Preparation and Characterization of Microemulsions of Myricetin for Improving Its Antiproliferative and Antioxidative Activities and Oral Bioavailability

Guo, Rui Xue; Fu, Xiong; Chen, Jian; Zhou, Lin; Gu, Chen

doi:10.1021/acs.jafc.6b02184

Cited by 52 publications

(23 citation statements)

References 52 publications

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“…The entrapment efficiency was measured by the HPLC method described in the previous study (Guo et al., 2016). In short, an HS15-Myr micelle solution was filtered with a 0.22 μm filter; then 100 μl of the filtrate was dissolved and diluted by the appropriate amount of methanol.…”

Section: Methodsmentioning

confidence: 99%

Ultra-small micelles based on polyoxyl 15 hydroxystearate for ocular delivery of myricetin: optimization, in vitro, and in vivo evaluation

et al. 2019

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2019) Ultra-small micelles based on polyoxyl 15 hydroxystearate for ocular delivery of myricetin: optimization, invitro, and invivo evaluation, Drug Delivery, 26:1, 158-167, ABSTRACT The aim was to develop a nanocarrier based on polyoxyl 15 hydroxystearate (KolliphorV R HS15, HS15) micelles for the solubility, stability, and ocular delivery of myricetin (Myr). An optimized ratio of HS15 and Myr was prepared to fabricate HS15-Myr micelle ophthalmic solution. Myr-encapsulating HS15 micelles (HS15-Myr micelles) were subjected to physicochemical characterizations. The chemical stability of Myr in HS15 micelles and storage stability of HS15-Myr micelle ophthalmic solutions were evaluated. In vitro parallel artificial membrane permeability assay and antioxidant activity of Myr in HS15 micelles were also measured. In vivo ocular tolerance, corneal permeation, and anti-inflammatory efficacy studies were conducted following ocular topical administration. HS15-Myr micelles were successfully prepared and presented transparent appearance with high encapsulation (96.12 ± 0.31%), ultra-small micelle size (a mean diameter of 12.17 ± 0.73 nm), uniform size distribution (polydispersity index [PDI] ¼ 0.137 ± 0.013), and negative surface charge (À [4.28 ± 0.42] mV). Myr in HS15 micelle solution demonstrated higher aqueous stability than the free Myr solution among the accepted pH range for eyedrops. HS15-Myr micelle ophthalmic solution demonstrated high storage stability at 4 C and 25 C. HS15 micelles could significantly improve in vitro antioxidant activity and faster membrane permeation of Myr. No irritations or corneal damage were revealed in rabbit eyes after ocular administration of HS15-Myr micelle solution.In vivo corneal permeation study demonstrated that HS15-Myr micelles could penetrate the cornea efficiently in mouse eyes. Further, HS15-Myr micelles also demonstrated significant in vivo anti-inflammatory activity. It can be concluded that HS15 micelles are a potential ophthalmic delivery nanocarrier for poorly soluble drugs such as Myr. ARTICLE HISTORY

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Section: Methodsmentioning

confidence: 99%

Ultra-small micelles based on polyoxyl 15 hydroxystearate for ocular delivery of myricetin: optimization, in vitro, and in vivo evaluation

et al. 2019

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“…Having a longer alcohol molecule, Transcutol can increase the rate of transport from the dermis layer in comparison to alcohol. These attribute to select Transcutol for the preparation of SQR-loaded SNEDDs 48Figure 1Solubility of SQR in various oils, surfactants, and cosurfactants.…”

Section: Resultsmentioning

confidence: 99%

“…Blood collection was performed as per the protocol, and serum SQR concentrations were used to calculate the pharmacokinetic parameters. An earlier reported HPLC method was used to determine the plasma SQR concentrations 48. The mobile phase in the system used was methanol/0.05M potassium dihydrogen orthophosphate buffer (pH 5.0; 85/15 v/v).…”

Section: Methodsmentioning

confidence: 99%

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<p>Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation</p>

Hosny¹

2019

IJN

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BackgroundSaquinavir mesylate (SQR) tablets are widely used against human immunodeficiency virus. SQR has bioavailability issues owing to its poor aqueous solubility, extensive first-pass metabolism, and even low gastrointestinal tract permeability and absorption.ObjectiveAn in-depth optimization process was carried out using factorial design to improve the permeation parameters and thereby the bioavailability of SQR by formulating self-nanoemulsifying drug delivery system (SNEDDS)-loaded polymeric transdermal films.MethodsThe solubility of SQR in different nanoemulsion components was examined. Various combinations of selected components were prepared in an extreme vertices mixture design to identify the useful nanoemulsion zone and to develop SNEDDS with minimum globule size. The optimized SQR-SNEDDS was loaded in polyvinyl alcohol (PVA)-based transdermal films. The Box-Behnken design was used to optimize and evaluate SQR permeability. The prepared films were characterized for thickness, tensile strength, elongation, folding endurance, and accelerated stability studies. The optimized film was examined for ex vivo skin permeation and in vivo pharmacokinetic parameters.ResultsThe optimized SQR-SNEDDS was prepared in proportions of 0.1, 0.55, and 0.35 of clove oil, labrasol, and Transcutol, respectively. The implemented Box-Behnken design indicated the optimized film consisted of 1.0% PVA, 0.25% propylene glycol, and clove oil as the oil phase. The tensile strength, thickness, percent elongation, and folding endurance of the optimized SQR-SNEDDS film were 0.93 ± 0.013 kg/cm2, 0.22 ± 0.006 mm, 43.1 ± 0.022%, and >200 times, respectively. A higher Cmax and double the AUC were observed for SQR-SNEDDS–loaded film in comparison to pure SQR-loaded films.ConclusionImplementation of a two-step design to optimize and control experimental factors in the preparation of SQR-SNEDDS and its loading onto PVA-based transdermal films was achieved. The films indicated improved ex vivo skin permeation, enhanced bioavailability, and overcame the limitations of the oral dosage form.

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“…Myricetin is stable at pH 2 and its degradation depends on pH and temperature [91]. A recent study showed that microemulsion formulation can improve the solubility of myricetin 1225 times greater than water and also enhance its anti-proliferative activity against human liver cancer cells (HepG2) [92]. Myricetin is a promising anti-carcinogen and chemo preventive agent with therapeutic potential reported in ovarian [93], colon [94], skin [95], liver [96] and breast [97] cancers.…”

Section: Myricetinmentioning

confidence: 99%

Bioactive Compounds: Natural Defense Against Cancer?

2019

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Cancer is a devastating disease that has claimed many lives. Natural bioactive agents from plants are gaining wide attention for their anticancer activities. Several studies have found that natural plant-based bioactive compounds can enhance the efficacy of chemotherapy, and in some cases ameliorate some of the side-effects of drugs used as chemotherapeutic agents. In this paper, we have reviewed the literature on the anticancer effects of four plant-based bioactive compounds namely, curcumin, myricetin, geraniin and tocotrienols (T3) to provide an overview on some of the key findings that are related to this effect. The molecular mechanisms through which the active compounds may exert their anticancer properties in cell and animal-based studies also discussed.

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Preparation and Characterization of Microemulsions of Myricetin for Improving Its Antiproliferative and Antioxidative Activities and Oral Bioavailability

Cited by 52 publications

References 52 publications

Ultra-small micelles based on polyoxyl 15 hydroxystearate for ocular delivery of myricetin: optimization, in vitro, and in vivo evaluation

Ultra-small micelles based on polyoxyl 15 hydroxystearate for ocular delivery of myricetin: optimization, in vitro, and in vivo evaluation

<p>Development Of Saquinavir Mesylate Nanoemulsion-Loaded Transdermal Films: Two-Step Optimization Of Permeation Parameters, Characterization, And Ex Vivo And In Vivo Evaluation</p>

Bioactive Compounds: Natural Defense Against Cancer?

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