Enhancement of Dissolution and Antioxidant Activity of Kaempferol Using a Nanoparticle Engineering Process

Tzeng, Cheng-Wei; Yen, Feng‐Lin; Wu, Tzu-Hui; Ko, Horng‐Huey; Lee, Chiang‐Wen; Tzeng, Wen-Sheng; Lin, Chun‐Ching

doi:10.1021/jf200354y

Cited by 63 publications

(46 citation statements)

References 44 publications

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“…64 The disappearance of the RSV melting peak in the DSC thermograms of RSV-loaded NPs ( Figure 6C) indicates the absence of the drug crystalline state, suggesting that entrapped RSV is in an amorphous state of a solid molecular dispersion into the polymer matrix. 65 Furthermore, in the thermogram of RSV-loaded PLGA NPs, the endothermic peak of PLGA appeared at about 375°C, as observed in the pure PLGA. The scans of PLGA-CS3 and PLGA-Alg3 NPs, chosen as examples, exhibited a considerable shifting of the endothermic decomposition peak of PLGA from about 375° to 317° and 327°C, respectively.…”

Section: Differential Scanning Calorimetrymentioning

confidence: 77%

Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Sanna¹,

Roggio²,

Siliani³

et al. 2012

IJN

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Background:Resveratrol, like other natural polyphenols, is an extremely photosensitive compound with low chemical stability, which limits the therapeutic application of its beneficial effects. The development of innovative formulation strategies, able to overcome physicochemical and pharmacokinetic limitations of this compound, may be achieved via suitable carriers able to associate controlled release and protection. In this context, nanotechnology is proving to be a powerful strategy. In this study, we developed novel cationic chitosan (CS)-and anionic alginate (Alg)-coated poly(d,l-lactide-co-glycolide) nanoparticles (NPs) loaded with the bioactive polyphenolic trans-(E)-resveratrol (RSV) for biomedical applications. Methods: NPs were prepared by the nanoprecipitation method and characterized in terms of morphology, size and zeta potential, encapsulation efficiency, Raman spectroscopy, swelling properties, differential scanning calorimetry, and in vitro release studies. The protective effect of the nanosystems under the light-stressed RSV and long-term stability were investigated. Results: NPs turned out to be spherical in shape, with size ranging from 135 to about 580 nm, depending on the composition and the amount of polyelectrolytes, while the encapsulation efficiencies increased from 8% of uncoated poly(d,l-lactide-co-glycolide) (PLGA) to 23% and 32% of Alg-and CS-coated PLGA NPs, respectively. All nanocarriers are characterized by a biphasic release pattern, and more effective controlled release rates are obtained for NPs formulated with higher polyelectrolyte concentrations. Stability studies revealed that encapsulation provides significant protection against light-exposure degradation, by reducing the trans-cis photoisomerization reaction. Moreover, the nanosystems are able to prevent the degradation of trans isoform and the leakage of RSV from the carrier for a period of 6 months. Conclusion: Our findings indicated that the newly developed CS-and Alg-coated PLGA NPs are suitable to be used for the delivery of bioactive RSV. The encapsulation of RSV into optimized polymeric NPs provides improved drug loading, effective controlled release, and protection against light-exposure degradation, thus opening new perspectives for the delivery of bioactive related phytochemicals to be used for (nano)chemoprevention/chemotherapy.

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Section: Differential Scanning Calorimetrymentioning

confidence: 77%

Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Sanna¹,

Roggio²,

Siliani³

et al. 2012

IJN

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“…225 Nanosized kaempferol enhances the antioxidant activity of kaempferol. 226 Nanokaempferol developed using a layer-bi-layer technique with a size range of 149-161 nm enhances the bioavailability of kaempferol in bone marrow. 227 Oral bioavailability of kaempferol is enhanced using self-nanoemulsifying drug delivery system and nanoniosome delivery techniques with a size range of 34-141 nm in dog and rat models.…”

Section: Nanokaempferolmentioning

confidence: 99%

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Ganesan¹,

Ko²,

Kim³

et al. 2015

IJN

102

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Oxidative stress plays a very critical role in neurodegenerative diseases, such as Parkinson’s disease (PD), which is the second most common neurodegenerative disease among elderly people worldwide. Increasing evidence has suggested that phytobioactive compounds show enhanced benefits in cell and animal models of PD. Curcumin, resveratrol, ginsenosides, quercetin, and catechin are phyto-derived bioactive compounds with important roles in the prevention and treatment of PD. However, in vivo studies suggest that their concentrations are very low to cross blood–brain barrier thereby it limits bioavailability, stability, and dissolution at target sites in the brain. To overcome these problems, nanophytomedicine with the controlled size of 1–100 nm is used to maximize efficiency in the treatment of PD. Nanosizing of phytobioactive compounds enhances the permeability into the brain with maximized efficiency and stability. Several nanodelivery techniques, including solid lipid nanoparticles, nanostructured lipid carriers, nanoliposomes, and nanoniosomes can be used for controlled delivery of nanobioactive compounds to brain. Nanocompounds, such as ginsenosides (19.9 nm) synthesized using a nanoemulsion technique, showed enhanced bioavailability in the rat brain. Here, we discuss the most recent trends and applications in PD, including 1) the role of phytobioactive compounds in reducing oxidative stress and their bioavailability; 2) the role of nanotechnology in reducing oxidative stress during PD; 3) nanodelivery systems; and 4) various nanophytobioactive compounds and their role in PD.

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“…Some studies have also demonstrated that EE-PVA effectively changed the crystalline structure of hydrophobic compounds such as quercetin, 28 kaempferol, 35 and silybinin. 36 In addition, we further investigated the intermolecular interactions of EE-PVA polymer with 734THIF using FTIR spectrometry and 1 H-NMR spectroscopy. FTIR spectra of raw 734THIF, 734N, and blank-N are shown in Figure 5A.…”

mentioning

confidence: 99%

Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration

Huang¹,

Hu²,

Lee³

et al. 2016

IJN

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7,3′,4′-Trihydroxyisoflavone (734THIF) is a secondary metabolite of daidzein and has been recently found to possess antioxidant, melanin inhibition, and skin cancer chemopreventive activities. However, the poor water solubility of 734THIF impedes its absorption and skin penetration and, therefore, limits its pharmacological effects when applied topically to the skin. We seek to use the nanoprecipitation method to prepare optimal eudragit E100 (EE)–polyvinyl alcohol (PVA)-loaded 734THIF nanoparticles (734N) to improve its physicochemical properties and thereby increase its water solubility, skin penetration, and biological activities. EE–PVA-loaded 734THIF nanoparticles (734N) were prepared, and their morphology and particle size were evaluated using a particle size analyzer and by electron microscopy. The drug loading and encapsulation efficiencies and in vitro solubility were determined using high-performance liquid chromatography. Hydrogen-bond formation was evaluated by 1 H-nuclear magnetic resonance and Fourier transform infrared spectroscopy, and crystalline-to-amorphous transformation was determined by differential scanning calorimetry and X-ray diffractometry. In vitro skin penetration was analyzed using fresh pig skin mounted on Franz diffusion cells, and cytotoxicity against human keratinocyte HaCaT cells was evaluated using the MTT assay. Antioxidant activity was determined by 2,2-diphenyl-1-picrylhydrazyl-free radical scavenging ability. EE–PVA-loaded 734THIF nanoparticles showed good drug loading and encapsulation efficiencies and were characterized by improved physicochemical properties, including reduction in particle size, amorphous transformation, and intermolecular hydrogen-bond formation. This is associated with increased water solubility and enhanced in vitro skin penetration, with no cytotoxicity toward HaCaT cells. In addition, 734THIF nanoparticles retained their antioxidant activity. In conclusion, 734THIF nanoparticles are characterized by improved physicochemical properties, increased water solubility, and enhanced skin penetration, and these may have potential use in the future as a topical delivery formulation for the treatment of skin diseases.

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Enhancement of Dissolution and Antioxidant Activity of Kaempferol Using a Nanoparticle Engineering Process

Cited by 63 publications

References 44 publications

Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration

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Enhancement of Dissolution and Antioxidant Activity of Kaempferol Using a Nanoparticle Engineering Process

Cited by 63 publications

References 44 publications

Development of novel cationic chitosan- and anionic alginate&ndash;coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Development of novel cationic chitosan- and anionic alginate&ndash;coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson&rsquo;s disease models

Design of acid-responsive polymeric nanoparticles for 7,3&#39;,4&#39;-trihydroxyisoflavone topical administration

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Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Development of novel cationic chitosan- and anionic alginate–coated poly(D,L-lactide-co-glycolide) nanoparticles for controlled release and light protection of resveratrol

Recent trends in the development of nanophytobioactive compounds and delivery systems for their possible role in reducing oxidative stress in Parkinson’s disease models

Design of acid-responsive polymeric nanoparticles for 7,3',4'-trihydroxyisoflavone topical administration