Fabrication and Optimization of Self‐Microemulsions to Improve the Oral Bioavailability of Total Flavones of <i>Hippophaë rhamnoides</i> L

Guo, Renhua; Guo, Xinbo; Hu, Xiaodan; Abbasi, Arshad Mehmood; Zhou, Lin; Li, Tong; Fu, Xiong; Liu, Rui Hai

doi:10.1111/1750-3841.13944

Cited by 17 publications

(11 citation statements)

References 43 publications

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“…Atovaquone was added into the thermally processed formulations at an amount that was several times in excess of atovaquone’s solubility in the SEC. Therefore, the formulations containing the SEC are not solid self-emulsifying drug delivery systems (SEDDS), where the drug is completely dissolved in the emulsifying component [ 56 , 57 , 58 , 59 ]. The formulations with SECs exhibiting different levels of atovaquone solubility allowed us to discriminate whether our formulations were SEDDS and an amorphous solid dispersion combined or something new from the overall combination of excipients and processing.…”

Section: Resultsmentioning

confidence: 99%

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

et al. 2018

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Glioblastoma multiforme (GBM) is the most common and lethal central nervous system tumor. Recently, atovaquone has shown inhibition of signal transducer and activator transcription 3, a promising target for GBM therapy. However, it is currently unable to achieve therapeutic drug concentrations in the brain with the currently reported and marketed formulations. The present study sought to explore the efficacy of atovaquone against GBM as well as develop a formulation of atovaquone that would improve oral bioavailability, resulting in higher amounts of drug delivered to the brain. Atovaquone was formulated as an amorphous solid dispersion using an optimized formulation containing a polymer and a spontaneously emulsifying component (SEC) with greatly improved wetting, disintegration, dispersibility, and dissolution properties. Atovaquone demonstrated cytotoxicity against GBM cell lines as well as provided a confirmed target for atovaquone brain concentrations in in vitro cell viability studies. This new formulation approach was then assessed in a proof-of-concept in vivo exposure study. Based on these results, the enhanced amorphous solid dispersion is promising for providing therapeutically effective brain levels of atovaquone for the treatment of GBM.

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Section: Resultsmentioning

confidence: 99%

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

et al. 2018

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“…Hydrous icaritin (HICT) is just such a flavonoid compound that can not only effectively inhibit the growth of breast cancer cells (Pan et al, 2007;Pan et al, 2010;Guo et al, 2011;Lai et al, 2013;Wang et al, 2017;Zhang et al, 2018) and cancer stem cells (Guo et al, 2011), but also relieve depression (Pan et al, 2007;Pan et al, 2010). However, like most flavonoids, HICT is water-insoluble, thus difficult to be effectively delivered in vivo, and meanwhile results into low bioavailability and limited effectiveness (Lewin et al, 2013;Guo et al, 2017). Encapsulation of hydrophobic drugs into nanoparticles, micelles or liposomes can well resolve the insolubility problem of this kind of drugs and achieve passive targeting through the enhanced permeability and retention (EPR) effect when intravenously administrated (Hashizume et al, 2000;Torchilin, 2011;Maeda et al, 2013;Prabhakar et al, 2013), and is thus suitable for hydrophobic antitumor agents.…”

Section: Introductionmentioning

confidence: 99%

Hydrous icaritin nanorods with excellent stability improves the in vitro and in vivo activity against breast cancer

Wang

Huang

et al. 2020

Drug Delivery

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Due to their various biological activities that are beneficial to human health and antitumor effect, flavonoid compounds have attracted much attention in recent years. Hydrous icaritin (HICT) was such a flavonoid that can inhibit the growth of breast cancer and cancer stem cells. In order to overcome the insolubility problem, HICT was fabricated into nanorods (NRs) through anti-solvent precipitation in this paper using D-a tocopherol acid polyethylene glycol succinate and sodium oleate as a co-stabilizer meanwhile using the mixture of ethanol and acetone (1:2, v/v) as the organic solvent. The obtained HICT NRs showed an average particle size 222.0 nm with a small polydispersity index value of 0.124 and a high zeta potential of-49.5 mV. HICT NRs could maintain similar particle size in various physiological medium and could be directly lyophilized without the addition of any cytoprotectants and then reconstituted into a colloidal system of similar size. The resultant HICT NRs had a high drug loading content of 55.6% and released HICT in a steady and constant pattern. MTT assay indicated NRs enhanced HICT's antitumor activity to ninefold against MCF-7 breast carcinoma cells. In vivo studies demonstrated oral administration free HICT had almost no tumor inhibitory effect while HICT NRs showed a tumor inhibition rate of 47.8%. When intravenously injected, HICT NRs displayed similar therapeutic efficacy to paclitaxel injections (70.4% vs. 74.5%, TIR). This may be partly due to the high accumulation of the injected HICT NRs in tumor ranking only second to that in the liver but much higher than in other organs. These results demonstrated that HICT NRs could be a promising antitumor agent for the treatment of breast cancer in clinic.

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“…There are many studies on the use of SMEDDS as carrier of poorly soluble drugs. Compared with the total flavones of Hippophaë rhamnoides L. (TFH), the TFH SMEDDS significantly enhances the solubility of the TFH up to 530 times in water, and its relative bioavailability is dramatically improved 3.09 times[17]. Wu X et al also reported that the SMEDDS improved the water solubility of curcumin, increasing the relative oral bioavailability of the SMEDDS by 12.13 times compared with pure curcumin[18].…”

Section: Introductionmentioning

confidence: 99%

Preparation and in vitro performance evaluation of resveratrol for oral self-microemulsion

Tang

Xiang

et al. 2019

PLoS ONE

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The purpose of this study was to improve the solubility of resveratrol (Res) by a self-microemulsifying drug-delivery system (SMEDDS). Through a solubility experiment, the pseudoternary phase diagram and ternary phase diagram were used to optimize the Res SMEDDS formula. The optimum formulation consisted of 5% IPM, 20% PEG400, and 65% Cremophor RH40. The water solubility, stability, in vitro release and antioxidant activity of the Res SMEDDS were characterized. The Res solubility in the SMEDDS was at least 1,000 times compared to that in water. The average droplet size of the microemulsion was 28.00±1.67 nm and uniform distribution. The Res SMEDDS should be stored at low temperature and in the dark to avoid light conditions. Res SMEDDS was able to improve the in vitro release rate of Res, and the in vitro release of Res from Res SMEDDS was significantly faster that of Res powder and unaffected by pH value of media. Antioxidant assays showed that antioxidant activities of Res in Res SMEDDS were unaffected compared to Res powder. Cytotoxicity study indicated that Res SMEDDS at the concentration of less than 100 μM was safe. These results demonstrated the potential use of Res SMEDDS for oral administration of Res.

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Fabrication and Optimization of Self‐Microemulsions to Improve the Oral Bioavailability of Total Flavones of Hippophaë rhamnoides L

Cited by 17 publications

References 43 publications

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier

Hydrous icaritin nanorods with excellent stability improves the in vitro and in vivo activity against breast cancer

Preparation and in vitro performance evaluation of resveratrol for oral self-microemulsion

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