Maria Inês Ré

Microparticles prepared with poly(hydroxybutyrate-co-hydroxyvalerate) and poly(ε-caprolactone) blends to control the release of a drug model

The objective of this work was to verify the influence of the poly(ϵ-caprolactone) PCL concentration in poly(hydroxybutyrate-co-hydroxyvalerate) P(HBHV)/PCL microparticles, prepared by an emulsion/solvent evaporation process, on the release behavior of a drug. Differential Scanning Calorimetry analyses demonstrated that the preparation process increased the crystallite heterogeneity for the P(HBHV) in the particles. The drug caused an increase in the glass transition of the P(HBHV) in the microparticles. Dexamethasone acetate-loaded microparticles demonstrated drug sustained releases (up to 250 h), which profiles fit the biexponential model. The release of dexamethasone acetate caused an increase in the surface area of the microparticles. The kinetic constants of the sustained phase increased with the augmentation of the PCL content in the blend. The drug release mechanism was dependent on the presence of PCL in the microparticles. A Fickian release was determined for the microparticles prepared exclusively with P(HBHV), while non-Fickian release behaviors were found for the P(HBHV)/PCL microparticles.

Nanoparticle-coated organic-inorganic microparticles: experimental design and gastrointestinal tolerance evaluation

The influences of the spray-drying parameters and the type of nanoparticles (nanocapsules or nanospheres) on the characteristics of nanoparticle-coated diclofenac-loaded microparticles were investigated by using a factorial design 32. Gastrointestinal tolerance following oral administration in rats was evaluated. Formulations were selected considering the best yields, the best encapsulation efficiencies and the lowest water contents, presenting surfaces completely coated by nanostructures and a decrease in the surface areas in relation to the uncoated core. In vitro drug release demonstrated the influence of the nanoparticle-coating on the dissolution profiles of diclofenac. Nanocapsule-coated microparticles presented a protective effect on the gastrointestinal mucosa.

Powder Characteristics of Pantoprazole Delivery Systems Produced in Different Spray-Dryer Scales

ABSTRACT The purpose of this study is to investigate the physical characteristics of pantoprazole-loaded enteric microparticles produced in different spray dryers and operational conditions. In all conditions tested it was possible to obtain powders that presented spherical shape microparticles, with mean sizes from 6.7 to 24.5 µm. The size was affected mainly by initial feed concentration (2.2 or 6.6% w/w). The integrity of microparticles affected surface area (24 to 113 m2/g)and drug release (71 to 98%). All powders presented very poor flow. The powder that presented higher release was produced with 6.6% solution and a rotating disc atomizer.

Surface morphology of spray-dried nanoparticle-coated microparticles designed as an oral drug delivery system

This paper was devoted to studying the influence of coating material (nanocapsules or nanospheres), drug model (diclofenac, acid or salt) and method of preparation on the morphological characteristics of nanoparticle-coated microparticles. The cores of microparticles were obtained by spray drying or evaporation and the coating was applied by spray drying. SEM analyses showed nanostructures coating the surface of nanocapsule-coated microparticles and a rugged surface for nanosphere-coated microparticles. The decrease in their surface areas was controlled by the nanoparticulated system, which was not dependent on microparticle size. Optical microscopy and X-ray analyses indicated that acid diclofenac crystals were present in formulations prepared with the acid as well as in the nanocapsule-coated microparticles prepared with the salt. The control of coating is dependent on the use of nanocapsules or nanospheres and independent of either the characteristics of the drug or the method of preparing the core.