Inclusion of the poorly water-soluble drug simvastatin in mesocellular foam nanoparticles: Drug loading and release properties

The purpose of this study was to develop spherical mesocellular foam (MCF) loaded with a poorly water-soluble drug, intended to be orally administered, able to improve the dissolution rate and enhance the drug loading capacity. Spherical MCF with a continuous 3-D pore system was synthesized using Pl...

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Veröffentlicht in:International journal of pharmaceutics 2011-05, Vol.410 (1), p.118-124
Hauptverfasser: Zhang, Yanzhuo, Zhang, Jinghai, Jiang, Tongying, Wang, Siling
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container_issue 1
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container_title International journal of pharmaceutics
container_volume 410
creator Zhang, Yanzhuo
Zhang, Jinghai
Jiang, Tongying
Wang, Siling
description The purpose of this study was to develop spherical mesocellular foam (MCF) loaded with a poorly water-soluble drug, intended to be orally administered, able to improve the dissolution rate and enhance the drug loading capacity. Spherical MCF with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. A model drug, simvastatin (SV), was loaded onto spherical MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and HPLC demonstrated the successful incorporation of SV into the MCF host. It was found that spherical MCF has a high drug loading efficiency up to 37.5%, and higher than that of fibrous SBA-15 with a pore diameter of 6.5 nm. It is worth noting that fast release rate of SV was obtained from spherical MCF compared with SBA-15 and pure crystalline SV using enzyme-free simulated intestinal fluid (SIF, pH 6.8).
doi_str_mv 10.1016/j.ijpharm.2010.07.040
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Spherical MCF with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. A model drug, simvastatin (SV), was loaded onto spherical MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and HPLC demonstrated the successful incorporation of SV into the MCF host. It was found that spherical MCF has a high drug loading efficiency up to 37.5%, and higher than that of fibrous SBA-15 with a pore diameter of 6.5 nm. 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Drug treatments ; Poloxalene - chemistry ; polymers ; Poorly water-soluble drugs ; scanning electron microscopy ; Simvastatin ; Simvastatin - administration &amp; dosage ; Simvastatin - chemistry ; Solubility ; solvents ; Solvents - chemistry ; Surface-Active Agents - chemistry ; surfactants ; thermogravimetry ; transmission electron microscopy ; X-ray diffraction</subject><ispartof>International journal of pharmaceutics, 2011-05, Vol.410 (1), p.118-124</ispartof><rights>2010 Elsevier B.V.</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2010 Elsevier B.V. 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Spherical MCF with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. A model drug, simvastatin (SV), was loaded onto spherical MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and HPLC demonstrated the successful incorporation of SV into the MCF host. It was found that spherical MCF has a high drug loading efficiency up to 37.5%, and higher than that of fibrous SBA-15 with a pore diameter of 6.5 nm. It is worth noting that fast release rate of SV was obtained from spherical MCF compared with SBA-15 and pure crystalline SV using enzyme-free simulated intestinal fluid (SIF, pH 6.8).</description><subject>Administration, Oral</subject><subject>adsorption</subject><subject>Biological and medical sciences</subject><subject>Cetrimonium</subject><subject>Cetrimonium Compounds - chemistry</subject><subject>Crystallization</subject><subject>differential scanning calorimetry</subject><subject>Drug delivery</subject><subject>Drug loading</subject><subject>drugs</subject><subject>Enhanced dissolution</subject><subject>evaporation</subject><subject>foams</subject><subject>General pharmacology</subject><subject>high performance liquid chromatography</subject><subject>Medical sciences</subject><subject>Mesocellular foam</subject><subject>Nanoparticles</subject><subject>nitrogen</subject><subject>oral administration</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Poloxalene - chemistry</subject><subject>polymers</subject><subject>Poorly water-soluble drugs</subject><subject>scanning electron microscopy</subject><subject>Simvastatin</subject><subject>Simvastatin - administration &amp; dosage</subject><subject>Simvastatin - chemistry</subject><subject>Solubility</subject><subject>solvents</subject><subject>Solvents - chemistry</subject><subject>Surface-Active Agents - chemistry</subject><subject>surfactants</subject><subject>thermogravimetry</subject><subject>transmission electron microscopy</subject><subject>X-ray diffraction</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM-L1DAYhoso7uzqn6DmIp46fvnRpvUisq66sOBB9xzS5OtshjSpSbuyF_92M8yoRyEQCM-b9-WpqhcUthRo-3a_dfv5Tqdpy6C8gdyCgEfVhnaS11zI9nG1AS67uqGSn1XnOe8BoGWUP63OGLRSSNZvql_Xwfg1uxhIHMlyh2SOMfkH8lMvmOoc_Tp4JDatO5LddK_zohcXSDkT5mjQ-9XrRMaoJxJ0iLNOizMe8zvy8RDyUVsXdkQHSxJ61LlUpDhjwTA_q56M2md8frovqttPV98vv9Q3Xz9fX364qY2g3VI3QoJspOgpQ95yHBpogY4NY6IbeBGArRmsbYztuQWGUsNIRwljz9kgqOAX1Zvjv6X6x4p5UZPLh_E6YFyz6lohu0b2XSGbI2lSzDnhqObkJp0eFAV1MK_26mReHcwrkKqYL7mXp4Z1mND-Tf1RXYDXJ0Bno_2YdDAu_-ME7csAWrhXR27UUeldKsztt9LUAFAmGG0K8f5IYDF27zCpbBwGg9YlNIuy0f1n7G9CwK84</recordid><startdate>20110530</startdate><enddate>20110530</enddate><creator>Zhang, Yanzhuo</creator><creator>Zhang, Jinghai</creator><creator>Jiang, Tongying</creator><creator>Wang, Siling</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>FBQ</scope><scope>IQODW</scope><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></search><sort><creationdate>20110530</creationdate><title>Inclusion of the poorly water-soluble drug simvastatin in mesocellular foam nanoparticles: Drug loading and release properties</title><author>Zhang, Yanzhuo ; Zhang, Jinghai ; Jiang, Tongying ; Wang, Siling</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c418t-54707574912e363eb50601f52248b3201e6cbdd5cd93d02e7a0f1f70f932b4143</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Administration, Oral</topic><topic>adsorption</topic><topic>Biological and medical sciences</topic><topic>Cetrimonium</topic><topic>Cetrimonium Compounds - chemistry</topic><topic>Crystallization</topic><topic>differential scanning calorimetry</topic><topic>Drug delivery</topic><topic>Drug loading</topic><topic>drugs</topic><topic>Enhanced dissolution</topic><topic>evaporation</topic><topic>foams</topic><topic>General pharmacology</topic><topic>high performance liquid chromatography</topic><topic>Medical sciences</topic><topic>Mesocellular foam</topic><topic>Nanoparticles</topic><topic>nitrogen</topic><topic>oral administration</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Poloxalene - chemistry</topic><topic>polymers</topic><topic>Poorly water-soluble drugs</topic><topic>scanning electron microscopy</topic><topic>Simvastatin</topic><topic>Simvastatin - administration &amp; dosage</topic><topic>Simvastatin - chemistry</topic><topic>Solubility</topic><topic>solvents</topic><topic>Solvents - chemistry</topic><topic>Surface-Active Agents - chemistry</topic><topic>surfactants</topic><topic>thermogravimetry</topic><topic>transmission electron microscopy</topic><topic>X-ray diffraction</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhang, Yanzhuo</creatorcontrib><creatorcontrib>Zhang, Jinghai</creatorcontrib><creatorcontrib>Jiang, Tongying</creatorcontrib><creatorcontrib>Wang, Siling</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><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><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhang, Yanzhuo</au><au>Zhang, Jinghai</au><au>Jiang, Tongying</au><au>Wang, Siling</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Inclusion of the poorly water-soluble drug simvastatin in mesocellular foam nanoparticles: Drug loading and release properties</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2011-05-30</date><risdate>2011</risdate><volume>410</volume><issue>1</issue><spage>118</spage><epage>124</epage><pages>118-124</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The purpose of this study was to develop spherical mesocellular foam (MCF) loaded with a poorly water-soluble drug, intended to be orally administered, able to improve the dissolution rate and enhance the drug loading capacity. Spherical MCF with a continuous 3-D pore system was synthesized using Pluronic 123 triblock polymer (P123) as a surfactant coupled with cetyltrimethyl ammonium bromide (CTAB) as a co-surfactant. A model drug, simvastatin (SV), was loaded onto spherical MCF via a procedure involving a combination of adsorption equilibrium and solvent evaporation. The drug release rate and the drug loading efficiency of spherical MCF were compared with those of fibrous SBA-15. Investigations using nitrogen adsorption, scanning electron microscopy (SEM), transmission electron microscopy (TEM), powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and HPLC demonstrated the successful incorporation of SV into the MCF host. It was found that spherical MCF has a high drug loading efficiency up to 37.5%, and higher than that of fibrous SBA-15 with a pore diameter of 6.5 nm. It is worth noting that fast release rate of SV was obtained from spherical MCF compared with SBA-15 and pure crystalline SV using enzyme-free simulated intestinal fluid (SIF, pH 6.8).</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>20674729</pmid><doi>10.1016/j.ijpharm.2010.07.040</doi><tpages>7</tpages></addata></record>
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identifier ISSN: 0378-5173
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source MEDLINE; ScienceDirect Journals (5 years ago - present)
subjects Administration, Oral
adsorption
Biological and medical sciences
Cetrimonium
Cetrimonium Compounds - chemistry
Crystallization
differential scanning calorimetry
Drug delivery
Drug loading
drugs
Enhanced dissolution
evaporation
foams
General pharmacology
high performance liquid chromatography
Medical sciences
Mesocellular foam
Nanoparticles
nitrogen
oral administration
Particle Size
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Poloxalene - chemistry
polymers
Poorly water-soluble drugs
scanning electron microscopy
Simvastatin
Simvastatin - administration & dosage
Simvastatin - chemistry
Solubility
solvents
Solvents - chemistry
Surface-Active Agents - chemistry
surfactants
thermogravimetry
transmission electron microscopy
X-ray diffraction
title Inclusion of the poorly water-soluble drug simvastatin in mesocellular foam nanoparticles: Drug loading and release properties
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