4.6 Article

Natural extracts into chitosan nanocarriers for rosmarinic acid drug delivery

Journal

PHARMACEUTICAL BIOLOGY
Volume 53, Issue 5, Pages 642-652

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.3109/13880209.2014.935949

Keywords

Antioxidants; oxidative diseases; pharmaceutical nanosystems; polymeric nanoparticles

Funding

  1. Fundacao para a Ciencia e a Tecnologia [SFRH/BD/61423/2009]
  2. National Funds from FCT - Fundacao para a Ciencia e a Tecnologia [PEst-OE/EQB/LA0016/2011]
  3. European Regional Development Fund (ERDF) through the Programa Operacional Factores de Competitividade - COMPETE
  4. Portuguese funds through FCT - Fundacao para a Ciencia e a Tecnologia [PEst-C/SAU/LA0002/2011]
  5. North Portugal Regional Operational Programme (ON.2 - O Novo Norte) under National Strategic Reference Framework (NSRF) [SAESCTN-PIICDT/2011]
  6. Fundação para a Ciência e a Tecnologia [SFRH/BD/61423/2009] Funding Source: FCT

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Context: Nanotechnology can be applied to deliver and protect antioxidants in order to control the oxidative stress phenomena in several chronic pathologies. Chitosan (CS) nanoparticles are biodegradable carriers that may protect antioxidants with potent biological activity such as rosmarinic acid (RA) in Salvia officinalis (sage) and Satureja montana (savory) extracts for safe and innovative therapies. Objective: Development and characterization of CS nanoparticles as a stable and protective vehicle to deliver RA for medical applications using natural extracts as sage and savory. Materials and methods: Antioxidant-CS based nanoparticles were prepared by ionic gelation with sodium tripolyphosphate (TPP), at pH 5.8 with a mass ratio of 7:1 (CS:TPP), with a theoretical antioxidant-CS loading of 40-50%. The nanoparticles were then characterized by different methods such as photon correlation spectroscopy, laser Doppler anemometry, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier-transform infrared (FTIR), high-performance liquid chromatographic (HPLC), association efficiency, and antioxidant activity. Results and discussion: Individual and small sizing nanoparticles, around 300 nm, were obtained. SEM confirmed smooth and spherical nanoparticles after freeze-drying. No chemical interactions were found between antioxidants and CS, after encapsulation, by DSC and FTIR. The association efficiency was 51.2% for RA (with 40% loading) and 96.1 and 98.2% for sage and savory nanoparticles, respectively (both with 50% loading). Antioxidant activity values were higher than 0.0348 eq [Asc. Ac.] g/L/g extract and 0.4251 mu mol/eq Trolox/g extract. Conclusion: The extracts under study are promising vehicles for RA drug delivery in CS nanocarriers.

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