Preparation of Caffeic Acid Phenethyl Ester-Incorporated Nanoparticles and Their Biological Activity

Lee, Hyo-Young; Jeong, Young‐Il; Kim, Eun Jin; Lee, Kyung Dong; Choi, Sung-Jong; Kim, Yun Jin; Kim, Da Hye; Choi, Ki-Seok

doi:10.1002/jps.24278

Cited by 41 publications

(22 citation statements)

References 31 publications

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“…Caffeic acid phenethyl ester (CAPE), a flavonoid-like compound ( Figure 1), is one of the most active components of honeybee propolis [1]. Numerous biological and pharmacological effects of CAPE have been reported, such as antiviral [2], antioxidant [3], antiallergic [4], anticarcinogenic [5], anti-inflammatory [6], antimicrobial [7], immunomodulatory [8], and anticancer [9,10] activities.…”

Section: Introductionmentioning

confidence: 99%

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Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

Derman

2015

Journal of Nanomaterials

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CAPE loaded PLGA nanoparticles were prepared using the oil in water (o/w) single emulsion solvent evaporation methods. Five different processing parameters including initial CAPE amount, initial PLGA amount, PVA concentration in aqueous phase, PVA volume, and solvent type were screened systematically to improve encapsulation of hydrophobic CAPE molecule, simultaneously minimize particle size, and raise the reaction yield. Obtained results showed that the encapsulation efficiency of the nanoparticles significantly increased with the increase of the initial CAPE amount (p<0.05) and particle size (p<0.05). Furthermore, the particle size is significantly influenced by initial polymer amount (p<0.05) and surfactant concentration (p<0.05). By the optimization of process parameters, the nanoparticles produced70±6% reaction yield,89±3% encapsulation efficiency,-34.4±2.5 mV zeta potential, and163±2 nm particle size with low polydispersity index0.119±0.002. The particle size and surface morphology of optimized nanoparticles were studied and analyses showed that the nanoparticles have uniform size distribution, smooth surface, and spherical shape. Lyophilized nanoparticles with different CAPE and PLGA concentration in formulation were examined forin vitrorelease at physiological pH. Interestingly, the optimized nanoparticles showed a high (83.08%) and sustained CAPE release (lasting for 16 days) compared to nonoptimized nanoparticle.

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Section: Introductionmentioning

confidence: 99%

“…Wang et al reported that the half-life of 5 g/mL CAPE at 37 ∘ C was 0.35 hours [22]. Additionally, poorly water soluble character of CAPE limits its in vivo and in vitro efficacy [1].…”

Section: Introductionmentioning

confidence: 99%

Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

Derman

2015

Journal of Nanomaterials

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“…However, a substantial burst release (32.59-66.72%, depending on the composition) attributed to adsorption of CAPE onto particle surface was observed. Another study reports high anticancer activity of CAPE embedded into poly(ethylene oxide)-bpoly(e-caprolactone) micelles [22]. These studies demonstrate that the encapsulation of CAPE in polymeric nanocarriers can improve its biopharmaceutical properties and anticancer activity.…”

Section: Introductionmentioning

confidence: 83%

Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles

Yoncheva

Tzankova

Yordanov

et al. 2019

Biotechnology & Biotechnological Equipment

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Caffeic acid phenethyl ester (CAPE), a hydrophobic constituent of poplar propolis of valuable biological activity, was immobilized in poly(ethylene oxide)-b-poly(e-caprolactone)-b-poly(ethylene oxide) (PEO-b-PCL-b-PEO) copolymer micelles to improve its solubility in water. CAPE was loaded in the micelles by dialysis, achieving ca. 50% encapsulation efficiency. The drug loaded micelles were characterized with a mean diameter of 39 nm, narrow size distribution and slightly positive zeta-potential (approximately 2 mV). The in vitro release profile showed an improved dissolution behavior of micellar CAPE than pure CAPE. In vitro studies on human hepatoma HepG2 and neuronal SH-SY5Y cells demonstrated that the empty PEO-b-PCL-b-PEO micelles were not cytotoxic, whereas the drug loaded micelles exerted cytotoxic effects proportional to CAPE content. The protective activity of pure and micellar CAPE was investigated in a model of H 2 O 2 induced oxidative damage in HepG2 and SH-SY5Y cells. In both cell types, micellar CAPE exhibited better protective activity against the oxidative damage than pure CAPE at very low concentrations (0.1 mg/mL), which is far from the cytotoxic concentration of CAPE-loaded micelles (71 mg/mL). Consequently, the developed micellar formulation has an improved activity against oxidative damage in hepatic and neuronal cells as comparing to pure CAPE.

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“…The same copolymer-CAPE formulation exerted moderate antimicrobial activity towards S. aureus and methicillin-resistant Staphylococcus aureus (MRSA) (Arasoglu et al 2016). Lee et al (2015) reported on another formulation of CAPE in methoxy poly(ethyleneglycol)-b-poly(ε-caprolactone) NPs with sizes of less than 300 nm, which were stable after liophylisation and reconstitution at concentrations as high as 20 mg/ml. CAPE, loaded in the resulting drug delivery system was effective in vitro by causing a commensurate propapoptotic effects with non-loaded CAPE and a better effectiveness in reducing the migration of CT-26 cells.…”

Section: Pharmaceutical Formulation Approachesmentioning

confidence: 99%

Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems

Yordanov¹

2019

PHAR

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Propolis is a natural product with a plethora of biological effects, utilized by traditional medicine since antiquity. However, its application as a pharmaceutical is hindered by its variable composition and difficult standardization. CAPE has been shown to be a major component of propolis, with a large contribution to its pharmacological effects, among which the anti-inflammatory, antioxidant and antineoplastic have been attracting most attention. The current review article aims to present the cornerstone pharmacological studies of CAPE throughout the years, following its discovery, which confirmed its primary importance among propolis constituents and opened the path to its intensive research as a potential pharmaceutical. We present the diversity of drug delivery systems of CAPE, which have been developed to improve its efficacy in in vitro and in vivo disease models and discuss their primary promises and weaknesses. The increased interest in recent years over more practical approaches of CAPE research such as its pharmaceutical formulation comes to show that it has a potential to become commercialized as a pharmaceutical.

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Preparation of Caffeic Acid Phenethyl Ester-Incorporated Nanoparticles and Their Biological Activity

Cited by 41 publications

References 31 publications

Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

Caffeic Acid Phenethyl Ester Loaded PLGA Nanoparticles: Effect of Various Process Parameters on Reaction Yield, Encapsulation Efficiency, and Particle Size

Evaluation of antioxidant activity of caffeic acid phenethyl ester loaded block copolymer micelles

Caffeic acid phenethyl ester (CAPE): cornerstone pharmacological studies and drug delivery systems

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