Preparation of pH-sensitive carboxymethyl chitosan nanoparticles loaded with ginsenoside Rb1 and evaluation of drug release in vitro

Oral absorption of ginsenoside Rb1 (Rb1) is often hindered by the gastrointestinal tract. Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted car...

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Veröffentlicht in:International journal of biological macromolecules 2024-05, Vol.267 (Pt 2), p.131487-131487, Article 131487
Hauptverfasser: An, Ziyuan, Dong, Yujia, Wang, Wanying, Wang, Jiani, Wu, Zhansheng, Wang, Wenfei, He, Yanhui, Bao, Guoqiang
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container_issue Pt 2
container_start_page 131487
container_title International journal of biological macromolecules
container_volume 267
creator An, Ziyuan
Dong, Yujia
Wang, Wanying
Wang, Jiani
Wu, Zhansheng
Wang, Wenfei
He, Yanhui
Bao, Guoqiang
description Oral absorption of ginsenoside Rb1 (Rb1) is often hindered by the gastrointestinal tract. Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted carboxymethyl chitosan as the carrier, which improved the stability and embedding rate of Rb1. In addition, the CMDA@Rb1-NPs was encapsulated with sodium alginate by ion crosslinking method with additional layer (CMDAlg@Rb1-NPs). Scanning electron microscopy showed that the nanoparticles were spherical, evenly distributed, smooth and without obvious adhesion. By evaluating drug loading, entrapment efficiency, the encapsulation efficiency of Rb1 increased from 60.07 % to 72.14 % after grafting deoxycholic acid improvement and optimization. In vitro release results showed that the cumulative release of Rb1 by CMDAlg-NPs showed a pH dependent effect, which was
doi_str_mv 10.1016/j.ijbiomac.2024.131487
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Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted carboxymethyl chitosan as the carrier, which improved the stability and embedding rate of Rb1. In addition, the CMDA@Rb1-NPs was encapsulated with sodium alginate by ion crosslinking method with additional layer (CMDAlg@Rb1-NPs). Scanning electron microscopy showed that the nanoparticles were spherical, evenly distributed, smooth and without obvious adhesion. By evaluating drug loading, entrapment efficiency, the encapsulation efficiency of Rb1 increased from 60.07 % to 72.14 % after grafting deoxycholic acid improvement and optimization. In vitro release results showed that the cumulative release of Rb1 by CMDAlg-NPs showed a pH dependent effect, which was &lt;10 % in simulated gastric juice with pH 1.2, completely released with pH 7.4 for about 48 h. In addition, Rb1 and CMDAlg@Rb1-NPs had inhibitory effects on A549 cells, and the inhibitory effect of CMDAlg@Rb1-NPs was better. Therefore, all results indicated that CMDA/Alg@Rb1 nanoparticles might be a novel drug delivery system to improve the stability and embedding rate of Rb1, and has the potential to be applied in oral pharmaceutical preparations.</description><identifier>ISSN: 0141-8130</identifier><identifier>EISSN: 1879-0003</identifier><identifier>DOI: 10.1016/j.ijbiomac.2024.131487</identifier><identifier>PMID: 38599430</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>absorption ; adhesion ; Carboxymethyl chitosan ; Cell Line, Tumor ; chitosan ; Chitosan - analogs &amp; derivatives ; Chitosan - chemistry ; crosslinking ; deoxycholic acid ; digestive tract ; Drug Carriers - chemistry ; drug delivery systems ; Drug Liberation ; drugs ; electron microscopy ; encapsulation ; gastric juice ; ginsenosides ; Ginsenosides - chemistry ; Ginsenosides - pharmacokinetics ; Ginsenosides - pharmacology ; Humans ; Hydrogen-Ion Concentration ; nanoparticles ; Nanoparticles - chemistry ; Particle Size ; pH sensitivity ; Release mechanism ; sodium alginate ; surfactants</subject><ispartof>International journal of biological macromolecules, 2024-05, Vol.267 (Pt 2), p.131487-131487, Article 131487</ispartof><rights>2024 Elsevier B.V.</rights><rights>Copyright © 2024 Elsevier B.V. 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Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted carboxymethyl chitosan as the carrier, which improved the stability and embedding rate of Rb1. In addition, the CMDA@Rb1-NPs was encapsulated with sodium alginate by ion crosslinking method with additional layer (CMDAlg@Rb1-NPs). Scanning electron microscopy showed that the nanoparticles were spherical, evenly distributed, smooth and without obvious adhesion. By evaluating drug loading, entrapment efficiency, the encapsulation efficiency of Rb1 increased from 60.07 % to 72.14 % after grafting deoxycholic acid improvement and optimization. In vitro release results showed that the cumulative release of Rb1 by CMDAlg-NPs showed a pH dependent effect, which was &lt;10 % in simulated gastric juice with pH 1.2, completely released with pH 7.4 for about 48 h. In addition, Rb1 and CMDAlg@Rb1-NPs had inhibitory effects on A549 cells, and the inhibitory effect of CMDAlg@Rb1-NPs was better. Therefore, all results indicated that CMDA/Alg@Rb1 nanoparticles might be a novel drug delivery system to improve the stability and embedding rate of Rb1, and has the potential to be applied in oral pharmaceutical preparations.</description><subject>absorption</subject><subject>adhesion</subject><subject>Carboxymethyl chitosan</subject><subject>Cell Line, Tumor</subject><subject>chitosan</subject><subject>Chitosan - analogs &amp; derivatives</subject><subject>Chitosan - chemistry</subject><subject>crosslinking</subject><subject>deoxycholic acid</subject><subject>digestive tract</subject><subject>Drug Carriers - chemistry</subject><subject>drug delivery systems</subject><subject>Drug Liberation</subject><subject>drugs</subject><subject>electron microscopy</subject><subject>encapsulation</subject><subject>gastric juice</subject><subject>ginsenosides</subject><subject>Ginsenosides - chemistry</subject><subject>Ginsenosides - pharmacokinetics</subject><subject>Ginsenosides - pharmacology</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>nanoparticles</subject><subject>Nanoparticles - chemistry</subject><subject>Particle Size</subject><subject>pH sensitivity</subject><subject>Release mechanism</subject><subject>sodium alginate</subject><subject>surfactants</subject><issn>0141-8130</issn><issn>1879-0003</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1vFDEMhiMEokvhL1Q5cpklnsxHcgNVQCtVAiE4RxnH081qNlmSzJa988M71ba99mTJel5b9sPYBYg1COg-bdd-O_i4s7iuRd2sQUKj-ldsBarXlRBCvmYrAQ1UCqQ4Y-9y3i7drgX1lp1J1WrdSLFi_38m2ttki4-Bx5Hvr6pMIfviD8TRpiH-O-6obI4Tx40vMdvAgw1xyRSPE2U-RevI8TtfNvzWhyUds3fEfw3AbXCcDnaan-e7NN_yRBPZTNwHfvAlxffszWinTB8e6zn78-3r78ur6ubH9-vLLzcVykaVymLbKdRy6FsclQZdo1Odg7HW0Fmp29FhCyMCDoiCdN_ScmdNdS80yG6U5-zjae4-xb8z5WJ2PiNNkw0U52wktLKXou7ly6hYSK16aBa0O6GYYs6JRrNPfmfT0YAwD7LM1jzJMg-yzEnWErx43DEPO3LPsSc7C_D5BNDylIOnZDJ6CkjOJ8JiXPQv7bgHa4-rQA</recordid><startdate>20240501</startdate><enddate>20240501</enddate><creator>An, Ziyuan</creator><creator>Dong, Yujia</creator><creator>Wang, Wanying</creator><creator>Wang, Jiani</creator><creator>Wu, Zhansheng</creator><creator>Wang, Wenfei</creator><creator>He, Yanhui</creator><creator>Bao, Guoqiang</creator><general>Elsevier B.V</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>7X8</scope><scope>7S9</scope><scope>L.6</scope></search><sort><creationdate>20240501</creationdate><title>Preparation of pH-sensitive carboxymethyl chitosan nanoparticles loaded with ginsenoside Rb1 and evaluation of drug release in vitro</title><author>An, Ziyuan ; Dong, Yujia ; Wang, Wanying ; Wang, Jiani ; Wu, Zhansheng ; Wang, Wenfei ; He, Yanhui ; Bao, Guoqiang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c348t-ac568c93b75cf89192cd86d1f2916a395fdc51fc1cbcc0e975e8592e2709136f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>absorption</topic><topic>adhesion</topic><topic>Carboxymethyl chitosan</topic><topic>Cell Line, Tumor</topic><topic>chitosan</topic><topic>Chitosan - analogs &amp; derivatives</topic><topic>Chitosan - chemistry</topic><topic>crosslinking</topic><topic>deoxycholic acid</topic><topic>digestive tract</topic><topic>Drug Carriers - chemistry</topic><topic>drug delivery systems</topic><topic>Drug Liberation</topic><topic>drugs</topic><topic>electron microscopy</topic><topic>encapsulation</topic><topic>gastric juice</topic><topic>ginsenosides</topic><topic>Ginsenosides - chemistry</topic><topic>Ginsenosides - pharmacokinetics</topic><topic>Ginsenosides - pharmacology</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>nanoparticles</topic><topic>Nanoparticles - chemistry</topic><topic>Particle Size</topic><topic>pH sensitivity</topic><topic>Release mechanism</topic><topic>sodium alginate</topic><topic>surfactants</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>An, Ziyuan</creatorcontrib><creatorcontrib>Dong, Yujia</creatorcontrib><creatorcontrib>Wang, Wanying</creatorcontrib><creatorcontrib>Wang, Jiani</creatorcontrib><creatorcontrib>Wu, Zhansheng</creatorcontrib><creatorcontrib>Wang, Wenfei</creatorcontrib><creatorcontrib>He, Yanhui</creatorcontrib><creatorcontrib>Bao, Guoqiang</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>AGRICOLA</collection><collection>AGRICOLA - Academic</collection><jtitle>International journal of biological macromolecules</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>An, Ziyuan</au><au>Dong, Yujia</au><au>Wang, Wanying</au><au>Wang, Jiani</au><au>Wu, Zhansheng</au><au>Wang, Wenfei</au><au>He, Yanhui</au><au>Bao, Guoqiang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation of pH-sensitive carboxymethyl chitosan nanoparticles loaded with ginsenoside Rb1 and evaluation of drug release in vitro</atitle><jtitle>International journal of biological macromolecules</jtitle><addtitle>Int J Biol Macromol</addtitle><date>2024-05-01</date><risdate>2024</risdate><volume>267</volume><issue>Pt 2</issue><spage>131487</spage><epage>131487</epage><pages>131487-131487</pages><artnum>131487</artnum><issn>0141-8130</issn><eissn>1879-0003</eissn><abstract>Oral absorption of ginsenoside Rb1 (Rb1) is often hindered by the gastrointestinal tract. Carboxymethyl chitosan deoxycholic acid loaded with ginsenoside Rb1 nanoparticles (CMDA@Rb1-NPs), were prepared as a delivery system using a self-assembly technique with amphipathic deoxycholic acid grafted carboxymethyl chitosan as the carrier, which improved the stability and embedding rate of Rb1. In addition, the CMDA@Rb1-NPs was encapsulated with sodium alginate by ion crosslinking method with additional layer (CMDAlg@Rb1-NPs). Scanning electron microscopy showed that the nanoparticles were spherical, evenly distributed, smooth and without obvious adhesion. By evaluating drug loading, entrapment efficiency, the encapsulation efficiency of Rb1 increased from 60.07 % to 72.14 % after grafting deoxycholic acid improvement and optimization. In vitro release results showed that the cumulative release of Rb1 by CMDAlg-NPs showed a pH dependent effect, which was &lt;10 % in simulated gastric juice with pH 1.2, completely released with pH 7.4 for about 48 h. In addition, Rb1 and CMDAlg@Rb1-NPs had inhibitory effects on A549 cells, and the inhibitory effect of CMDAlg@Rb1-NPs was better. Therefore, all results indicated that CMDA/Alg@Rb1 nanoparticles might be a novel drug delivery system to improve the stability and embedding rate of Rb1, and has the potential to be applied in oral pharmaceutical preparations.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>38599430</pmid><doi>10.1016/j.ijbiomac.2024.131487</doi><tpages>1</tpages></addata></record>
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subjects absorption
adhesion
Carboxymethyl chitosan
Cell Line, Tumor
chitosan
Chitosan - analogs & derivatives
Chitosan - chemistry
crosslinking
deoxycholic acid
digestive tract
Drug Carriers - chemistry
drug delivery systems
Drug Liberation
drugs
electron microscopy
encapsulation
gastric juice
ginsenosides
Ginsenosides - chemistry
Ginsenosides - pharmacokinetics
Ginsenosides - pharmacology
Humans
Hydrogen-Ion Concentration
nanoparticles
Nanoparticles - chemistry
Particle Size
pH sensitivity
Release mechanism
sodium alginate
surfactants
title Preparation of pH-sensitive carboxymethyl chitosan nanoparticles loaded with ginsenoside Rb1 and evaluation of drug release in vitro
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