Intracellular availability of poorly soluble drugs from lipid nanocapsules.

Lipid nanocapsules (LNCs) are extensively used as drug carrier systems, due to their small size distribution, biocompatibility and ease of preparation. They are especially useful for lipophilic drugs to overcome physicochemical constraints that limit their efficacy, such as low solubility in aqueous media. The aim of this work was to investigate the relationship between the intracellular availability of poorly soluble drugs delivered via LNCs and their biological efficacy in cells in vitro.

Nanoparticles Targeting Retinal and Choroidal Capillaries In Vivo.

The functionalization of nanoparticles with specific receptor ligands enables their accumulation in targeted tissues and can be used therapeutically to transport drugs or for diagnostic purposes (Parveen et al., Nanomedicine 8:147-166, 2012). We could recently show that targeting endothelial cells in retinal and choroidal capillaries can be realized even under physiological conditions using quantum dots as model nanoparticles functionalized with an integrin-binding peptide (Pollinger et al.

Cyclic RGD peptides target human trabecular meshwork cells while ameliorating connective tissue growth factor-induced fibrosis.

The major risk factor for primary open-angle glaucoma is increased intraocular pressure stemming from elevated outflow resistance in the trabecular meshwork (TM) region. Integrins play a pivotal role in the TM by influencing its biological properties and growth factor signaling. Pathologic changes in the TM are partially mediated by growth factors like connective tissue growth factor (CTGF).

Multivalent nanoparticles bind the retinal and choroidal vasculature.

The angiotensin II receptor type 1 (AT1R), which is expressed in blood vessels of the posterior eye, is of paramount significance in the pathogenesis of severe ocular diseases such as diabetic retinopathy and age-related macular degeneration. However, small molecule angiotensin receptor blockers (ARBs) have not proven to be a significant therapeutic success. We report here on a nanoparticle system consisting of ARB molecules presented in a multivalent fashion on the surface of quantum dots (Qdots).