Abstract

A redispersible spray-dried formulation containing curcumin-loaded, lipid-core nanocapsules (LNC-C) was developed for oral administration. The neuroprotective activity of curcumin after the spray-drying process was evaluated in vitro. The spray-dried powder (SD-LNC-C) was produced using a drying adjuvant composed of a blend of maltodextrin and L-leucine (90:10 w/w). Acceptable process yield (~ 70%) and drug content (6.5 ± 0.2mgg-1) were obtained. SD-LNC-C was formed by smooth, spherical-shaped particles, and confocal Raman analysis indicated the distribution of the LNC-C on the surface of the leucine/maltodextrin agglomerates. The surface of the agglomerates was formed by a combination of LNC-C and adjuvants, and laser diffraction showed that SD-LNC-C had adequate aqueous redispersion, with no loss of controlled drug release behaviour of LNC-C. The in vitro curcumin activity against the lipopolysaccharide (LPS)-induced proinflammatory response in organotypic hippocampal slice cultures was evaluated. Both formulations (LNC-C and SD-LNC-C) reduced TNF-α to similar levels. Therefore, neuroprotection of curcumin in vitro may be improved by nanoencapsulation followed by spray-drying, with no loss of this superior performance. Hence, the redispersible spray-dried powder proposed here represents a suitable approach for the development of innovative nanomedicines containing curcumin for the prevention/treatment of neurodegenerative diseases.

Highlights

  • IntroductionCurcumin has been commercialized as a flavouring agent, preservative, colouring agent, and food supplement in several countries

  • Electronic supplementary material The online version of this article contains supplementary material, which is available to authorized users.Curcumin has been commercialized as a flavouring agent, preservative, colouring agent, and food supplement in several countries

  • Over the past few years, promising results have been reported for lipid-core nanocapsules (LNC)-C, such as their ability to improve the protection of the central nervous system (CNS), after oral administration in rats, against a cognitive impairment and redox imbalance induced by cigarette smoke [7] and in a model of cognitive impairment induced by the peptide Aβ[1,2,3,4,5,6,7,8,9,10,11,12,13,14,15,16,17,18,19,20,21,22,23,24,25,26,27,28,29,30,31,32,33,34,35,36,37,38,39,40,41,42] [6], as well as its

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Summary

Introduction

Curcumin has been commercialized as a flavouring agent, preservative, colouring agent, and food supplement in several countries. It is a polyphenol derived from the root of the rhizome Curcuma longa (turmeric) [1]. LNC are vesicular structures containing an organogel composed of liquid and solid lipids as the core, which is surrounded by a polymeric wall [8,9]. Using this system to encapsulate a drug-

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