Influence of different surfactants on the technological properties and in vivo ocular tolerability of lipid nanoparticles

[Display omitted] Addition of one or more surfactant agents is often necessary for the production of nanostructured lipid and polymeric systems. The removal of residual surfactants is a required step for technological and toxicological reasons, especially for peculiar applications, such as the ophth...

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Bibliographic Details
Published in:International journal of pharmaceutics 2014-08, Vol.470 (1-2), p.133-140
Main Authors: Leonardi, Antonio, Bucolo, Claudio, Romano, Giovanni Luca, Platania, Chiara Bianca Maria, Drago, Filippo, Puglisi, Giovanni, Pignatello, Rosario
Format: Article
Language:English
Subjects:
Animals
Drug Carriers - administration & dosage
Drug Carriers - chemistry
Drug Stability
Eye - drug effects
Eye - pathology
Eye tolerability
Irritants - administration & dosage
Irritants - chemistry
Lipids - administration & dosage
Lipids - chemistry
Male
Nanoparticles - administration & dosage
Nanoparticles - chemistry
Ocular drug delivery systems
Ocular safety
Particle Size
Rabbits
Solid lipid nanoparticles
Surface-Active Agents - administration & dosage
Surface-Active Agents - chemistry
Surfactants
Toxicity Tests, Acute
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Summary:[Display omitted] Addition of one or more surfactant agents is often necessary for the production of nanostructured lipid and polymeric systems. The removal of residual surfactants is a required step for technological and toxicological reasons, especially for peculiar applications, such as the ophthalmic field. This study was planned to assess the technological properties of some surfactants, commonly used for the production of lipid nanoparticles, as well as their ocular safety profile. Stable and small-size solid lipid nanoparticles were obtained using Dynasan® 114 as the lipid matrix and all the tested surfactants. However, from a toxicological point of view, the nanocarriers produced using Kolliphor® P188 were the most valuable, showing no irritant effect on the ocular surface up to the highest tested surfactant concentration (0.4%, w/v). The SLN produced using Cremophor® A25 and Lipoid® S100 were tolerated up to a surfactant concentration of 0.2% by weight, while for Tween® 80 and Kolliphor® HS 15 a maximum concentration of 0.05% can be considered totally not-irritant.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2014.04.061