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Development of polymethacrylate nanospheres as targeted delivery systems for catechin within the gastrointestinal tract

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Abstract

In this study, pH-sensitive nanospheres were fabricated using a polymethacrylate-based copolymer to encapsulate, protect, and release catechin, and thereby overcome its poor water solubility and low oral bioaccessibility. The polymer used was a polymethacrylic acid-co-ethyl acrylate 1:1 copolymer that dissolves above pH 5.5, and so can be used to retain and protect bioactives within the stomach but releases them in the small intestine. Catechin-loaded nanospheres were fabricated using the solvent displacement method. Physicochemical characterization of the nanospheres indicated that they were relatively small (d = 160 nm) and had a high negative charge (ζ = − 36 mV), which meant that they had good stability to aggregation under physiological conditions (pH 7.2). Catechin was trapped within the nanospheres at an encapsulation efficiency of about 51% in an amorphous state. A simulated gastrointestinal study showed that catechin was slowly released under gastric conditions (pH 2.5), but rapidly released under small intestine conditions (pH 7.2). The observed improvement in the antioxidant activity and bioaccessibility of catechin after encapsulation was attributed to the fact that it was in an amorphous state and had good water dispersibility. This study provides useful information for the formulation of novel delivery systems to improve the dispersibility, bioaccessibility, and bioactivity of catechin and potentially other active components. These delivery systems could be used to improve the efficacy of bioactive components in foods, supplements, and pharmaceutical products.

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Abbreviations

Cat:

Catechin

PMA:

Polymethacrylic acid-co-ethyl acrylate 1:1 copolymer

NPs:

Nanoparticles

NSs:

Nanospheres

PMA NSs:

PMA nanospheres

Cat-PMA NSs:

Catechin-loaded PMA nanospheres

Eud:

Eudragit L30-D55

GIT:

Gastrointestinal tract

diH2O:

Deionized water

rpm:

Revolutions per minute

PVA:

Polyvinyl alcohol

KBr:

Potassium bromide

HCl:

Hydrochloric acid

NaOH:

Sodium hydroxide

KCl:

Potassium chloride

DMSO:

Dimethyl sulfoxide

PI:

Polydispersity index

ζ :

Zeta potential

SEM:

Scanning electron microscopy

EE:

Drug entrapment efficiency

DPV:

Differential pulse voltammetry

DSC:

Differential scanning calorimetry

XRD:

X-ray diffraction

DRIFT:

Diffuse reflectance of infrared by Fourier transform

mM:

Millimolar

O2•− :

Superoxide anion radicals

NADH:

β-Nicotinamide adenine dinucleotide

NBT:

Nitroblue tetrazolium

PMS:

Phenazine methosulfate

SI:

Small intestine

LI:

Large intestine

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Acknowledgments

The authors thank the National Council for Science and Technology (CONACYT) (Mexico) for scholarship granted. Also, we would like to thank Araceli Mauricio, José Eleazar, and Luz María Aviles for the technical support of DRIFT, SEM, and zeta potential analyses, respectively.

Funding

This work received financial support from the US Department of Agriculture, CREES, NRI and AFRI Grants, and Massachusetts Department of Agricultural Resources.

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Authors and Affiliations

  1. Centro de Investigación y Estudios Avanzados (CINVESTAV) del Instituto Politécnico Nacional, unidad Queretaro, 76230, Queretaro, Mexico

    Hector Pool & Gabriel Luna-Barcenas

  2. Biopolymers and Colloids Research Laboratory, Department of Food Science, University of Massachusetts, Amherst, MA, 01003, USA

    David Julian McClements

  3. Departamento de Investigación y Posgrado en Alimentos, Facultad de Química, Universidad Autónoma de Queretaro, 76010, Queretaro, Mexico

    Sandra Mendoza

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  1. Hector Pool
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  2. Gabriel Luna-Barcenas
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  4. Sandra Mendoza
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Correspondence to Sandra Mendoza.

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Pool, H., Luna-Barcenas, G., McClements, D.J. et al. Development of polymethacrylate nanospheres as targeted delivery systems for catechin within the gastrointestinal tract. J Nanopart Res 19, 324 (2017). https://doi.org/10.1007/s11051-017-4007-3

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