Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability

Fung, Wai Yee; Liong, Min‐Tze; Yuen, Kah Hay

doi:10.1111/jphp.12502

Cited by 13 publications

(5 citation statements)

References 17 publications

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“…Generally, topical antioxidant nanoparticle formulations can effectively reduce the particle size and change the form from crystalline to amorphous for ingredients showing poor water solubility [ 24 ] such as quercetin [ 25 ], resveratrol [ 26 ], lutein [ 27 ], and coenzyme Q10 [ 28 ], increasing their dissolution, skin penetration, and bioavailability. Our preliminary test of this study used PVPK30 or HPBCD as an excipient independently to prepare the ACM nanoparticle.…”

Section: Discussionmentioning

confidence: 99%

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

et al. 2021

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Antioxidants from plant extracts are often used as additives in skincare products to prevent skin problems induced by environmental pollutants. Artocarpus communis methanol extract (ACM) has many biological effects, such as antioxidant, anti-inflammatory, wound healing, and photoprotective effects; however, the poor water solubility of raw ACM has limited its applications in medicine and cosmetics. Topical antioxidant nanoparticles are one of the drug-delivery systems for overcoming the poor water solubility of antioxidants for increasing their skin penetration. The present study demonstrated that ACM-loaded hydroxypropyl-β-cyclodextrin and polyvinylpyrrolidone K30 nanoparticles (AHP) were successfully prepared and could effectively increase the skin penetration of ACM through changing the physicochemical characteristics of raw ACM, including reducing the particle size, increasing the surface area, and inducing amorphous transformation. Our results also revealed that AHP had significantly better antioxidant activity than raw ACM for preventing photocytotoxicity because the AHP formulation increased the cellular uptake of the ACM in UVB-irradiated HaCaT keratinocytes. In conclusion, our results suggest that AHP may be used as a good topical antioxidant nanoparticle for delivering ACM into deep layers of the skin for preventing UVB-induced skin problems.

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Section: Discussionmentioning

confidence: 99%

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

et al. 2021

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“…As such, our research group remains committed to further investigating an oro-buccal delivered nanoparticle formulation for the enhanced delivery of CoQ 10 to intracellular and mitochondrial targets. In vitro and in vivo studies have recently demonstrated that electro-spraying microparticles may comprise a possible future technology for improving the bioavailability of compounds such as CoQ 10 [26].…”

Section: Discussionmentioning

confidence: 99%

The Plasma Bioavailability of Coenzyme Q10 Absorbed from the Gut and the Oral Mucosa

Vitetta

Leong

Zhou

et al. 2018

JFB

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Coenzyme Q10 (CoQ10) has a central role in the generation of cellular bioenergy and its regulation. The hydrophobicity exhibited by the CoQ10 molecule leads to reports of poor absorption profiles, therefore, the optimization of formulations and modes of delivery is an ever-evolving therapeutic goal. The aim of this study was to investigate different CoQ10 formulations. The article summarizes the findings from an Australian comparative study involving adults administered CoQ10 through different oral delivery platforms. A total of 11 participants (six males and five females) voluntarily participated in a comparative clinical study of three different CoQ10 formulations across a six-week period, completing 198 person-hours of cumulative contribution equivalent to n = 33 participation. All of the eligible participants (n = 11) administered the three formulations blinded from who the commercial supplier of the formulation was and from what the chemical form of the CoQ10 was that was being administered. The dosing between the CoQ10 preparations were dispensed sequentially and were administered following three-week washouts. Three commercial preparations were tested, which included the following: formulations with capsules each containing ubiquinol and ubiquinone (150 mg/capsule), and a liposome ubiquinone formulation (40 mg/mL at 2 actuations of the pump). A significant inter-subject variation in the plasma level of CoQ10 at baseline that was observed to increase with an increase in age. This trend persisted in the post administration of the different formulations. Furthermore, it was observed that the intestinal absorption and bioavailability of CoQ10 varied significantly in the plasma between subjects, irrespective of whether the ubiquinol or ubiquinone forms were administered. The administration of CoQ10 as a liposome for preparation showed the poorest response in bioavailability. Although the ubiquinol capsule form of CoQ10 was observed to have increased in the plasma versus the ubiquinone capsules and the ubiquinol liposome at the two-hour interval, the inter-subject variation was such that the difference was not significant (p > 0.05). All of the CoQ10 formulations showed no further increases in their plasma levels over the remaining study period (i.e., four hours). This study further concluded that the intestinal absorption of CoQ10 is highly variable and is independent of the molecular form administered. Furthermore, it also concludes that liposomes are not an effective vehicle for the oral administration of CoQ10, and as such, did not improve the oral mucosal/sublingual absorption and bioavailability of the molecule. Of interest was the observation that with the increasing subject age, there was an observed increase in the baseline plasma CoQ10 levels in the participants prior to dosing. It was posited that the increase in the baseline plasma levels of CoQ10 with an increase in age could be due to the loss of skeletal muscle mass, a result that still needs to be verified.

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“…A few studies explored the possibility of using electrospraying to encapsulate enzymes. Fung et al (2016) electrosprayed coenzyme Q10 in copovidone (Kollidon® VA64) using acetone as the solvent. Both in vitro and in vivo evaluation showed enhanced bioavailability of the electrosprayed microparticles.…”

Section: Bioactive Cargos Electrosprayed Inside Carriersmentioning

confidence: 99%

Electrospraying: Possibilities and Challenges of Engineering Carriers for Biomedical Applications—A Mini Review

2019

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Electrospraying, a liquid atomization-based technique, has been used to produce and formulate micro/nanoparticular cargo carriers for various biomedical applications, including drug delivery, biomedical imaging, implant coatings, and tissue engineering. In this mini review, we begin with the main features of electrospraying methods to engineer carriers with various bioactive cargos, including genes, growth factors, and enzymes. In particular, this review focuses on the improvement of traditional electrospraying technology for the fabrication of carriers for living cells and providing a suitable condition for gene transformation. Subsequently, the major applications of the electrosprayed carriers in the biomedical field are highlighted. Finally, we finish with conclusions and future perspectives of electrospraying for high efficiency and safe production.

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Preparation, in-vitro and in-vivo characterisation of CoQ10 microparticles: electrospraying-enhanced bioavailability

Abstract: Based on the findings in this study, electrospraying is a highly prospective technology to produce functional nano- and micro-structures as delivery vehicles for drugs with poor oral bioavailability due to rate-limiting solubility.

Cited by 13 publications

References 17 publications

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

Topical Artocarpus communis Nanoparticles Improved the Water Solubility and Skin Permeation of Raw A. communis Extract, Improving Its Photoprotective Effect

The Plasma Bioavailability of Coenzyme Q10 Absorbed from the Gut and the Oral Mucosa

Electrospraying: Possibilities and Challenges of Engineering Carriers for Biomedical Applications—A Mini Review

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