Carla Martins Lopes

Effect of polymer viscosity on physicochemical properties and ocular tolerance of FB-loaded PLGA nanospheres

Poly(lactide-co-glycolide) acid (PLGA) nanospheres incorporating flurbiprofen (FB) were produced by the solvent displacement technique, for ocular applications aiming to avoid/minimize inflammation induced by surgical trauma. In this work, a PLGA of low viscosity has been tested and the results obtained were compared with those previously reported by Vega et al. The physicochemical properties of the developed formulations were evaluated by measuring particle size, zeta potential and FB entrapment efficiency, showing no significant differences. Release studies demonstrated that the formulation produced with PLGA of higher viscosity revealed a slower drug release rate. Stability analysis, for a period of 75 days, was performed using three complementary methods: (i) turbidity experiments using a Turbiscan optical analyzer, (ii) particle size measurements, and (iii) zeta potential analysis. The results revealed long-term physicochemical stability suitability for ophthalmic use, being independent from the polymer viscosity. The ocular tolerance was assessed by an alternative in vitro method to animal experimentation, the HET-CAM. For all developed formulations no ocular irritancy has been detected.

Cationic solid lipid nanoparticles (cSLN): Structure, stability and DNA binding capacity correlation studies

Cationic solid lipid nanoparticles (cSLN) are promising lipid nanocarriers for intracellular gene delivery based on well-known and widely accepted materials. cSLN containing single-chained cationic lipid cetyltrimethylammonium bromide were produced by high pressure homogenization and characterized in terms of (a) particle size distribution by photon correlation spectroscopy (PCS) and laser diffractometry (LD), (b) thermal behaviour using differential scanning calorimetry (DSC) and (c) the presence of various polymorphic phases was confirmed by X-ray diffraction (WAXD). SLN composed of Imwitor 900P (IMW) showed different pDNA stability and binding capacity in comparison to those of Compritol 888 ATO (COM). IMW-SLN, having z-ave=138-157 nm and d(0.5)=0.15-0.158 μm could maintain this size for 14 days at room temperature. COM-SLN had z-ave=334 nm and d(0.5)=0.42 μm on the day of production and could maintain similar size during 90 days. IMW-SLN revealed improved pDNA binding capacity. We attempted to explain these differences by different interactions between the solid lipid and the tested cationic lipid.

Modified Rose Bengal assay for surface hydrophobicity evaluation of cationic solid lipid nanoparticles (cSLN)

Surface hydrophobicity of nanocarriers influences protein binding and subsequently fate of nanoparticles in blood circulation. Therefore, characterization of surface hydrophobicity of nanocarriers provides important preclinical information. Here, a modified classical adsorption method for the needs of characterization of cationic solid lipid nanoparticles (cSLN) was developed. We have identified possible method limitations that should be considered when performing the analysis, i.e. the problems associated with particle separation from the dispersion and their own absorbance in visible spectrum. We propose two modified methods for performing the assay overcoming the stated limitations. We also discuss here evaluation by different approaches (calculation of binding constants or partitioning quotient) and their suitability for the prepared cSLN formulation. Overall, we confirmed that our modified adsorption method can provide useful information about surface properties of (cationic) SLN, however, performing and evaluation of the assay need special attention in order to obtain the desired results.

Nanobiotechnology approaches for targeted delivery of pharmaceutics and cosmetics ingredients

Nanobiotechnology refers to the ability to create and manipulate biological and bio-chemical materials, devices, and systems at atomic and molecular levels. Nano delivery systems hold great potential to overcome some of the obstacles in bio-pharmaceutical production, such as water soluble/insoluble pharmaceutical drugs and cosmetic ingredients, risks of toxicity, increasing bio-active efficacy, specificity, tolerability and its therapeutic index. Within nanoparticulate carriers, polymeric and lipid nanoparticles have risen to the forefront of bio-technology, having diverse applications in several fields of pharmaceuticals for oral, topical, ocular and intravenous administration, as well as in dermo-cosmetic products.