Biomedical subjects

Hatem Fessi

Publications and source records attributed to Hatem Fessi.

23 records · Page 2Linked to original sources

PubMed2004

Enhancement of topical delivery from biodegradable nanoparticles.

PURPOSE: To determine whether and how encapsulation of lipophilic compounds in polymeric nanoparticles is able to improve topical delivery to the skin. METHODS: The penetration of octyl methoxycinnamate (OMC; Parsol MCX), a highly lipophilic sunscreen, into and across porcine ear skin in vitro was investigated, subsequent to encapsulation in poly(epsilon-caprolactone) nanoparticles, using tape-stripping. Confocal laser scanning microscopy (CLSM) was used to visualize the distribution of nanoparticles, charged with Nile red (NR), a lipophilic and fluorescent dye. RESULTS: Quantification of OMC in the skin using tape-stripping demonstrated that nanoparticulate encapsulation produced a 3.4-fold increase in the level of OMC within the stratum corneum (SC), although the use of nanoparticles did not appear to increase skin permeation (it was not possible to detect OMC in the receiver compartment after 6 h). The confocal images showed that the fluorescence profile observed in the skin after application of NR-containing nanoparticles was clearly different from that seen following application of NR dissolved in propylene glycol. Two hours postapplication of NR-containing nanoparticles, fluorescence was perceptible at greater depths (up to 60 microm) within the skin. CONCLUSIONS: i) Nanoparticulate encapsulation of OMC increased its "availability" with the SC. ii) The altered distribution of NR when delivered via nanoparticles was due, at least in part, to its altered thermodynamic activity (relative to that in propylene glycol) and, as a result, an increase in its partition coefficient into the SC.

Administration, Topical↗

PubMed2003

Synthesis and characterisation of sulfated amphiphilic alpha-, beta- and gamma-cyclodextrins: application to the complexation of acyclovir.

The synthesis of sulfated amphiphilic alpha-, beta- and gamma-cyclodextrins was achieved according to the standard protection-deprotection procedure. The formation of inclusion complexes between the amphiphilic alpha-, beta- and gamma-cyclodextrins and an antiviral molecule, acyclovir (ACV) was investigated by UV-visible spectroscopy (UV-Vis) and electrospray ionisation mass spectrometry (ESIMS). UV-Vis spectroscopy allowed determination of the stoichiometry and stability constants of complexes, whereas ESIMS, a soft ionisation technique, allowed the detection of the inclusion complexes. The results showed that the non-sulfated amphiphilic cyclodextrins exhibit a 1:2 stoichiometry with acyclovir, while sulfated amphiphilic cyclodextrins, except gamma-cyclodextrin, exhibit a 1:1 stoichiometry indicating the loss of one interaction site. Non-covalent interactions between acyclovir and non-sulfated amphiphilic cyclodextrins appear to take place both in the cavity of the cyclodextrin and inside the hydrophobic zone generated by alkanoyl chains. In contrast, in the case of sulfated amphiphilic cyclodextrins, the interactions appear to involve only the hydrophobic region of the alkanoyl chains.

Acyclovir↗

PubMed2003

Scanning electron microscopy and atomic force microscopy imaging of solid lipid nanoparticles derived from amphiphilic cyclodextrins.

Scanning electron microscopy (SEM) and atomic force microscopy (AFM) have been applied to the imagery of solid lipid nanoparticles (SLNs) formulated from an amphiphilic cyclodextrin, 2,3-di-o-alkanoyl-beta-cyclodextrin, beta-CD21C6. Comparison of the results shows that the vacuum drying technique used in sample preparation for SEM causes shrinkage in the size of the SLNs, whereas the deposition method used for AFM causes the SLNs to form small clusters. The hydrodynamic diameter determined from photon correlation spectroscopy (PCS) is 359+/-15 nm and the zeta potential is -25 mV.

Cyclodextrins↗

PubMed2002

Molecular recognition by Kluyveromyces of amphotericin B-loaded, galactose-tagged, poly (lactic acid) microspheres.

In an effort to develop a new way of drug delivery, especially for polyenic antifungal molecules, we have incorporated amphotericin B (AmB) into biodegradable galactosylated poly (L-lactic acid) (L-PLA) and poly (L-lactic-co-glycolic acid) (PLGA) microspheres. These drug carriers were prepared by solvent evaporation using an oil/water (o/w) emulsion. The ratio of galactosyl spacers with different chain lengths was 1.74-2.78%. The maximal quantity of AmB encapsulated reported to 100 mg of the galactosylated microspheres was 7.14 mg for L-PLA (encapsulation rate 45% of mole) and 6.42 mg for PLGA derivatives (encapsulation rate 81% of mole). In our yeast model, drug release depended on three factors: (i) presence of galactosylated antennae, (ii) length of galactosyl antenna and (iii) nature of the polymer. More of the AmB trapped in PLGA microspheres was released than from PLA microspheres. These novel functionalised microspheres could be required for the delivering of therapeutic agents according to their recognition to specific cells.

Amphotericin B↗

PubMedDate not supplied

Comparative scale-up of three methods for producing ibuprofen-loaded nanoparticles.

The lack of information related to the scaling-up of technologies used for preparing polymeric nanoparticles (NP) might hinder the introduction of these colloidal carriers into the pharmaceutical market. In the present study, the scale-up of ibuprofen-loaded NP produced by three manufacturing processes--salting-out, emulsification-diffusion and nanoprecipitation--was assessed at pilot-scale by increasing 20-fold the laboratory-batch volume from 60 ml to 1.5l. Eudragit L100-55 and poly(vinyl alcohol) (PVAL) were used as polymer and emulsifying agent, respectively. The influence of the hydrodynamic conditions on the NP characteristics such as mean size, drug content, residual PVAL and morphology was also investigated. At pilot-scale, stirring rates of 790-2000 rpm lead to NP mean sizes ranging from 557 to 174 nm for salting-out and from 562 to 230 nm for emulsification-diffusion. An increase in the stirring rate enhances the droplet break-up phenomenon which leads to the formation of finer emulsion droplets and thus smaller NP. Moreover, the influence of the stirring rate on the mean size of NP can be predicted using a model based on a simple power law. The continuous method used for nanoprecipitation scale-up allows production of NP in a reproducible way over a relatively short time. Finally, for the three methods, NP characteristics were reproduced well at both scales. However, the scale-up process induced a slight reduction in the size and drug loading of NP.

Chemical Precipitation↗