Resveratrol-Loaded Lipid Nanocarriers: Correlation between In Vitro Occlusion Factor and In Vivo Skin Hydrating Effect.

Lucia Montenegro,Carmela Parenti,Rita Turnaturi,Lorella Pasquinucci

doi:10.3390/pharmaceutics9040058

Lucia Montenegro, Carmela Parenti + Show 2 more

Open Access

https://doi.org/10.3390/pharmaceutics9040058

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Journal: Pharmaceutics	Publication Date: Dec 10, 2017
Citations: 54	License type: CC BY 4.0

Affiliation: University of Catania

Abstract

Lipid nanocarriers show occlusive properties that may be related to their ability to improve skin hydration. The aim of this work was to evaluate the relationship between in vitro occlusion factor and in vivo skin hydration for three types of lipid nanocarriers: nanoemulsions (NEs), solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs). These lipid nanocarriers were loaded with trans-resveratrol (RSV) and incorporated in gel vehicles. In vitro occlusion factor was in the order SLNs > NLCs > NEs. Gels containing unloaded or RSV loaded lipid nanocarriers were applied on the back of a hand of 12 healthy volunteers twice a day for one week, recording skin hydration changes using the instrument Soft Plus. An increase of skin hydration was observed for all lipid nanocarriers (SLNs > NLCs > NEs). RSV loading into these nanocarriers did not affect in vitro and in vivo lipid nanocarriers effects. A linear relationship (r2 = 0.969) was observed between occlusion factor and in vivo increase of skin hydration. Therefore, the results of this study showed the feasibility of using the occlusion factor to predict in vivo skin hydration resulting from topical application of different lipid nanocarriers loading an active ingredient with no inherent hydrating activity.

Highlights

Nanocarriers are colloidal systems whose particles or droplets sizes range between 1 and 1000 nm.In the 1960s, the first colloidal systems consisting of water, oil, and surfactants were defined as microemulsions (MEs) [1], a term that is misleading as the droplets’ sizes of these systems are in the nanometric range (10–100 nm)
As a linear relationship was observed between in vitro occlusion factor and in vivo skin hydration, the results of this study suggest that determining in vitro occlusion factor could be a useful tool to predict the effect on skin hydration of lipid nanocarriers containing active ingredients with no intrinsic hydrating properties
As small-sized lipid nanocarriers are regarded as more occlusive than large-sized ones, in this work we used the phase inversion temperature (PIT) method for NEs, nanostructured lipid carriers (NLCs), and solid lipid nanoparticles (SLNs) preparation owing to the ability of this method to provide small-sized lipid nanocarriers [26,27]

Summary

Introduction

Nanocarriers are colloidal systems whose particles or droplets sizes range between 1 and 1000 nm.In the 1960s, the first colloidal systems consisting of water, oil, and surfactants were defined as microemulsions (MEs) [1], a term that is misleading as the droplets’ sizes of these systems are in the nanometric range (10–100 nm). Being the core of SLNs solid, lipid crystallization may occur during their preparation and storage This phenomenon may induce expulsion of the incorporated drug into the external medium, resulting in poor stability of the formulation. SLNs show low drug loading capacity as the ordered structure of the lipid core can incorporate only small amounts of active ingredients. To overcome these drawbacks, lipid nanoparticles with a less ordered lipid matrix, consisting of mixtures of solid and liquid lipids, were developed and defined as nanostructured lipid carriers (NLCs) [5]. Due to the structure of their lipid core, NLCs showed greater loading capacity

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