Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method
β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (P...
Gespeichert in:
Veröffentlicht in: | Drug development and industrial pharmacy 2018-05, Vol.44 (5), p.750-756 |
---|---|
Hauptverfasser: | , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
container_end_page | 756 |
---|---|
container_issue | 5 |
container_start_page | 750 |
container_title | Drug development and industrial pharmacy |
container_volume | 44 |
creator | dos Santos, Klecia M. Barbosa, Raquel de Melo Vargas, Fernanda Grace A. de Azevedo, Eduardo Pereira Lins, Antônio Cláudio da Silva Camara, Celso A. Aragão, Cícero F. S. Moura, Tulio Flavio de Lima e Raffin, Fernanda Nervo |
description | β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap. |
doi_str_mv | 10.1080/03639045.2017.1411942 |
format | Article |
fullrecord | <record><control><sourceid>pubmed_infor</sourceid><recordid>TN_cdi_pubmed_primary_29206496</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>29206496</sourcerecordid><originalsourceid>FETCH-LOGICAL-c366t-9a3009a481c1da2771925c9267bca560a448bcb18a9e96508ae8196094a283303</originalsourceid><addsrcrecordid>eNp9kNFKwzAUQIMobk4_QckPdN4kTdq8KXNOYeAe1DcJt23KKm1TkjrZb_khfpMrcz76dOFyzr1wCLlkMGWQwjUIJTTEcsqBJVMWM6ZjfkTGTHKIZKL4MRkPTDRAI3IWwjsA41rKUzLimoOKtRqTtzu7sbXrGtv21JU0uLoqaFGFzvpQuTYMy--vqMYO87VrLa1aupovKLYFXb2uaLYdnM2g2w12zmO_02hj-7UrzslJiXWwF79zQl7u58-zh2j5tHic3S6jXCjVRxoFgMY4ZTkrkCcJ01zmmqsky1EqwDhOszxjKWqrlYQUbcq0Ah0jT4UAMSFyfzf3LgRvS9P5qkG_NQzMkMsccpkhl_nNtfOu9l73kTW2-LMOfXbAzR6o2tL5Bj-drwvT47Z2vvTY5lUw4v8fP7vTeVo</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method</title><source>Business Source Complete</source><creator>dos Santos, Klecia M. ; Barbosa, Raquel de Melo ; Vargas, Fernanda Grace A. ; de Azevedo, Eduardo Pereira ; Lins, Antônio Cláudio da Silva ; Camara, Celso A. ; Aragão, Cícero F. S. ; Moura, Tulio Flavio de Lima e ; Raffin, Fernanda Nervo</creator><creatorcontrib>dos Santos, Klecia M. ; Barbosa, Raquel de Melo ; Vargas, Fernanda Grace A. ; de Azevedo, Eduardo Pereira ; Lins, Antônio Cláudio da Silva ; Camara, Celso A. ; Aragão, Cícero F. S. ; Moura, Tulio Flavio de Lima e ; Raffin, Fernanda Nervo</creatorcontrib><description>β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.1080/03639045.2017.1411942</identifier><identifier>PMID: 29206496</identifier><language>eng</language><publisher>England: Taylor & Francis</publisher><subject>dissolution rate ; PEG 6000 ; PVP K30 ; solid dispersion ; β-Lapachone</subject><ispartof>Drug development and industrial pharmacy, 2018-05, Vol.44 (5), p.750-756</ispartof><rights>2017 Informa UK Limited, trading as Taylor & Francis Group 2017</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c366t-9a3009a481c1da2771925c9267bca560a448bcb18a9e96508ae8196094a283303</citedby><cites>FETCH-LOGICAL-c366t-9a3009a481c1da2771925c9267bca560a448bcb18a9e96508ae8196094a283303</cites><orcidid>0000-0002-3434-2602</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/29206496$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>dos Santos, Klecia M.</creatorcontrib><creatorcontrib>Barbosa, Raquel de Melo</creatorcontrib><creatorcontrib>Vargas, Fernanda Grace A.</creatorcontrib><creatorcontrib>de Azevedo, Eduardo Pereira</creatorcontrib><creatorcontrib>Lins, Antônio Cláudio da Silva</creatorcontrib><creatorcontrib>Camara, Celso A.</creatorcontrib><creatorcontrib>Aragão, Cícero F. S.</creatorcontrib><creatorcontrib>Moura, Tulio Flavio de Lima e</creatorcontrib><creatorcontrib>Raffin, Fernanda Nervo</creatorcontrib><title>Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap.</description><subject>dissolution rate</subject><subject>PEG 6000</subject><subject>PVP K30</subject><subject>solid dispersion</subject><subject>β-Lapachone</subject><issn>0363-9045</issn><issn>1520-5762</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2018</creationdate><recordtype>article</recordtype><recordid>eNp9kNFKwzAUQIMobk4_QckPdN4kTdq8KXNOYeAe1DcJt23KKm1TkjrZb_khfpMrcz76dOFyzr1wCLlkMGWQwjUIJTTEcsqBJVMWM6ZjfkTGTHKIZKL4MRkPTDRAI3IWwjsA41rKUzLimoOKtRqTtzu7sbXrGtv21JU0uLoqaFGFzvpQuTYMy--vqMYO87VrLa1aupovKLYFXb2uaLYdnM2g2w12zmO_02hj-7UrzslJiXWwF79zQl7u58-zh2j5tHic3S6jXCjVRxoFgMY4ZTkrkCcJ01zmmqsky1EqwDhOszxjKWqrlYQUbcq0Ah0jT4UAMSFyfzf3LgRvS9P5qkG_NQzMkMsccpkhl_nNtfOu9l73kTW2-LMOfXbAzR6o2tL5Bj-drwvT47Z2vvTY5lUw4v8fP7vTeVo</recordid><startdate>20180504</startdate><enddate>20180504</enddate><creator>dos Santos, Klecia M.</creator><creator>Barbosa, Raquel de Melo</creator><creator>Vargas, Fernanda Grace A.</creator><creator>de Azevedo, Eduardo Pereira</creator><creator>Lins, Antônio Cláudio da Silva</creator><creator>Camara, Celso A.</creator><creator>Aragão, Cícero F. S.</creator><creator>Moura, Tulio Flavio de Lima e</creator><creator>Raffin, Fernanda Nervo</creator><general>Taylor & Francis</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><orcidid>https://orcid.org/0000-0002-3434-2602</orcidid></search><sort><creationdate>20180504</creationdate><title>Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method</title><author>dos Santos, Klecia M. ; Barbosa, Raquel de Melo ; Vargas, Fernanda Grace A. ; de Azevedo, Eduardo Pereira ; Lins, Antônio Cláudio da Silva ; Camara, Celso A. ; Aragão, Cícero F. S. ; Moura, Tulio Flavio de Lima e ; Raffin, Fernanda Nervo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c366t-9a3009a481c1da2771925c9267bca560a448bcb18a9e96508ae8196094a283303</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2018</creationdate><topic>dissolution rate</topic><topic>PEG 6000</topic><topic>PVP K30</topic><topic>solid dispersion</topic><topic>β-Lapachone</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>dos Santos, Klecia M.</creatorcontrib><creatorcontrib>Barbosa, Raquel de Melo</creatorcontrib><creatorcontrib>Vargas, Fernanda Grace A.</creatorcontrib><creatorcontrib>de Azevedo, Eduardo Pereira</creatorcontrib><creatorcontrib>Lins, Antônio Cláudio da Silva</creatorcontrib><creatorcontrib>Camara, Celso A.</creatorcontrib><creatorcontrib>Aragão, Cícero F. S.</creatorcontrib><creatorcontrib>Moura, Tulio Flavio de Lima e</creatorcontrib><creatorcontrib>Raffin, Fernanda Nervo</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><jtitle>Drug development and industrial pharmacy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>dos Santos, Klecia M.</au><au>Barbosa, Raquel de Melo</au><au>Vargas, Fernanda Grace A.</au><au>de Azevedo, Eduardo Pereira</au><au>Lins, Antônio Cláudio da Silva</au><au>Camara, Celso A.</au><au>Aragão, Cícero F. S.</au><au>Moura, Tulio Flavio de Lima e</au><au>Raffin, Fernanda Nervo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method</atitle><jtitle>Drug development and industrial pharmacy</jtitle><addtitle>Drug Dev Ind Pharm</addtitle><date>2018-05-04</date><risdate>2018</risdate><volume>44</volume><issue>5</issue><spage>750</spage><epage>756</epage><pages>750-756</pages><issn>0363-9045</issn><eissn>1520-5762</eissn><abstract>β-lapachone (βlap) has shown potential use in various medical applications. However, its poor solubility has limited its systemic administration and clinical applications. The aim of this work is to develop solid dispersions of βlap using poly (ethylene glycol) (PEG 6000) and polyvinylpyrrolidone (PVP K30) as hydrophilic polymers and evaluate the dissolution rate in aqueous medium. Solid dispersions were prepared by solvent evaporation method using different weight ratios of βlap and hydrophilic polymer (1:1, 1:2, and 1:3). Characterization performed by differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy showed that βlap was molecularly dispersed within the polymer matrix. The in vitro dissolution tests showed an enhancement in the dissolution profile of βlap as solid dispersions prepared in both PVP and PEG, although the former showed better results. The drug:polymer ratio influenced βlap dissolution rate, as higher amounts of hydrophilic polymer led to enhanced drug dissolution. Thus, this study demonstrated that solid dispersions of βlap in PVP offers an effective way to overcome the poor dissolution of βlap.</abstract><cop>England</cop><pub>Taylor & Francis</pub><pmid>29206496</pmid><doi>10.1080/03639045.2017.1411942</doi><tpages>7</tpages><orcidid>https://orcid.org/0000-0002-3434-2602</orcidid></addata></record> |
fulltext | fulltext |
identifier | ISSN: 0363-9045 |
ispartof | Drug development and industrial pharmacy, 2018-05, Vol.44 (5), p.750-756 |
issn | 0363-9045 1520-5762 |
language | eng |
recordid | cdi_pubmed_primary_29206496 |
source | Business Source Complete |
subjects | dissolution rate PEG 6000 PVP K30 solid dispersion β-Lapachone |
title | Development of solid dispersions of β-lapachone in PEG and PVP by solvent evaporation method |
url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-27T20%3A16%3A15IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-pubmed_infor&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Development%20of%20solid%20dispersions%20of%20%CE%B2-lapachone%20in%20PEG%20and%20PVP%20by%20solvent%20evaporation%20method&rft.jtitle=Drug%20development%20and%20industrial%20pharmacy&rft.au=dos%20Santos,%20Klecia%20M.&rft.date=2018-05-04&rft.volume=44&rft.issue=5&rft.spage=750&rft.epage=756&rft.pages=750-756&rft.issn=0363-9045&rft.eissn=1520-5762&rft_id=info:doi/10.1080/03639045.2017.1411942&rft_dat=%3Cpubmed_infor%3E29206496%3C/pubmed_infor%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/29206496&rfr_iscdi=true |