Melatonin-loaded silica coated with hydroxypropyl methylcellulose phthalate for enhanced oral bioavailability: Preparation, and in vitro-in vivo evaluation

Li, Yuanyuan; Zhao, Xiuhua; Zu, Yuangang; Wang, Lingling; Wei, Weiwei; Deng, Yiping; Zu, Chang; Liu, Yanjie

doi:10.1016/j.ejpb.2016.11.003

Cited by 30 publications

(21 citation statements)

References 29 publications

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“…However, it is possible to improve the antioxidant activity of melatonin by delivering it using a specific nanoparticle drug delivery system, resulting in controlled release and a decreased decomposition rate, which ultimately prolongs its time of effect. Thus, many kinds of materials such as silica and poly(D,L‐lactide‐co‐glycolide) (PLGA) , have been used as drug carriers. PLGA‐mPEG drug carrier has good biocompatibility, biodegradability, and excellent encapsulation properties for lipophilic drugs .…”

Section: Discussionmentioning

confidence: 99%

Poly(Lactide-Co-Glycolide)-Monomethoxy-Poly-(Polyethylene Glycol) Nanoparticles Loaded with Melatonin Protect Adipose-Derived Stem Cells Transplanted in Infarcted Heart Tissue

Yang

Huang

et al. 2018

Stem Cells

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Stem cell transplantation is a promising therapeutic strategy for myocardial infarction. However, transplanted cells face low survival rates due to oxidative stress and the inflammatory microenvironment in ischemic heart tissue. Melatonin has been used as a powerful endogenous antioxidant to protect cells from oxidative injury. However, melatonin cannot play a long-lasting effect against the hostile microenvironment. Nano drug delivery carriers have the ability to protect the loaded drug from degradation in physiological environments in a controlled manner, which results in longer effects and decreased side effects. Therefore, we constructed poly(lactide-co-glycolide)-monomethoxy-poly-(polyethylene glycol) (PLGA-mPEG) nanoparticles to encapsulate melatonin. We tested whether the protective effect of melatonin encapsulated by PLGA-mPEG nanoparticles (melatonin nanoparticles [Mel-NPs]) on adipose-derived mesenchymal stem cells (ADSCs) was enhanced compared to that of free melatonin both in vitro and in vivo. In the in vitro study, we found that Mel-NPs reduced formation of the p53- cyclophilin D complex, prevented mitochondrial permeability transition pores from opening, and rescued ADSCs from hypoxia/reoxygenation injury. Moreover, Mel-NPs can achieve higher ADSC survival rates than free melatonin in rat myocardial infarction areas, and the therapeutic effects of ADSCs pretreated with Mel-NPs were more apparent. Hence, the combination of Mel-NPs and stem cell transplantation may be a promising strategy for myocardial infarction therapy. Stem Cells 2018;36:540-550.

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Section: Discussionmentioning

confidence: 99%

Poly(Lactide-Co-Glycolide)-Monomethoxy-Poly-(Polyethylene Glycol) Nanoparticles Loaded with Melatonin Protect Adipose-Derived Stem Cells Transplanted in Infarcted Heart Tissue

Yang

Huang

et al. 2018

Stem Cells

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“…Therefore, considering the natural decline of MLT and its potential therapeutic effects, the exogenous administration of this molecule might be useful. However, MLT oral bioavailability is lower than 20% due to its poor absorption and/or extensive first-pass metabolism [12] , [13] , [14] , [15] . Nanotechnology-based drug delivery systems offer an alternative to circumventing these drawbacks.…”

Section: Introductionmentioning

confidence: 99%

Application of a validated HPLC-PDA method for the determination of melatonin content and its release from poly(lactic acid) nanoparticles

Martins

Khalil

Mainardes

2017

Journal of Pharmaceutical Analysis

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Melatonin is a natural hormone and with the advancement of age its production declines and thereby may result in some neurological disorders. Exogenous administration of melatonin has been suggested as a neuroprotective agent. Due to its low oral bioavailability, the loading of melatonin in polymeric nanoparticles could be an important tool to effectively use exogenous melatonin. The quantification of the incorporated drug within polymeric nanoparticles is an important step in nanoparticles characterization. An analytical method using high performance liquid chromatography equipped with photodiode array detector (HPLC-PDA) was developed and validated for melatonin determination in poly (lactic acid) nanoparticles obtained by a single emulsion-solvent evaporation technique. The melatonin in vitro release profile also was determined by the HPLC method. Mobile phase consisted of acetonitrile: water (65:35, v/v) pumped at a flow rate of 0.9 mL/min, in the isocratic mode and PDA detector was set at 220 nm. The method was validated in terms of the selectivity, linearity, precision, accuracy, robustness, limits of detection and quantification. Analytical curve was linear over the concentration range of 10–100 μg/mL, and limits of detection and quantification were 25.9 ng/mL and 78.7 ng/mL, respectively. The mean recovery for melatonin was 100.47% (RSD = 1.25%, n = 9). In the intra- and inter-assay, the coefficient of variation was less than 2%. Robustness was proved performing changes in mobile phase, column temperature and flow rate. The method was suitable for the determination of melatonin encapsulation efficiency in poly(lactic acid) nanoparticles and for the evaluation of melatonin in vitro release profile.

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“…Various techniques have been used to assess the drawbacks of raw/oral MEL; for example, recently, a group in Italy studied the bioavailability of MEL in gel capsules and found that compared to powdered MEL, the capsule improved serum bioavailability of MEL in humans [36]. Other techniques include melt crystallization technique to enhance solubility of MEL [37] and nanotechnology, where MEL is encapsulated into a nano-matrix called a nanosphere for sustained release of MEL [38,39].…”

Section: Sources Of Melmentioning

confidence: 99%

“…Over 30 oral MEL supplements were analyzed by liquid chromatography for detection of MEL and serotonin content and found that 26% of the oral supplements contained serotonin [53], suggesting that MEL supplements are not free of contaminants and may affect other physiological factors. To address this, a group in China proposed a method using nanotechnology whereby silicon dioxide as a nanosphere coated with hydroxypropyl methylcellulose phthalate was used as MEL carrier in rats, ensuring that it was only MEL being absorbed upon administration [39]. The nanosphere increased maximum peak concentration of MEL in the plasma and increased the AUC compared to commercial oral MEL in rats [39].…”

Section: Sources Of Melmentioning

confidence: 99%

“…To address this, a group in China proposed a method using nanotechnology whereby silicon dioxide as a nanosphere coated with hydroxypropyl methylcellulose phthalate was used as MEL carrier in rats, ensuring that it was only MEL being absorbed upon administration [39]. The nanosphere increased maximum peak concentration of MEL in the plasma and increased the AUC compared to commercial oral MEL in rats [39]. Future studies are required to determine the effects of nanosphere MEL in animal studies followed by the pharmacokinetic parameters in humans to establish whether it can be beneficial in releasing MEL into the bloodstream with improved bioavailability.…”

Section: Sources Of Melmentioning

confidence: 99%

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Melatonin May Increase Anticancer Potential of Pleiotropic Drugs

Bojková

Kubatka

Qaradakhi

et al. 2018

IJMS

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Melatonin (N-acetyl-5-methoxytryptamine) is not only a pineal hormone, but also an ubiquitary molecule present in plants and part of our diet. Numerous preclinical and some clinical reports pointed to its multiple beneficial effects including oncostatic properties, and as such, it has become one of the most aspiring goals in cancer prevention/therapy. A link between cancer and inflammation and/or metabolic disorders has been well established and the therapy of these conditions with so-called pleiotropic drugs, which include non-steroidal anti-inflammatory drugs, statins and peroral antidiabetics, modulates a cancer risk too. Adjuvant therapy with melatonin may improve the oncostatic potential of these drugs. Results from preclinical studies are limited though support this hypothesis, which, however, remains to be verified by further research.

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Melatonin-loaded silica coated with hydroxypropyl methylcellulose phthalate for enhanced oral bioavailability: Preparation, and in vitro-in vivo evaluation

Cited by 30 publications

References 29 publications

Poly(Lactide-Co-Glycolide)-Monomethoxy-Poly-(Polyethylene Glycol) Nanoparticles Loaded with Melatonin Protect Adipose-Derived Stem Cells Transplanted in Infarcted Heart Tissue

Poly(Lactide-Co-Glycolide)-Monomethoxy-Poly-(Polyethylene Glycol) Nanoparticles Loaded with Melatonin Protect Adipose-Derived Stem Cells Transplanted in Infarcted Heart Tissue

Application of a validated HPLC-PDA method for the determination of melatonin content and its release from poly(lactic acid) nanoparticles

Melatonin May Increase Anticancer Potential of Pleiotropic Drugs

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