Enhanced efficacy of baicalin-loaded TPGS polymeric micelles against periodontitis
As a chronic infectious disease, periodontitis is the main cause of teeth exfoliation due to its severe inflammatory reaction and periodontal tissue destruction. Recent reports have shown that baicalin could inhibit the NF-κB signaling pathway in inflammatory activity of periodontitis, but the effic...
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| Veröffentlicht in: | Materials Science & Engineering C 2019-08, Vol.101, p.387-395 |
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| creator | Liu, Xiaochen Chen, Yunong Chen, Xin Su, Jiansheng Huang, Chen |
| description | As a chronic infectious disease, periodontitis is the main cause of teeth exfoliation due to its severe inflammatory reaction and periodontal tissue destruction. Recent reports have shown that baicalin could inhibit the NF-κB signaling pathway in inflammatory activity of periodontitis, but the efficacy of baicalin is limited due to its poor water solubility. In this work, we report the fabrication and application of baicalin encapsulated D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) polymeric micelles (PMs) through thin-film hydration method. The monodispersed micelles showed a spherical shape in aqueous solution and a prolonged drug-release kinetic. After baicalin was loaded into PMs, cytotoxicity and apoptosis induction were both decreased. The expression of genes (including TNF-α, IL-1β, RANKL and NF-κB) and the phosphorylation level of NF-κB p65 protein in lipopolysaccharide (LPS)-induced rat gingival fibroblasts were also reduced. Further investigation of drug efficacy in a rat periodontal disease model confirmed that the use of baicalin-PMs could reduce the destruction of alveolar bone and gingival fiber. Moreover, the therapeutic effect of baicalin-PMs was significantly better than that of free baicalin. These results suggest that the direct injection of micelles containing water-insoluble drugs may become a simple but effective method for treating periodontitis.
[Display omitted]
•Sub-30 nm baicalin-loaded polymeric micelles were successfully synthesized by thin-film hydration method.•Compared with free drugs, baicalin-loaded micelles showed less cytotoxicity to cell proliferation.•Baicalin-loaded micelles significantly suppressed the development of periodontitis through NF- κB signaling pathway.•Rat periodontitis model proved the treatment efficacy of baicalin-loaded micelles. |
| doi_str_mv | 10.1016/j.msec.2019.03.103 |
| format | Article |
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[Display omitted]
•Sub-30 nm baicalin-loaded polymeric micelles were successfully synthesized by thin-film hydration method.•Compared with free drugs, baicalin-loaded micelles showed less cytotoxicity to cell proliferation.•Baicalin-loaded micelles significantly suppressed the development of periodontitis through NF- κB signaling pathway.•Rat periodontitis model proved the treatment efficacy of baicalin-loaded micelles.</description><identifier>ISSN: 0928-4931</identifier><identifier>EISSN: 1873-0191</identifier><identifier>DOI: 10.1016/j.msec.2019.03.103</identifier><identifier>PMID: 31029332</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Alveolar bone ; Animals ; Apoptosis ; Apoptosis - drug effects ; Aqueous solutions ; Baicalin ; Cytotoxicity ; Destruction ; Disease Models, Animal ; Drug delivery ; Effectiveness ; Fabrication ; Fibroblasts ; Fibroblasts - drug effects ; Fibroblasts - metabolism ; Fibroblasts - pathology ; Flavonoids - pharmacokinetics ; Flavonoids - pharmacology ; Flavonoids - therapeutic use ; Gene expression ; Gingiva - pathology ; Gum disease ; IL-1β ; Infectious diseases ; Inflammation ; Interleukin-1beta - metabolism ; Lipopolysaccharides ; Male ; Materials science ; Micelles ; NF-kappa B - metabolism ; NF-κB protein ; Periodontal disease ; Periodontal diseases ; Periodontitis ; Periodontitis - drug therapy ; Phosphorylation ; Polyethylene glycol ; Polymeric micelles ; Rats ; Signal transduction ; Synaptotagmin ; Teeth ; Thin films ; Tocopherol ; Toxicity ; TRANCE protein ; Tumor Necrosis Factor-alpha - metabolism ; Tumor necrosis factor-α ; Vitamin E ; Vitamin E - chemistry ; X-Ray Diffraction ; X-Ray Microtomography</subject><ispartof>Materials Science & Engineering C, 2019-08, Vol.101, p.387-395</ispartof><rights>2019 Elsevier B.V.</rights><rights>Copyright © 2019 Elsevier B.V. All rights reserved.</rights><rights>Copyright Elsevier BV Aug 2019</rights><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c450t-321c186cb1126a670e2664d09b2aab1431b4c3ef930833d4f992f0c44bb44c303</citedby><cites>FETCH-LOGICAL-c450t-321c186cb1126a670e2664d09b2aab1431b4c3ef930833d4f992f0c44bb44c303</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S092849311733730X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3536,27903,27904,65309</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/31029332$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Liu, Xiaochen</creatorcontrib><creatorcontrib>Chen, Yunong</creatorcontrib><creatorcontrib>Chen, Xin</creatorcontrib><creatorcontrib>Su, Jiansheng</creatorcontrib><creatorcontrib>Huang, Chen</creatorcontrib><title>Enhanced efficacy of baicalin-loaded TPGS polymeric micelles against periodontitis</title><title>Materials Science & Engineering C</title><addtitle>Mater Sci Eng C Mater Biol Appl</addtitle><description>As a chronic infectious disease, periodontitis is the main cause of teeth exfoliation due to its severe inflammatory reaction and periodontal tissue destruction. Recent reports have shown that baicalin could inhibit the NF-κB signaling pathway in inflammatory activity of periodontitis, but the efficacy of baicalin is limited due to its poor water solubility. In this work, we report the fabrication and application of baicalin encapsulated D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) polymeric micelles (PMs) through thin-film hydration method. The monodispersed micelles showed a spherical shape in aqueous solution and a prolonged drug-release kinetic. After baicalin was loaded into PMs, cytotoxicity and apoptosis induction were both decreased. The expression of genes (including TNF-α, IL-1β, RANKL and NF-κB) and the phosphorylation level of NF-κB p65 protein in lipopolysaccharide (LPS)-induced rat gingival fibroblasts were also reduced. Further investigation of drug efficacy in a rat periodontal disease model confirmed that the use of baicalin-PMs could reduce the destruction of alveolar bone and gingival fiber. Moreover, the therapeutic effect of baicalin-PMs was significantly better than that of free baicalin. These results suggest that the direct injection of micelles containing water-insoluble drugs may become a simple but effective method for treating periodontitis.
[Display omitted]
•Sub-30 nm baicalin-loaded polymeric micelles were successfully synthesized by thin-film hydration method.•Compared with free drugs, baicalin-loaded micelles showed less cytotoxicity to cell proliferation.•Baicalin-loaded micelles significantly suppressed the development of periodontitis through NF- κB signaling pathway.•Rat periodontitis model proved the treatment efficacy of baicalin-loaded micelles.</description><subject>Alveolar bone</subject><subject>Animals</subject><subject>Apoptosis</subject><subject>Apoptosis - drug effects</subject><subject>Aqueous solutions</subject><subject>Baicalin</subject><subject>Cytotoxicity</subject><subject>Destruction</subject><subject>Disease Models, Animal</subject><subject>Drug delivery</subject><subject>Effectiveness</subject><subject>Fabrication</subject><subject>Fibroblasts</subject><subject>Fibroblasts - drug effects</subject><subject>Fibroblasts - metabolism</subject><subject>Fibroblasts - pathology</subject><subject>Flavonoids - pharmacokinetics</subject><subject>Flavonoids - pharmacology</subject><subject>Flavonoids - therapeutic use</subject><subject>Gene expression</subject><subject>Gingiva - pathology</subject><subject>Gum disease</subject><subject>IL-1β</subject><subject>Infectious diseases</subject><subject>Inflammation</subject><subject>Interleukin-1beta - metabolism</subject><subject>Lipopolysaccharides</subject><subject>Male</subject><subject>Materials science</subject><subject>Micelles</subject><subject>NF-kappa B - metabolism</subject><subject>NF-κB protein</subject><subject>Periodontal disease</subject><subject>Periodontal diseases</subject><subject>Periodontitis</subject><subject>Periodontitis - drug therapy</subject><subject>Phosphorylation</subject><subject>Polyethylene glycol</subject><subject>Polymeric micelles</subject><subject>Rats</subject><subject>Signal transduction</subject><subject>Synaptotagmin</subject><subject>Teeth</subject><subject>Thin films</subject><subject>Tocopherol</subject><subject>Toxicity</subject><subject>TRANCE protein</subject><subject>Tumor Necrosis Factor-alpha - metabolism</subject><subject>Tumor necrosis factor-α</subject><subject>Vitamin E</subject><subject>Vitamin E - chemistry</subject><subject>X-Ray Diffraction</subject><subject>X-Ray Microtomography</subject><issn>0928-4931</issn><issn>1873-0191</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LJDEQhoO4rKO7f8CDNHjx0mMqlUl3gxcZ_ALBZdc9h3S6WjN0d8akR5h_b5pRDx48Jbz11EvxMHYMfA4c1Plq3keyc8GhmnNMGe6xGZQF5imBfTbjlShzWSEcsMMYV5yrEgvxkx0gcFEhihn7ezU8m8FSk1HbOmvsNvNtVpv07dyQd940afb45-ZftvbdtqfgbNY7S11HMTNPxg1xzNYp9o0fRje6-Iv9aE0X6ff7e8T-X189Lm_z-4ebu-XlfW7lgo85CrBQKlsDCGVUwUkoJRte1cKYGiRCLS1SWyEvERvZVpVouZWyrmUacDxiZ7vedfAvG4qj7l2cDjMD-U3UQoAqioWQkNDTL-jKb8KQrkuUlEqW5UImSuwoG3yMgVq9Dq43YauB68m4XunJuJ6Ma44pw7R08l69qXtqPlc-FCfgYgdQcvHqKOhoHU3KXSA76sa77_rfAHoZkF0</recordid><startdate>201908</startdate><enddate>201908</enddate><creator>Liu, Xiaochen</creator><creator>Chen, Yunong</creator><creator>Chen, Xin</creator><creator>Su, Jiansheng</creator><creator>Huang, Chen</creator><general>Elsevier B.V</general><general>Elsevier BV</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QF</scope><scope>7QO</scope><scope>7QQ</scope><scope>7SC</scope><scope>7SE</scope><scope>7SP</scope><scope>7SR</scope><scope>7T7</scope><scope>7TA</scope><scope>7TB</scope><scope>7U5</scope><scope>8BQ</scope><scope>8FD</scope><scope>C1K</scope><scope>F28</scope><scope>FR3</scope><scope>H8D</scope><scope>H8G</scope><scope>JG9</scope><scope>JQ2</scope><scope>KR7</scope><scope>L7M</scope><scope>L~C</scope><scope>L~D</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>201908</creationdate><title>Enhanced efficacy of baicalin-loaded TPGS polymeric micelles against periodontitis</title><author>Liu, Xiaochen ; 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Recent reports have shown that baicalin could inhibit the NF-κB signaling pathway in inflammatory activity of periodontitis, but the efficacy of baicalin is limited due to its poor water solubility. In this work, we report the fabrication and application of baicalin encapsulated D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) polymeric micelles (PMs) through thin-film hydration method. The monodispersed micelles showed a spherical shape in aqueous solution and a prolonged drug-release kinetic. After baicalin was loaded into PMs, cytotoxicity and apoptosis induction were both decreased. The expression of genes (including TNF-α, IL-1β, RANKL and NF-κB) and the phosphorylation level of NF-κB p65 protein in lipopolysaccharide (LPS)-induced rat gingival fibroblasts were also reduced. Further investigation of drug efficacy in a rat periodontal disease model confirmed that the use of baicalin-PMs could reduce the destruction of alveolar bone and gingival fiber. Moreover, the therapeutic effect of baicalin-PMs was significantly better than that of free baicalin. These results suggest that the direct injection of micelles containing water-insoluble drugs may become a simple but effective method for treating periodontitis.
[Display omitted]
•Sub-30 nm baicalin-loaded polymeric micelles were successfully synthesized by thin-film hydration method.•Compared with free drugs, baicalin-loaded micelles showed less cytotoxicity to cell proliferation.•Baicalin-loaded micelles significantly suppressed the development of periodontitis through NF- κB signaling pathway.•Rat periodontitis model proved the treatment efficacy of baicalin-loaded micelles.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>31029332</pmid><doi>10.1016/j.msec.2019.03.103</doi><tpages>9</tpages></addata></record> |
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| subjects | Alveolar bone Animals Apoptosis Apoptosis - drug effects Aqueous solutions Baicalin Cytotoxicity Destruction Disease Models, Animal Drug delivery Effectiveness Fabrication Fibroblasts Fibroblasts - drug effects Fibroblasts - metabolism Fibroblasts - pathology Flavonoids - pharmacokinetics Flavonoids - pharmacology Flavonoids - therapeutic use Gene expression Gingiva - pathology Gum disease IL-1β Infectious diseases Inflammation Interleukin-1beta - metabolism Lipopolysaccharides Male Materials science Micelles NF-kappa B - metabolism NF-κB protein Periodontal disease Periodontal diseases Periodontitis Periodontitis - drug therapy Phosphorylation Polyethylene glycol Polymeric micelles Rats Signal transduction Synaptotagmin Teeth Thin films Tocopherol Toxicity TRANCE protein Tumor Necrosis Factor-alpha - metabolism Tumor necrosis factor-α Vitamin E Vitamin E - chemistry X-Ray Diffraction X-Ray Microtomography |
| title | Enhanced efficacy of baicalin-loaded TPGS polymeric micelles against periodontitis |
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