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1.
Pharm Res ; 24(4): 650-61, 2007 Apr.
Article in English | MEDLINE | ID: mdl-17318421

ABSTRACT

PURPOSE: Spray-drying process was used for the development of dried polymeric nanocapsules. The purpose of this research was to investigate the effects of formulation and process variables on the resulting powder characteristics in order to optimize them. MATERIALS AND METHODS: Experimental designs were used in order to estimate the influence of formulation parameters (nanocapsules and silica concentrations) and process variables (inlet temperature, spray-flow air, feed flow rate and drying air flow rate) on spray-dried nanocapsules when using silica as drying auxiliary agent. The interactions among the formulation parameters and process variables were also studied. Responses analyzed for computing these effects and interactions were outlet temperature, moisture content, operation yield, particles size, and particulate density. Additional qualitative responses (particles morphology, powder behavior) were also considered. RESULTS: Nanocapsules and silica concentrations were the main factors influencing the yield, particulate density and particle size. In addition, they were concerned for the only significant interactions occurring among two different variables. None of the studied variables had major effect on the moisture content while the interaction between nanocapsules and silica in the feed was of first interest and determinant for both the qualitative and quantitative responses. The particles morphology depended on the feed formulation but was unaffected by the process conditions. CONCLUSION: This study demonstrated that drying nanocapsules using silica as auxiliary agent by spray drying process enables the obtaining of dried micronic particle size. The optimization of the process and the formulation variables resulted in a considerable improvement of product yield while minimizing the moisture content.


Subject(s)
Colloids , Nanocapsules , Polyesters/chemistry , Research Design , Silicon Dioxide/chemistry , Technology, Pharmaceutical/methods , Chemistry, Pharmaceutical , Densitometry , Desiccation/methods , Drug Compounding , Microscopy, Electron, Scanning , Models, Statistical , Particle Size , Powders , Surface Properties , Temperature , Water/chemistry
2.
Eur J Pharm Sci ; 30(2): 124-35, 2007 Feb.
Article in English | MEDLINE | ID: mdl-17150339

ABSTRACT

Nanoparticles suspensions very often present a physicochemical instability during their storage. In order to overcome this lack of stability and facilitate the handling of these colloidal systems, the water elimination from the aqueous dispersions to obtain a dry solid form appears as the most promising strategy. The present paper reports the use of the spray-drying technique for the nanocapsules (NC) suspensions conversion into redispersible dried solid particles in presence of different water-soluble excipients as drying auxiliaries. Following the combination of additives solutions with NC suspension, the final dispersion homogeneity was favoured, avoiding phase separations. According to the size measurement after a simple atomisation experiment, the NC, which have a thin and fragile shell structure can withstand the shear forces developed for the feed disintegration in droplets. During drying, certain additives molecules are able to act as NC protectors. The physicochemical characterization of the spray-dried powders included an investigation of their properties, such as residual moisture content, particulate density, morphology and redispersion in water. Using a NC concentration of 1% (w/v), the best result was obtained with the preparation containing 10% (w/v) of lactose which led to more desirable powder morphology and favouring NC suspension reconstitution with only approximately 2% of the size distribution in the micrometer range. The spray-drying technique is an attractive method to improve the NC conservation and facilitate future handling.


Subject(s)
Freeze Drying/methods , Nanocapsules/chemistry , Technology, Pharmaceutical/methods , Colloids/chemistry , Colloids/classification , Lactose/chemistry , Mannitol/chemistry , Microscopy, Electron, Scanning , Molecular Weight , Nanocapsules/ultrastructure , Osmolar Concentration , Particle Size , Polymers/chemistry , Polymers/classification , Polysaccharides/chemistry , Povidone/analogs & derivatives , Povidone/chemistry , Powders/chemistry , Solubility , Technology, Pharmaceutical/instrumentation , Technology, Pharmaceutical/trends , Water/chemistry
3.
Int J Pharm ; 325(1-2): 63-74, 2006 Nov 15.
Article in English | MEDLINE | ID: mdl-16872767

ABSTRACT

Up to now, the full potential of polymer-based nanoparticles is not yet exploited because of a lack of stability when conserved in aqueous medium. The present paper reports the water elimination from nanocapsules (NC) dispersions by means of the spray-drying technique with the aim to achieve dried solid forms of interest using colloidal silicon dioxide as drying auxiliary. The influence of formulation parameters on the suspension behaviour and on the powders characteristics was also evaluated. Our findings demonstrated that the mixing protocol, the concentrations of both NC and silica are crucial parameters that affect the feed behaviour and the spray-dried particles characteristics. Interactions occurring in the feed are directed by hydrogen bounds and were more sensitive to the silica concentration than that of NC as evidenced by rheological measurements. The NC are entrapped within solid dried matrixes following their interaction with silica particles in the feed. SEM analyses of the obtained powders showed spherical separated microparticles formed by the association of NC and silica when they are mixed at adequate concentrations in the feed before spray-drying. On the other hand, fused agglomerated particles presenting NC at their surface, characterised by irregular shapes and a strong adhesiveness were prepared when the silica concentration was not sufficient. The surface composition of the spray-dried powders was investigated using the ESCA technique and revealed the NC exclusion from the surface to obtain powders suitable for further handling.


Subject(s)
Freeze Drying/methods , Nanocapsules/chemistry , Polymers/chemistry , Chemistry, Pharmaceutical/methods , Colloids/analysis , Densitometry/instrumentation , Densitometry/methods , Microscopy, Energy-Filtering Transmission Electron/methods , Nanocapsules/analysis , Particle Size , Polymers/analysis , Porosity , Powders , Silicon Dioxide/analysis , Static Electricity , Surface Properties , Suspensions , Technology, Pharmaceutical/methods , Viscosity
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