Development of Epirubicin-Loaded Biocompatible Polymer PLA-PEG-PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment
Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI...
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| Veröffentlicht in: | Polymers 2021-04, Vol.13 (8), p.1212 |
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| creator | Massadeh, Salam Almohammed, Iman Barhoush, Eman Omer, Mustafa Aldhawi, Nouf Almalik, Abdulaziz Alaamery, Manal |
| description | Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI in its free form.
In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA-PEG-PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry.
The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells' viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days.
EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects. |
| doi_str_mv | 10.3390/polym13081212 |
| format | Article |
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In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA-PEG-PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry.
The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells' viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days.
EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects.</description><identifier>ISSN: 2073-4360</identifier><identifier>EISSN: 2073-4360</identifier><identifier>DOI: 10.3390/polym13081212</identifier><identifier>PMID: 33918625</identifier><language>eng</language><publisher>Switzerland: MDPI AG</publisher><subject>Apoptosis ; Biocompatibility ; Breast cancer ; Cancer ; Cancer therapies ; Chemical synthesis ; Doxorubicin ; Drug delivery systems ; Drug dosages ; Encapsulation ; Entrapment ; Estrogens ; Ethylene glycol ; Flow cytometry ; Free form ; Molecular weight ; Nanoparticles ; Particle size ; Penicillin ; Photon correlation spectroscopy ; Polymers ; Quantum dots ; Room temperature ; Side effects ; Stability analysis ; Statistical analysis ; Toxicity ; Transmission electron microscopy</subject><ispartof>Polymers, 2021-04, Vol.13 (8), p.1212</ispartof><rights>2021 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2021 by the authors. 2021</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-b677d8d923b16b4a418c778cea074baf99538ebbc9d549a868a07633b900fa193</citedby><cites>FETCH-LOGICAL-c415t-b677d8d923b16b4a418c778cea074baf99538ebbc9d549a868a07633b900fa193</cites><orcidid>0000-0001-9193-0008 ; 0000-0001-8072-9149 ; 0000-0003-1705-7137</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070301/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC8070301/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,881,27901,27902,53766,53768</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33918625$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Massadeh, Salam</creatorcontrib><creatorcontrib>Almohammed, Iman</creatorcontrib><creatorcontrib>Barhoush, Eman</creatorcontrib><creatorcontrib>Omer, Mustafa</creatorcontrib><creatorcontrib>Aldhawi, Nouf</creatorcontrib><creatorcontrib>Almalik, Abdulaziz</creatorcontrib><creatorcontrib>Alaamery, Manal</creatorcontrib><title>Development of Epirubicin-Loaded Biocompatible Polymer PLA-PEG-PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment</title><title>Polymers</title><addtitle>Polymers (Basel)</addtitle><description>Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI in its free form.
In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA-PEG-PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry.
The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells' viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days.
EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects.</description><subject>Apoptosis</subject><subject>Biocompatibility</subject><subject>Breast cancer</subject><subject>Cancer</subject><subject>Cancer therapies</subject><subject>Chemical synthesis</subject><subject>Doxorubicin</subject><subject>Drug delivery systems</subject><subject>Drug dosages</subject><subject>Encapsulation</subject><subject>Entrapment</subject><subject>Estrogens</subject><subject>Ethylene glycol</subject><subject>Flow cytometry</subject><subject>Free form</subject><subject>Molecular weight</subject><subject>Nanoparticles</subject><subject>Particle size</subject><subject>Penicillin</subject><subject>Photon correlation spectroscopy</subject><subject>Polymers</subject><subject>Quantum dots</subject><subject>Room temperature</subject><subject>Side effects</subject><subject>Stability analysis</subject><subject>Statistical analysis</subject><subject>Toxicity</subject><subject>Transmission electron microscopy</subject><issn>2073-4360</issn><issn>2073-4360</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>BENPR</sourceid><recordid>eNpVUc9rFDEUDqLYUnv0KgGvOzaZZCaJB2Fdt7WwtAtVryHJZNyUmWSaZArrP-O_apbW0r7Le_C-X_AB8B6jT4QIdDaFYT9igjiucf0KHNeIkYqSFr1-dh-B05RuURnatC1mb8FRIWPe1s0x-PvN3tshTKP1GYYericXZ-2M89UmqM528KsLJoyTyk4PFm4PjjbC7WZZbdcXVdnwSvkwqZidGWz6DG_2Pu9scmkBVzsVlck2uj-FH_wC3mSl3eDyfgGV7-Clh79cjgEufaErb2wMc4LLlGxKh0zvwJteDcmePu4T8PN8_WP1vdpcX1yulpvKUNzkSreMdbwTNdG41VRRzA1j3FiFGNWqF6Ih3GptRNdQoXjLy6MlRAuEeoUFOQFfHnSnWY-2M8U6qkFO0Y0q7mVQTr78eLeTv8O95IghgnAR-PgoEMPdbFOWt2GOvmSWddOgmgpGaEFVDygTQ0rR9k8OGMlDpfJFpQX_4XmsJ_T_Ask_iwWgOw</recordid><startdate>20210409</startdate><enddate>20210409</enddate><creator>Massadeh, Salam</creator><creator>Almohammed, Iman</creator><creator>Barhoush, Eman</creator><creator>Omer, Mustafa</creator><creator>Aldhawi, Nouf</creator><creator>Almalik, Abdulaziz</creator><creator>Alaamery, Manal</creator><general>MDPI AG</general><general>MDPI</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7SR</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>HCIFZ</scope><scope>JG9</scope><scope>KB.</scope><scope>PDBOC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0001-9193-0008</orcidid><orcidid>https://orcid.org/0000-0001-8072-9149</orcidid><orcidid>https://orcid.org/0000-0003-1705-7137</orcidid></search><sort><creationdate>20210409</creationdate><title>Development of Epirubicin-Loaded Biocompatible Polymer PLA-PEG-PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment</title><author>Massadeh, Salam ; Almohammed, Iman ; Barhoush, Eman ; Omer, Mustafa ; Aldhawi, Nouf ; Almalik, Abdulaziz ; Alaamery, Manal</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-b677d8d923b16b4a418c778cea074baf99538ebbc9d549a868a07633b900fa193</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>Apoptosis</topic><topic>Biocompatibility</topic><topic>Breast cancer</topic><topic>Cancer</topic><topic>Cancer therapies</topic><topic>Chemical synthesis</topic><topic>Doxorubicin</topic><topic>Drug delivery systems</topic><topic>Drug dosages</topic><topic>Encapsulation</topic><topic>Entrapment</topic><topic>Estrogens</topic><topic>Ethylene glycol</topic><topic>Flow cytometry</topic><topic>Free form</topic><topic>Molecular weight</topic><topic>Nanoparticles</topic><topic>Particle size</topic><topic>Penicillin</topic><topic>Photon correlation spectroscopy</topic><topic>Polymers</topic><topic>Quantum dots</topic><topic>Room temperature</topic><topic>Side effects</topic><topic>Stability analysis</topic><topic>Statistical analysis</topic><topic>Toxicity</topic><topic>Transmission electron microscopy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Massadeh, Salam</creatorcontrib><creatorcontrib>Almohammed, Iman</creatorcontrib><creatorcontrib>Barhoush, Eman</creatorcontrib><creatorcontrib>Omer, Mustafa</creatorcontrib><creatorcontrib>Aldhawi, Nouf</creatorcontrib><creatorcontrib>Almalik, Abdulaziz</creatorcontrib><creatorcontrib>Alaamery, Manal</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Engineered Materials Abstracts</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>Materials Science & Engineering Collection</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Materials Science Collection</collection><collection>ProQuest Central Korea</collection><collection>SciTech Premium Collection</collection><collection>Materials Research Database</collection><collection>Materials Science Database</collection><collection>Materials Science Collection</collection><collection>Publicly Available Content Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>Polymers</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Massadeh, Salam</au><au>Almohammed, Iman</au><au>Barhoush, Eman</au><au>Omer, Mustafa</au><au>Aldhawi, Nouf</au><au>Almalik, Abdulaziz</au><au>Alaamery, Manal</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of Epirubicin-Loaded Biocompatible Polymer PLA-PEG-PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment</atitle><jtitle>Polymers</jtitle><addtitle>Polymers (Basel)</addtitle><date>2021-04-09</date><risdate>2021</risdate><volume>13</volume><issue>8</issue><spage>1212</spage><pages>1212-</pages><issn>2073-4360</issn><eissn>2073-4360</eissn><abstract>Epirubicin (EPI) is an anti-cancerous chemotherapeutic drug that is an effective epimer of doxorubicin with less cardiotoxicity. Although EPI has fewer side effects than its analog, doxorubicin, this study aims to develop EPI nanoparticles as an improved formula of the conventional treatment of EPI in its free form.
In this study, EPI-loaded polymeric nanoparticles (EPI-NPs) were prepared by the double emulsion method using a biocompatible poly (lactide) poly (ethylene glycol) poly(lactide) (PLA-PEG-PLA) polymer. The physicochemical properties of the EPI-NPs were determined by dynamic light scattering (DLS), transmission electron microscopy (TEM), differential scanning calorimetry (DSC), entrapment efficiency and stability studies. The effect of EPI-NPs on cancer cells was determined by high throughput imaging and flow cytometry.
The synthesis process resulted in monodisperse EPI-NPs with a size of 166.93 ± 1.40 nm and an elevated encapsulation efficiency (EE) of 88.3%. In addition, TEM images revealed the spherical uniformness of EPI-NPs with no aggregation, while the cellular studies presented the effect of EPI-NPs on MCF-7 cells' viability; after 96 h of treatment, the MCF-7 cells presented considerable apoptotic activity. The stability study showed that the EPI-NPs remained stable at room temperature at physiological pH for over 30 days.
EPI-NPs were successfully encapsulated within a highly stable biocompatible polymer with minimal loss of the drug. The used polymer has low cytotoxicity and EPI-NPs induced apoptosis in estrogen-positive cell line, making them a promising, safe treatment for cancer with less adverse side effects.</abstract><cop>Switzerland</cop><pub>MDPI AG</pub><pmid>33918625</pmid><doi>10.3390/polym13081212</doi><orcidid>https://orcid.org/0000-0001-9193-0008</orcidid><orcidid>https://orcid.org/0000-0001-8072-9149</orcidid><orcidid>https://orcid.org/0000-0003-1705-7137</orcidid><oa>free_for_read</oa></addata></record> |
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| subjects | Apoptosis Biocompatibility Breast cancer Cancer Cancer therapies Chemical synthesis Doxorubicin Drug delivery systems Drug dosages Encapsulation Entrapment Estrogens Ethylene glycol Flow cytometry Free form Molecular weight Nanoparticles Particle size Penicillin Photon correlation spectroscopy Polymers Quantum dots Room temperature Side effects Stability analysis Statistical analysis Toxicity Transmission electron microscopy |
| title | Development of Epirubicin-Loaded Biocompatible Polymer PLA-PEG-PLA Nanoparticles: Synthesis, Characterization, Stability, and In Vitro Anticancerous Assessment |
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