Pharmaceutical nanotechnology
Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products

https://doi.org/10.1016/j.ijpharm.2008.10.003Get rights and content

Abstract

Solid lipid nanoparticles (SLN) are distinguishable from nanostructured lipid carriers (NLC) by the composition of the solid particle matrix. Both are an alternative carrier system to liposomes and emulsions. This review paper focuses on lipid nanoparticles for dermal application. Production of lipid nanoparticles and final products containing lipid nanoparticles is feasible by well-established production methods. SLN and NLC exhibit many features for dermal application of cosmetics and pharmaceutics, i.e. controlled release of actives, drug targeting, occlusion and associated with it penetration enhancement and increase of skin hydration. Due to the production of lipid nanoparticles from physiological and/or biodegradable lipids, this carrier system exhibits an excellent tolerability. The lipid nanoparticles are a “nanosafe” carrier. Furthermore, an overview of the cosmetic products currently on the market is given and the improvement of the benefit/risk ratio of the topical therapy is shown.

Introduction

At the beginning of the 1990s there were only the research groups of Müller (Berlin, Germany), Gasco (Turin, Italy) and Westesen (Braunschweig, Germany) working on lipid nanoparticles. Currently more than 20 research groups are working on lipid nanoparticles world wide, estimated by the published articles. This proves the increasing interest in the field of lipid nanoparticles. Lipid nanoparticles have been investigated for various pharmaceutical applications, e.g. parenteral (Wissing et al., 2004a, Blasi et al., 2007, Bondi et al., 2007, Brioschi et al., 2007), peroral (Müller et al., 2006, Martins et al., 2007, Sarmento et al., 2007, Yuan et al., 2007), dermal (Müller et al., 2002, Priano et al., 2007), ocular (Ugazio et al., 2002, Attama and Müller-Goymann, 2008) and pulmonary (Xiang et al., 2007, Liu et al., 2008) administration. Moreover, since the last decade, they have been studied intensively for dermal application, both in pharmaceutical and cosmetic uses. This review paper provides an overview of the ongoing research in cosmetic and pharmaceutical dermal preparations containing SLN or NLC. The production technology of these lipid nanoparticles and preparation of lipid nanoparticles containing products for dermal application is presented. Furthermore, the excellent tolerability of these carriers for dermal application is outlined and discussed based on available data.

Section snippets

What exactly are lipid nanoparticles?

Solid lipid nanoparticles (SLN) were developed at the beginning of the 1990s as an alternative carrier system to emulsions, liposomes and polymeric nanoparticles. SLN are produced by replacing the liquid lipid (oil) of an o/w emulsion by a solid lipid or a blend of solid lipids, i.e. the lipid particle matrix being solid at both room and body temperature (Lucks and Müller, 1991). SLN are composed of 0.1% (w/w) to 30% (w/w) solid lipid dispersed in an aqueous medium and if necessary stabilized

Production and incorporation into creams

Many different techniques for the production of lipid nanoparticles have been described in the literature. These methods are high pressure homogenization (Liedtke et al., 2000, Mehnert and Mäder, 2001, Wissing et al., 2004a), microemulsion technique (Gasco, 1993, Gasco, 1997, Priano et al., 2007), emulsification-solvent evaporation (Sjöström and Bergenstahl, 1992), emulsification-solvent diffusion method (Hu et al., 2002, Trotta et al., 2003), solvent injection (or solvent displacement) method (

Science-based cosmetics: formulations and products

Both NLC and SLN have many features that are advantageous for dermal application. They are colloidal carriers providing controlled release profiles for many substances. They are composed of physiological and biodegradable lipids exhibiting low toxicity and low cytotoxicity, that means an excellent tolerability. The small size ensures a close contact to the stratum corneum and can increase the amount of drug penetrated into the skin. Due to the occlusive properties of lipid nanoparticles, an

Pharmaceutical formulations and benefits

Topical treatment of skin diseases has the advantage that high drug levels can be achieved at the site of disease and systemic side effects can be reduced compared to oral or parenteral drug administration. Topical drug administration is still a challenge in pharmaceutics due to the difficulties in controlling and determining the exact amount of drug that reaches the different skin layers. The drugs and the vehicles physicochemical properties are considered to be the main features responsible

Lipid nanoparticles: a “nanosave” carrier

During the last decade there was an increasing hype about nanotechnology in almost any discipline, ranging from computer technology via products of daily life (e.g. coating of clothes, supratex) to cosmetic and pharmaceutical formulations and products. Nanotechnology seemed to open unexpected perspectives (what indeed many nanotechnology products are doing!). Within this enthusiasm about nanotechnology, the potential “dark side” of each technology was forgotten. In the last years there was an

Conclusion and perspectives

SLN and NLC are very well-tolerated carrier systems for dermal application. The production of these carrier systems as well as of lipid nanoparticle containing topical formulations is feasible in laboratory and on large scale. The physical stability of the SLN and NLC in dermal products was proven for various formulations and can be assessed using well-established methods.

Many features of SLN and NLC that are advantageous for dermal application of cosmetic and pharmaceutical products have been

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