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Role of Nanoconstructs in Ameliorating Chemopreventive and Chemotherapeutic Potential of Plant Bioactives
Published in Bhupinder Singh, Om Prakash Katare, Eliana B. Souto, NanoAgroceuticals & NanoPhytoChemicals, 2018
Rajneet Kaur Khurana, Teenu Sharma, Satvinder Kaur, Ashay Jain, Bhupinder Singh
Zhang et al. (2011) investigated the oral and pulmonary delivery of nanocrystals to augment the bioavailability of baicalein, a bioactive flavonoid, isolated from the root of Scutellaria baicalensis Georgi. Baicalein nanocrystals were prepared by antisolvent recrystallization, followed subsequently by high-pressure homogenization. No change in crystalline structure was deciphered after fabrication. Baicalein nanocrystals containing small quantities of stabilizer significantly enhanced its dissolution rate. The mean relative bioavailability of baicalein nanocrystal administered perorally was found to be 1.67-fold that of oral baicalein. Pulmonary delivery of baicalein nanocrystal exhibited rapid and extensive absorption with pharmacokinetic parameters analogous to intravenous baicalein injection.
Dual-responsive antibiotic and baicalein co-delivery nanoparticles with enhanced synergistic antibacterial activity
Published in Journal of Biomaterials Science, Polymer Edition, 2023
Yujia Liu, Jun Qian, Xiufen Zhao, Tianyu Lan, Yongjun Luo, Qianqian Guo, Xiangchun Shen
Pseudomonas aeruginosa (P. aeruginosa) is an important conditional pathogen. Once P. aeruginosa-caused infection occurs, it is not easy to treat due to the high frequency of drug resistance and the formation of biofilms [3]. Bacterial biofilms represent major virulence factors, which is the root cause of refractory infection. The generation of biofilms is a highly effective strategy for environmental fortification and protection, Therefore, to inhibit or disrupt the bacterial biofilms may be an available strategy to treat the refractory infection. Some flavonoid compounds exhibit antimicrobial and anti-biofilm activity [4–7]. e.g. baicalein (Bai) is a flavonoid monomer extracted from Scutellaria baicalensis roots, shows broad-spectrum antibacterial effects, and enhance sensitivity in drug-resistance bacteria [8–11]. Bai also inhibits biofilm formation by interfering with the quorum sensing (QS) system [9]. However, Bai has poor water solubility, is easily oxidized, and has limited use in clinical settings. Most pathogens produce an extracellular polymeric substances (EPS) matrix which hampers antibiotic into biofilms. Bai and antibiotic combinations have been used to exert synergistic effects on antibacterial and antibiofilm activity [8]. Therefore, methods for effectively delivering Bai and such antibiotics should be developed to overcome drug-resistance bacterial recalcitrance to antimicrobial treatments.
Solubility and thermodynamic properties of baicalein in water and ethanol mixtures from 283.15 to 328.15 K
Published in Chemical Engineering Communications, 2021
Fei Mo, Jia Ma, Peipei Zhang, Dawei Zhang, Huihui Fan, Xin Yang, Liqiang Zhi, Jiye Zhang
Scutellaria baicalensis Georgi is a traditional Chinese medicine (Bochorakova et al. 2003), which contains a significant amount of flavonoids with various pharmacological effects. Among them, baicalein (5,6,7-trihydroxyflavone, C15H10O5, Figure 1A), and baicalin (5,6-dihydroxy-4-oxygen-2-phenyl-4H-1-benzopyran-7-β-d-glucopyranoseacid, C21H18O11, Figure 1B) are two major bioactive flavonoids. Baicalein has been reported with anti-inflammatory (Liu et al. 2015), anti-pathogen (Jang et al. 2014), anti-allergenic (Lu et al. 2007), antioxidant (Cho et al. 2011) and neuroprotective activity (Cheng et al. 2008). More importantly, its antitumor effect has drawn increasing attention in recent years (Kim et al. 2014; Liu et al., 2015; Wang et al. 2010). It was proved to be cytotoxic to various solid tumor cells and it suppressed the tumor growth without systemic toxicity in lots of studies (Gong et al. 2017; Li-Weber 2009). Baicalin has the similar biological activities with baicalein due to their similar structures, however, its absorption in gastrointestinal tract, permeability across the skin and pharmacological effects are much poorer than baicalein (Lai et al. 2003; Li et al. 2013; Miao et al. 2016; Xing et al. 2005a, 2005b). Therefore, compared with baicalin, baicalein is a much more promising therapeutic candidate.