autoclaving process. In vivo assessment was carried out in rats by intratracheal instillation of either placebo or SLM dispersion, and by bronchoalveolar lavage for cytological analysis. Mean particle size of 4 to 5 mum was achieved using 0.3% and 0.4% ( wt/ wt) of emulsifier ( Poloxamer 188) and emulsification times of 2 and 5 minutes. The particles showed spherical shape and smooth surface. The morphology of microparticles, the size, and the size distribution were not substantially modified after lyophilization and sterilization. Total cell counts showed no significant differences between placebo and SLM 0.5% or 2.5% groups. Regarding cytology, percentage of polymorphonuclear neutrophils and macrophages did not significantly differ between groups. These results suggest that a single intratracheal administration of the SLMs does not induce a significant inflammatory airway response in rats and that the SLMs might be a potential carrier for encapsulated drug via the pulmonary route. [less ▲]

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See detailDelivery of granulocyte-macrophage colony-stimulating factor in bioadhesive hydrogel stimulates migration of dendritic cells in models human papillomavirus-associated (pre)neoplastic epithelial lesions
Hubert, Pascale ULg; Evrard, Brigitte ULg; Maillard, Catherine ULg et al

in Antimicrobial Agents and Chemotherapy (2004), 48(11), 4342-4348

Because of the central role of dendritic cells and/or Langerhans cells(DC/LC) in the induction of cellular immune responses, pharmacological agents that modulate the recruitment of these cells might have ... [more ▼]

Because of the central role of dendritic cells and/or Langerhans cells(DC/LC) in the induction of cellular immune responses, pharmacological agents that modulate the recruitment of these cells might have a clinical interest. The present study was designed to evaluate the capacity of several pharmaceutical formulations to topically deliver granulocyte-macrophage colony-stimulating factor (GM-CSF) on human papillomavirus (HPV)-associated genital (pre)neoplastic lesions. The formulations were evaluated for their bioactivity and for their potential to recruit DC in organotypic cultures of HPV-transformed keratinocytes. We found that a bioadhesive polycarbophil gel (Noveon) at pH 5.5 is able to maintain the bioactivity of GM-CSF at 4 or 37°C for at least 7 days, whereas a decreased activity of GM-CSF was observed when the molecule is included in other polymer gels. GM-CSF incorporated in the polycarbophil gel was also a potent factor in enhancing the colonization of DC into organotypic cultures of HPV-transformed keratinocytes since the infiltration of DC in the in vitro-formed (pre)neoplastic epithelium was very low under basal conditions and dramatically increased in the presence of GM-CSF gel. We next demonstrated that GM-CSF incorporated in polycarbophil gel induces the recruitment of human DC in a human (pre)neoplastic epithelium grafted into NOD/SCID mice. The efficacy of GM-CSF in this formulation was equivalent to that observed with liquid GM-CSF. These results suggest that GM-CSF incorporated in polycarbophil gel could play an important role in the recruitment of DC/LC in mucosal surfaces and be useful as a new immunotherapeutic approach for genital HPV-associated (pre)neoplastic lesions. [less ▲]

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See detailApplication of molecular modeling to the study of cyproterone acetate stability in the presence of cyclodextrin derivatives
Henry de Hassonville, Sandrine; Dive, Georges ULg; Evrard, Brigitte ULg et al

in Journal of Drug Delivery Science and Technology (2004), 14(5, SEP-OCT), 357-362

The ability of cyclodextrins (CDs) to increase the solubility of cyproterone acetate (CPA) was previously shown by phase-solubility and NMR studies [1]. In the present work, the influence of various CDs ... [more ▼]

The ability of cyclodextrins (CDs) to increase the solubility of cyproterone acetate (CPA) was previously shown by phase-solubility and NMR studies [1]. In the present work, the influence of various CDs on the stability of CPA was studied in pH 6 and pH 8 aqueous solutions at 25degreesC. Different CDs were tested: hydroxypropyl-beta-cyclodextrin (HPbetaCD), randomly methylated beta-cyclodextrin (RAMEB), hydroxypropyl-gamma-cyclodextrin (HPgammaCD) and gamma-cyclodextrin (gammaCD). At pH 6, the presence of these CDs reduces the degradation of CPA. Nevertheless, at pH 8, the gamma-CD derivatives are ineffective against the degradation of CPA, whereas the beta-CD derivatives (HPbetaCD and RAMEB) allow decreasing CPA hydrolysis. Molecular modeling was performed to theoretically calculate some of the most energetically favorable conformations for gamma-CD and RAMEB complexes with CPA. The position of the ester group in the CD caivity seems to be the most important factor influencing the hydrolysis of CPA. Other factors, such as the size of the cavity, the substitution of the CD hydroxyls and the stability constant also have a strong incidence on CPA stability. [less ▲]

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See detailLa Rameb, un promoteur d’absorption cutanée pour l’acétate de cypro-térone ?
Henry de Hassonville, S.; Christiaens, B.; Piel, Géraldine ULg et al

Conference (2004)

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