Lipophilic effect of various pluronic-grafted gelatin copolymers on the quercetin delivery efficiency in these self-assembly nanogels

Thoai, Dinh Van; Nguyen, Duc‐Tho; Dang, Le Hang; Nguyen, Ngoc Hao; Nguyen, Van Toan; Doan, Phuong L.; Nguyen, Bich Tram; Thu, Le Van; Nguyen, Tung Ngoc; Quyen, Tran Ngoc

doi:10.1007/s10965-020-02216-z

Cited by 28 publications

(12 citation statements)

References 48 publications

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“…To the best of our knowledge, most of the literatures available on amphiphilic gelatin-pluronic mixture are based on chemically conjugating pluronic with gelatin and using these conjugates to prepare micellar or gel formulations. 29,30 On contrary, we have physically co-assembled pluronic blend with gelatin to prepare nanoparticles for drug delivery applications. 12 The results have revealed that HLB of pluronic affected mainly the size and hydrophobicity of gelatin nanoparticles.…”

Section: Discussionmentioning

confidence: 99%

“…The present manuscript addresses this issue by synthesizing gelatin‐pluronic nano‐composite of different HLB values ranging from 22 to 8 and using these nano‐systems to study the uptake of CUR (model hydrophobic bioactive compound) in A549 lung cancer cells. To the best of our knowledge, most of the literatures available on amphiphilic gelatin‐pluronic mixture are based on chemically conjugating pluronic with gelatin and using these conjugates to prepare micellar or gel formulations 29,30 . On contrary, we have physically co‐assembled pluronic blend with gelatin to prepare nanoparticles for drug delivery applications 12 .…”

Section: Discussionmentioning

confidence: 99%

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Balancing loading, cellular uptake, and toxicity of gelatin‐pluronic nanocomposite for drug delivery: Influence of HLB of pluronic

Das

Gandhi

Singh

et al. 2021

J Biomedical Materials Res

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In this study, pluronic stabilized gelatin nanocomposite of varying hydrophilic-lipophilic balance (HLB) were synthesized to study the effect of surface hydrophobicity on their cellular uptake and in turn the delivery of a model hydrophobic bioactive compound, curcumin (CUR). Notably, the variation in HLB from 22 to 8 did not cause much change in morphology (~spherical) and surface charge (~À6.5 mV) while marginally reducing the size of nanocomposite from 165 ± 097 nm to 134 ± 074 nm. On contrary, nanocomposites exhibited a very significant increase in their numbers, hydrophobicity as well as CUR loading with decreasing HLB values (22-8) of pluronic. Further, the cellular uptake of CUR through pluronic-gelatin nanocomposites was studied in human lung carcinoma (A549) cells. The results indicated that cellular uptake of CUR through nanocomposites followed the order HLB 22 > HLB 18 > HLB 15 > HLB 8. This was also reflected in terms of the decrease in cytotoxicity of CUR through nanocomposite of HLB 8 as compared to that of HLB 22. Interestingly, bare nanocomposite of HLB 8 showed significantly higher cytotoxicity as compared to that of HLB 22. Together these results suggested that although higher hydrophobicity of the gelatin-pluronic nanocomposite facilitated higher entrapment of CUR, the carrier per se became toxic due to its hydrophobic interaction with lipid bilayer of plasma membrane. Thus, HLB parameter is very important in designing hybrid nanocomposite systems involving protein and pluronic to ensure both bio-compatibility of the carrier and the optimum cellular delivery of the pay load.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Balancing loading, cellular uptake, and toxicity of gelatin‐pluronic nanocomposite for drug delivery: Influence of HLB of pluronic

Das

Gandhi

Singh

et al. 2021

J Biomedical Materials Res

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“…To overcome these problems, various strategies have been examined to improve the bioavailability of quercetin, including manufacturing the flavonoid analogs, its glycosides or modification with ester groups (Peñalva et al, 2019), and developed several modified dosage forms of Quercetin, mostly comprising micro emulsions, nanoparticles, and other carriers (Das et al, 2020; Gao et al, 2009; Jain et al, 2013; Q. Liu et al, 2019; Niazvand et al, 2019; Rahimi, Khoee, & Ghandi, 2019; Sapino et al, 2015; Tan et al, 2012; Trendafilova et al, 2017; Van Thoai et al, 2020). In addition, much research has been conducted on quercetin in the nanotechnology field to improve its bioavailability.…”

Section: Drug Delivery Of Quercetinmentioning

confidence: 99%

O‐Glycosidequercetin derivatives: Biological activities, mechanisms of action, and structure–activity relationship for drug design, a review

Alizadeh

Ebrahimzadeh

2021

Phytotherapy Research

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Quercetin as a valuable natural flavonoid has shown extensive biological activities, including anticancer, antioxidant, antibacterial, antiinflammatory, anti-Alzheimer, antifungal, antiviral, antithalassemia, iron chelation, antiobesity, antidiabetic, antihypertension, and antiphospholipase A2 (PLA2) activities, by the modulation of various targets and signaling pathways that have attracted much attention. However, the low solubility and poor bioavailability of quercetin have limited its applications; therefore, the researchers have tried to design and synthesize many new derivatives of quercetin through different strategies to modify quercetin restrictions and improve its biological activities. This review categorized the O-glycoside derivatives of Quercetin into two main classes, 3-O-glycoside and other O-glycoside derivatives. Also, it studied biological activities, structure-activity relationship (SAR), and the action mechanism of O-glycoside quercetin derivatives. Overall, we summarized past and present research for discovering new potent lead compounds. Highlights• Quercetin is a natural flavonoid with a valuable scaffold.• O-Glycoside quercetin derivatives represents broad-spectrum biological activities.• The structure-activity relationship investigation is discussed after modifying the scaffold of quercetin.• This review can help researchers to rationally design/develop various drugs.

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“…The percentage of CisOH and Cur successfully co-loaded into HP403 nanogel was determined by inductively coupled plasma mass spestrometer (ICP-MS, NexION 2000, Perkin Elmer, MA, USA), and UV-Vis (Agilent, Santa Clara, CA, USA). Drug loading (DL%) and entrapment efficiency (EE%) of micelle polymer or nanogel were referred to published formulas [ 31 , 33 , 50 ]

…”

Section: Methodsmentioning

confidence: 99%

“…The hydrophobic cores containing water-insoluble drugs are surrounded by the hydrophilic shell, thus increasing the solubility and permeability of loaded compounds [ 32 ]. Within this category, poloxamer P403 is a prospective material due to its high ratio of PPO (as compared to poloxamer P407, pluronic F127), low critical micelle concentration (CMC) value, and considerable internal space [ 33 ]. The poloxamer-based drug-carrier system can also achieve higher oral availability by inhibiting the drug efflux mediated by P-glycoprotein [ 34 ].…”

Section: Introductionmentioning

confidence: 99%

Curcuminoid Co-Loading Platinum Heparin-Poloxamer P403 Nanogel Increasing Effectiveness in Antitumor Activity

Nguyen

Bui

Nguyen

et al. 2022

Gels

Self Cite

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Nanosized multi-drug delivery systems provide synergistic effects between drugs and bioactive compounds, resulting in increased overall efficiency and restricted side effects compared to conventional single-drug chemotherapy. In this study, we develop an amphiphilic heparin-poloxamer P403 (HP403) nanogel that could effectively co-load curcuminoid (Cur) and cisplatin hydrate (CisOH) (HP403@CisOH@Cur) via two loading mechanisms. The HP403 nanogels and HP403@CisOH@Cur nanogels were closely analyzed with 1H-NMR spectroscopy, FT-IR spectroscopy, TEM, and DLS, exhibiting high stability in spherical forms. In drug release profiles, accelerated behavior of Cur and CisOH at pH 5.5 compared with neutral pH was observed, suggesting effective delivery of the compounds in tumor sites. In vitro studies showed high antitumor activity of HP403@CisOH@Cur nanogels, while in vivo assays showed that the dual-drug platform prolonged the survival time of mice and prevented tail necrosis. In summary, HP403@CisOH@Cur offers an intriguing strategy to achieve the cisplatin and curcumin synergistic effect in a well-designed delivery platform that increases antitumor effectiveness and overcomes undesired consequences caused by cisplatin in breast cancer treatment.

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Lipophilic effect of various pluronic-grafted gelatin copolymers on the quercetin delivery efficiency in these self-assembly nanogels

Cited by 28 publications

References 48 publications

Balancing loading, cellular uptake, and toxicity of gelatin‐pluronic nanocomposite for drug delivery: Influence of HLB of pluronic

Balancing loading, cellular uptake, and toxicity of gelatin‐pluronic nanocomposite for drug delivery: Influence of HLB of pluronic

O‐Glycosidequercetin derivatives: Biological activities, mechanisms of action, and structure–activity relationship for drug design, a review

Curcuminoid Co-Loading Platinum Heparin-Poloxamer P403 Nanogel Increasing Effectiveness in Antitumor Activity

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