Spray-dried indomethacin-loaded polyester nanocapsules and nanospheres: development, stability evaluation and nanostructure models

• Published in: European journal of pharmaceutical sciences 2002-09, Vol.16 (4), p.305-312
• Main Authors: Raffin Pohlmann, Adriana, Weiss, Valeria, Mertins, Omar, Pesce da Silveira, Nádya, Stanisçuaski Guterres, Sı́lvia
• Format: Article
• Language: English
• Subjects: Capsules; Drug Compounding - methods; Drug Stability; Dynamic light scattering; Hydrogen-Ion Concentration; Indomethacin; Indomethacin - chemistry; Lactic Acid - chemistry; Microspheres; Nanotechnology; Particle Size; Polyesters; Polyesters - chemistry; Polymeric nanoparticles; Polymers - chemistry; Silicon Dioxide - chemistry; Spray-drying; Stability study; Suspensions
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/S0928-0987(02)00127-6

The industrial development of polymeric nanoparticle suspensions, as drug delivery systems, is limited due to the problems in maintaining stability of suspensions. In this work, a spray-drying technique was applied to dry nanocapsule and nanosphere suspensions prepared by nanoprecipitation of polyesters using SiO 2 as adjuvant. Powders obtained from nanocapsules presented stable drug recoveries and morphological characteristics after 5 months. For nanocapsules, nanostructures around 200 nm were observed by scanning electron microscopy (SEM) on the surface of microparticles of SiO 2, whereas for the nanosphere formulation, nanostructures with a reduced diameter (60–90 nm) were observed, despite the particle sizes of each original suspension being similar, when measured by photon correlation spectroscopy (PCS). In order to investigate the morphological aspects of nanocapsule and nanosphere powders, several nanosphere formulations were spray-dried using different concentrations of SiO 2 and a comparative study of the different colloidal systems (nanocapsules, nanospheres, nanoemulsion or nanodispersion) was carried out by PCS. SEM analyses showed that nanostructures with reduced diameter are formed independently of the adjuvant concentration. The dynamic properties of these systems allowed to suggest that the structure of the nanosphere particle (polymer, sorbitan monostearate and polysorbate 80) was a polymeric matrix dispersing the sorbitan monostearate which, when submitted to the spray-drying process in the presence of SiO 2, gave nanostructures presenting diameters around 80 nm covering the microparticles due to the release of lipophilic surfactant from the polymeric matrix.