ParkinsonFranceV1, PascalFrancis, Corpus, bibRecord, 000403

Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug

Identifieur interne : 000403 ( PascalFrancis/Corpus ); précédent : 000402; suivant : 000404

Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug

Auteurs : E. D'Aurizio ; C. F. Van Nostrum ; M. J. Van Steenbergen ; P. Sozio ; F. Siepmann ; J. Siepmann ; W. E. Hennink ; A. Di Stefano

Source :

International journal of pharmaceutics [ 0378-5173 ] ; 2011.

RBID : Pascal:11-0233851

Descripteurs français

Pascal (Inist)
- Préparation, Caractérisation, Copolymère, Lactique acide copolymère, Glycolique acide copolymère, Microsphère, Antiparkinsonien, Promédicament, Maladie de Parkinson, Lévodopa, Acide 1,2-dithiolane-3-valérique, Hydrolyse, Cinétique, Lactique acide polymère, Glycolique acide polymère, Libération, Technologie pharmaceutique, Lactone copolymère, Lactone polymère, Polymère aliphatique.

English descriptors

KwdEn :
- Aliphatic polymer, Antiparkinson agent, Characterization, Copolymer, Glycolic acid copolymer, Glycolic acid polymer, Hydrolysis, Kinetics, Lactic acid copolymer, Lactic acid polymer, Lactone copolymer, Lactone polymer, Levodopa, Microsphere, Parkinson disease, Pharmaceutical technology, Preparation, Prodrug, Release, Thioctic acid.

Abstract

L-Dopa-α-lipoic acid (LD-LA) is a new multifunctional prodrug for the treatment of Parkinson's disease. In human plasma, LD-LA catechol esters and amide bonds are chemically and enzymatically cleaved, respectively, resulting in a half-life time of about fifty minutes. In the present work, the unstable LD-LA was entrapped into biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres designed as depot systems to protect this prodrug against degradation and to obtain a sustained release of the intact compound. The microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique and the effect of formulation and processing parameters (polymer concentration in the organic solvent, volumes ratio of the phases, rate of the organic solvent evaporation) on microspheres characteristics (size, loading, morphology, release) was investigated. Also emphasis was given on the stability of the drug before and after release as well as on the underlying mass transport mechanisms controlling LD-LA release. Interestingly, when encapsulated in appropriate conditions into PLGA microspheres, the labile prodrug was stabilized and released via Fickian diffusion up to more than one week.

Notice en format standard (ISO 2709)

Pour connaître la documentation sur le format Inist Standard.

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Format Inist (serveur)

NO :	PASCAL 11-0233851 INIST
ET :	Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug
AU :	D'AURIZIO (E.); VAN NOSTRUM (C. F.); VAN STEENBERGEN (M. J.); SOZIO (P.); SIEPMANN (F.); SIEPMANN (J.); HENNINK (W. E.); DI STEFANO (A.)
AF :	Department of Pharmaceutical Sciences, "G. DAnnunzio" University, Via dei Vestini 31/66100 Chieti/Italie (1 aut., 4 aut., 8 aut.); Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082/3508 TB Utrecht/Pays-Bas (2 aut., 3 aut., 7 aut.); INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, College of Pharmacy, University Lille Nord de France/Lille/France (5 aut., 6 aut.)
DT :	Publication en série; Niveau analytique
SO :	International journal of pharmaceutics; ISSN 0378-5173; Coden IJPHDE; Pays-Bas; Da. 2011; Vol. 409; No. 1-2; Pp. 289-296; Bibl. 3/4 p.
LA :	Anglais
EA :	L-Dopa-α-lipoic acid (LD-LA) is a new multifunctional prodrug for the treatment of Parkinson's disease. In human plasma, LD-LA catechol esters and amide bonds are chemically and enzymatically cleaved, respectively, resulting in a half-life time of about fifty minutes. In the present work, the unstable LD-LA was entrapped into biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres designed as depot systems to protect this prodrug against degradation and to obtain a sustained release of the intact compound. The microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique and the effect of formulation and processing parameters (polymer concentration in the organic solvent, volumes ratio of the phases, rate of the organic solvent evaporation) on microspheres characteristics (size, loading, morphology, release) was investigated. Also emphasis was given on the stability of the drug before and after release as well as on the underlying mass transport mechanisms controlling LD-LA release. Interestingly, when encapsulated in appropriate conditions into PLGA microspheres, the labile prodrug was stabilized and released via Fickian diffusion up to more than one week.
CC :	002B02A03
FD :	Préparation; Caractérisation; Copolymère; Lactique acide copolymère; Glycolique acide copolymère; Microsphère; Antiparkinsonien; Promédicament; Maladie de Parkinson; Lévodopa; Acide 1,2-dithiolane-3-valérique; Hydrolyse; Cinétique; Lactique acide polymère; Glycolique acide polymère; Libération; Technologie pharmaceutique; Lactone copolymère; Lactone polymère; Polymère aliphatique
FG :	Microparticule; Pathologie de l'encéphale; Syndrome extrapyramidal; Maladie dégénérative; Pathologie du système nerveux central; Pathologie du système nerveux; Agoniste; Récepteur dopaminergique D2; Antioxydant
ED :	Preparation; Characterization; Copolymer; Lactic acid copolymer; Glycolic acid copolymer; Microsphere; Antiparkinson agent; Prodrug; Parkinson disease; Levodopa; Thioctic acid; Hydrolysis; Kinetics; Lactic acid polymer; Glycolic acid polymer; Release; Pharmaceutical technology; Lactone copolymer; Lactone polymer; Aliphatic polymer
EG :	Microparticle; Cerebral disorder; Extrapyramidal syndrome; Degenerative disease; Central nervous system disease; Nervous system diseases; Agonist; D2 Dopamine receptor; Antioxidant
SD :	Preparación; Caracterización; Copolímero; Láctico ácido copolímero; Glicolico acido copolimero; Microsfera; Antiparkinsoniano; Promedicamento; Parkinson enfermedad; Levodopa; Tióctico ácido; Hidrólisis; Cinética; Láctico ácido polímero; Glicólico ácido polímero; Liberación; Tecnología farmacéutica; Lactona copolímero; Lactona polímero; Polímero alifático
LO :	INIST-16510.354000192046770360
ID :	11-0233851

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Pascal:11-0233851

Le document en format XML

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<author><name sortKey="Siepmann, F" sort="Siepmann, F" uniqKey="Siepmann F" first="F." last="Siepmann">F. Siepmann</name>
<affiliation><inist:fA14 i1="03"><s1>INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, College of Pharmacy, University Lille Nord de France</s1>
<s2>Lille</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Siepmann, J" sort="Siepmann, J" uniqKey="Siepmann J" first="J." last="Siepmann">J. Siepmann</name>
<affiliation><inist:fA14 i1="03"><s1>INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, College of Pharmacy, University Lille Nord de France</s1>
<s2>Lille</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Hennink, W E" sort="Hennink, W E" uniqKey="Hennink W" first="W. E." last="Hennink">W. E. Hennink</name>
<affiliation><inist:fA14 i1="02"><s1>Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082</s1>
<s2>3508 TB Utrecht</s2>
<s3>NLD</s3>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>7 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
<author><name sortKey="Di Stefano, A" sort="Di Stefano, A" uniqKey="Di Stefano A" first="A." last="Di Stefano">A. Di Stefano</name>
<affiliation><inist:fA14 i1="01"><s1>Department of Pharmaceutical Sciences, "G. DAnnunzio" University, Via dei Vestini 31</s1>
<s2>66100 Chieti</s2>
<s3>ITA</s3>
<sZ>1 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>8 aut.</sZ>
</inist:fA14>
</affiliation>
</author>
</analytic>
<series><title level="j" type="main">International journal of pharmaceutics</title>
<title level="j" type="abbreviated">Int. j. pharm.</title>
<idno type="ISSN">0378-5173</idno>
<imprint><date when="2011">2011</date>
</imprint>
</series>
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<seriesStmt><title level="j" type="main">International journal of pharmaceutics</title>
<title level="j" type="abbreviated">Int. j. pharm.</title>
<idno type="ISSN">0378-5173</idno>
</seriesStmt>
</fileDesc>
<profileDesc><textClass><keywords scheme="KwdEn" xml:lang="en"><term>Aliphatic polymer</term>
<term>Antiparkinson agent</term>
<term>Characterization</term>
<term>Copolymer</term>
<term>Glycolic acid copolymer</term>
<term>Glycolic acid polymer</term>
<term>Hydrolysis</term>
<term>Kinetics</term>
<term>Lactic acid copolymer</term>
<term>Lactic acid polymer</term>
<term>Lactone copolymer</term>
<term>Lactone polymer</term>
<term>Levodopa</term>
<term>Microsphere</term>
<term>Parkinson disease</term>
<term>Pharmaceutical technology</term>
<term>Preparation</term>
<term>Prodrug</term>
<term>Release</term>
<term>Thioctic acid</term>
</keywords>
<keywords scheme="Pascal" xml:lang="fr"><term>Préparation</term>
<term>Caractérisation</term>
<term>Copolymère</term>
<term>Lactique acide copolymère</term>
<term>Glycolique acide copolymère</term>
<term>Microsphère</term>
<term>Antiparkinsonien</term>
<term>Promédicament</term>
<term>Maladie de Parkinson</term>
<term>Lévodopa</term>
<term>Acide 1,2-dithiolane-3-valérique</term>
<term>Hydrolyse</term>
<term>Cinétique</term>
<term>Lactique acide polymère</term>
<term>Glycolique acide polymère</term>
<term>Libération</term>
<term>Technologie pharmaceutique</term>
<term>Lactone copolymère</term>
<term>Lactone polymère</term>
<term>Polymère aliphatique</term>
</keywords>
</textClass>
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<front><div type="abstract" xml:lang="en">L-Dopa-α-lipoic acid (LD-LA) is a new multifunctional prodrug for the treatment of Parkinson's disease. In human plasma, LD-LA catechol esters and amide bonds are chemically and enzymatically cleaved, respectively, resulting in a half-life time of about fifty minutes. In the present work, the unstable LD-LA was entrapped into biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres designed as depot systems to protect this prodrug against degradation and to obtain a sustained release of the intact compound. The microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique and the effect of formulation and processing parameters (polymer concentration in the organic solvent, volumes ratio of the phases, rate of the organic solvent evaporation) on microspheres characteristics (size, loading, morphology, release) was investigated. Also emphasis was given on the stability of the drug before and after release as well as on the underlying mass transport mechanisms controlling LD-LA release. Interestingly, when encapsulated in appropriate conditions into PLGA microspheres, the labile prodrug was stabilized and released via Fickian diffusion up to more than one week.</div>
</front>
</TEI>
<inist><standard h6="B"><pA><fA01 i1="01" i2="1"><s0>0378-5173</s0>
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<fA02 i1="01"><s0>IJPHDE</s0>
</fA02>
<fA03 i2="1"><s0>Int. j. pharm.</s0>
</fA03>
<fA05><s2>409</s2>
</fA05>
<fA06><s2>1-2</s2>
</fA06>
<fA08 i1="01" i2="1" l="ENG"><s1>Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug</s1>
</fA08>
<fA11 i1="01" i2="1"><s1>D'AURIZIO (E.)</s1>
</fA11>
<fA11 i1="02" i2="1"><s1>VAN NOSTRUM (C. F.)</s1>
</fA11>
<fA11 i1="03" i2="1"><s1>VAN STEENBERGEN (M. J.)</s1>
</fA11>
<fA11 i1="04" i2="1"><s1>SOZIO (P.)</s1>
</fA11>
<fA11 i1="05" i2="1"><s1>SIEPMANN (F.)</s1>
</fA11>
<fA11 i1="06" i2="1"><s1>SIEPMANN (J.)</s1>
</fA11>
<fA11 i1="07" i2="1"><s1>HENNINK (W. E.)</s1>
</fA11>
<fA11 i1="08" i2="1"><s1>DI STEFANO (A.)</s1>
</fA11>
<fA14 i1="01"><s1>Department of Pharmaceutical Sciences, "G. DAnnunzio" University, Via dei Vestini 31</s1>
<s2>66100 Chieti</s2>
<s3>ITA</s3>
<sZ>1 aut.</sZ>
<sZ>4 aut.</sZ>
<sZ>8 aut.</sZ>
</fA14>
<fA14 i1="02"><s1>Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082</s1>
<s2>3508 TB Utrecht</s2>
<s3>NLD</s3>
<sZ>2 aut.</sZ>
<sZ>3 aut.</sZ>
<sZ>7 aut.</sZ>
</fA14>
<fA14 i1="03"><s1>INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, College of Pharmacy, University Lille Nord de France</s1>
<s2>Lille</s2>
<s3>FRA</s3>
<sZ>5 aut.</sZ>
<sZ>6 aut.</sZ>
</fA14>
<fA20><s1>289-296</s1>
</fA20>
<fA21><s1>2011</s1>
</fA21>
<fA23 i1="01"><s0>ENG</s0>
</fA23>
<fA43 i1="01"><s1>INIST</s1>
<s2>16510</s2>
<s5>354000192046770360</s5>
</fA43>
<fA44><s0>0000</s0>
<s1>© 2011 INIST-CNRS. All rights reserved.</s1>
</fA44>
<fA45><s0>3/4 p.</s0>
</fA45>
<fA47 i1="01" i2="1"><s0>11-0233851</s0>
</fA47>
<fA60><s1>P</s1>
</fA60>
<fA61><s0>A</s0>
</fA61>
<fA64 i1="01" i2="1"><s0>International journal of pharmaceutics</s0>
</fA64>
<fA66 i1="01"><s0>NLD</s0>
</fA66>
<fC01 i1="01" l="ENG"><s0>L-Dopa-α-lipoic acid (LD-LA) is a new multifunctional prodrug for the treatment of Parkinson's disease. In human plasma, LD-LA catechol esters and amide bonds are chemically and enzymatically cleaved, respectively, resulting in a half-life time of about fifty minutes. In the present work, the unstable LD-LA was entrapped into biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres designed as depot systems to protect this prodrug against degradation and to obtain a sustained release of the intact compound. The microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique and the effect of formulation and processing parameters (polymer concentration in the organic solvent, volumes ratio of the phases, rate of the organic solvent evaporation) on microspheres characteristics (size, loading, morphology, release) was investigated. Also emphasis was given on the stability of the drug before and after release as well as on the underlying mass transport mechanisms controlling LD-LA release. Interestingly, when encapsulated in appropriate conditions into PLGA microspheres, the labile prodrug was stabilized and released via Fickian diffusion up to more than one week.</s0>
</fC01>
<fC02 i1="01" i2="X"><s0>002B02A03</s0>
</fC02>
<fC03 i1="01" i2="X" l="FRE"><s0>Préparation</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="ENG"><s0>Preparation</s0>
<s5>01</s5>
</fC03>
<fC03 i1="01" i2="X" l="SPA"><s0>Preparación</s0>
<s5>01</s5>
</fC03>
<fC03 i1="02" i2="X" l="FRE"><s0>Caractérisation</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="ENG"><s0>Characterization</s0>
<s5>02</s5>
</fC03>
<fC03 i1="02" i2="X" l="SPA"><s0>Caracterización</s0>
<s5>02</s5>
</fC03>
<fC03 i1="03" i2="X" l="FRE"><s0>Copolymère</s0>
<s2>NK</s2>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="ENG"><s0>Copolymer</s0>
<s2>NK</s2>
<s5>03</s5>
</fC03>
<fC03 i1="03" i2="X" l="SPA"><s0>Copolímero</s0>
<s2>NK</s2>
<s5>03</s5>
</fC03>
<fC03 i1="04" i2="X" l="FRE"><s0>Lactique acide copolymère</s0>
<s2>NK</s2>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="ENG"><s0>Lactic acid copolymer</s0>
<s2>NK</s2>
<s5>04</s5>
</fC03>
<fC03 i1="04" i2="X" l="SPA"><s0>Láctico ácido copolímero</s0>
<s2>NK</s2>
<s5>04</s5>
</fC03>
<fC03 i1="05" i2="X" l="FRE"><s0>Glycolique acide copolymère</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="ENG"><s0>Glycolic acid copolymer</s0>
<s5>05</s5>
</fC03>
<fC03 i1="05" i2="X" l="SPA"><s0>Glicolico acido copolimero</s0>
<s5>05</s5>
</fC03>
<fC03 i1="06" i2="X" l="FRE"><s0>Microsphère</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="ENG"><s0>Microsphere</s0>
<s5>06</s5>
</fC03>
<fC03 i1="06" i2="X" l="SPA"><s0>Microsfera</s0>
<s5>06</s5>
</fC03>
<fC03 i1="07" i2="X" l="FRE"><s0>Antiparkinsonien</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="ENG"><s0>Antiparkinson agent</s0>
<s5>07</s5>
</fC03>
<fC03 i1="07" i2="X" l="SPA"><s0>Antiparkinsoniano</s0>
<s5>07</s5>
</fC03>
<fC03 i1="08" i2="X" l="FRE"><s0>Promédicament</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="ENG"><s0>Prodrug</s0>
<s5>08</s5>
</fC03>
<fC03 i1="08" i2="X" l="SPA"><s0>Promedicamento</s0>
<s5>08</s5>
</fC03>
<fC03 i1="09" i2="X" l="FRE"><s0>Maladie de Parkinson</s0>
<s2>NM</s2>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="ENG"><s0>Parkinson disease</s0>
<s2>NM</s2>
<s5>09</s5>
</fC03>
<fC03 i1="09" i2="X" l="SPA"><s0>Parkinson enfermedad</s0>
<s2>NM</s2>
<s5>09</s5>
</fC03>
<fC03 i1="10" i2="X" l="FRE"><s0>Lévodopa</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="ENG"><s0>Levodopa</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="10" i2="X" l="SPA"><s0>Levodopa</s0>
<s2>NK</s2>
<s2>FR</s2>
<s5>10</s5>
</fC03>
<fC03 i1="11" i2="X" l="FRE"><s0>Acide 1,2-dithiolane-3-valérique</s0>
<s2>NK</s2>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="ENG"><s0>Thioctic acid</s0>
<s2>NK</s2>
<s5>11</s5>
</fC03>
<fC03 i1="11" i2="X" l="SPA"><s0>Tióctico ácido</s0>
<s2>NK</s2>
<s5>11</s5>
</fC03>
<fC03 i1="12" i2="X" l="FRE"><s0>Hydrolyse</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="ENG"><s0>Hydrolysis</s0>
<s5>12</s5>
</fC03>
<fC03 i1="12" i2="X" l="SPA"><s0>Hidrólisis</s0>
<s5>12</s5>
</fC03>
<fC03 i1="13" i2="X" l="FRE"><s0>Cinétique</s0>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="ENG"><s0>Kinetics</s0>
<s5>13</s5>
</fC03>
<fC03 i1="13" i2="X" l="SPA"><s0>Cinética</s0>
<s5>13</s5>
</fC03>
<fC03 i1="14" i2="X" l="FRE"><s0>Lactique acide polymère</s0>
<s2>NK</s2>
<s5>14</s5>
</fC03>
<fC03 i1="14" i2="X" l="ENG"><s0>Lactic acid polymer</s0>
<s2>NK</s2>
<s5>14</s5>
</fC03>
<fC03 i1="14" i2="X" l="SPA"><s0>Láctico ácido polímero</s0>
<s2>NK</s2>
<s5>14</s5>
</fC03>
<fC03 i1="15" i2="X" l="FRE"><s0>Glycolique acide polymère</s0>
<s2>NK</s2>
<s5>15</s5>
</fC03>
<fC03 i1="15" i2="X" l="ENG"><s0>Glycolic acid polymer</s0>
<s2>NK</s2>
<s5>15</s5>
</fC03>
<fC03 i1="15" i2="X" l="SPA"><s0>Glicólico ácido polímero</s0>
<s2>NK</s2>
<s5>15</s5>
</fC03>
<fC03 i1="16" i2="X" l="FRE"><s0>Libération</s0>
<s5>16</s5>
</fC03>
<fC03 i1="16" i2="X" l="ENG"><s0>Release</s0>
<s5>16</s5>
</fC03>
<fC03 i1="16" i2="X" l="SPA"><s0>Liberación</s0>
<s5>16</s5>
</fC03>
<fC03 i1="17" i2="X" l="FRE"><s0>Technologie pharmaceutique</s0>
<s5>23</s5>
</fC03>
<fC03 i1="17" i2="X" l="ENG"><s0>Pharmaceutical technology</s0>
<s5>23</s5>
</fC03>
<fC03 i1="17" i2="X" l="SPA"><s0>Tecnología farmacéutica</s0>
<s5>23</s5>
</fC03>
<fC03 i1="18" i2="X" l="FRE"><s0>Lactone copolymère</s0>
<s2>NK</s2>
<s5>24</s5>
</fC03>
<fC03 i1="18" i2="X" l="ENG"><s0>Lactone copolymer</s0>
<s2>NK</s2>
<s5>24</s5>
</fC03>
<fC03 i1="18" i2="X" l="SPA"><s0>Lactona copolímero</s0>
<s2>NK</s2>
<s5>24</s5>
</fC03>
<fC03 i1="19" i2="X" l="FRE"><s0>Lactone polymère</s0>
<s2>NK</s2>
<s5>25</s5>
</fC03>
<fC03 i1="19" i2="X" l="ENG"><s0>Lactone polymer</s0>
<s2>NK</s2>
<s5>25</s5>
</fC03>
<fC03 i1="19" i2="X" l="SPA"><s0>Lactona polímero</s0>
<s2>NK</s2>
<s5>25</s5>
</fC03>
<fC03 i1="20" i2="X" l="FRE"><s0>Polymère aliphatique</s0>
<s5>26</s5>
</fC03>
<fC03 i1="20" i2="X" l="ENG"><s0>Aliphatic polymer</s0>
<s5>26</s5>
</fC03>
<fC03 i1="20" i2="X" l="SPA"><s0>Polímero alifático</s0>
<s5>26</s5>
</fC03>
<fC07 i1="01" i2="X" l="FRE"><s0>Microparticule</s0>
<s5>37</s5>
</fC07>
<fC07 i1="01" i2="X" l="ENG"><s0>Microparticle</s0>
<s5>37</s5>
</fC07>
<fC07 i1="01" i2="X" l="SPA"><s0>Micropartícula</s0>
<s5>37</s5>
</fC07>
<fC07 i1="02" i2="X" l="FRE"><s0>Pathologie de l'encéphale</s0>
<s5>38</s5>
</fC07>
<fC07 i1="02" i2="X" l="ENG"><s0>Cerebral disorder</s0>
<s5>38</s5>
</fC07>
<fC07 i1="02" i2="X" l="SPA"><s0>Encéfalo patología</s0>
<s5>38</s5>
</fC07>
<fC07 i1="03" i2="X" l="FRE"><s0>Syndrome extrapyramidal</s0>
<s5>39</s5>
</fC07>
<fC07 i1="03" i2="X" l="ENG"><s0>Extrapyramidal syndrome</s0>
<s5>39</s5>
</fC07>
<fC07 i1="03" i2="X" l="SPA"><s0>Extrapiramidal síndrome</s0>
<s5>39</s5>
</fC07>
<fC07 i1="04" i2="X" l="FRE"><s0>Maladie dégénérative</s0>
<s5>40</s5>
</fC07>
<fC07 i1="04" i2="X" l="ENG"><s0>Degenerative disease</s0>
<s5>40</s5>
</fC07>
<fC07 i1="04" i2="X" l="SPA"><s0>Enfermedad degenerativa</s0>
<s5>40</s5>
</fC07>
<fC07 i1="05" i2="X" l="FRE"><s0>Pathologie du   système nerveux central</s0>
<s5>41</s5>
</fC07>
<fC07 i1="05" i2="X" l="ENG"><s0>Central nervous system disease</s0>
<s5>41</s5>
</fC07>
<fC07 i1="05" i2="X" l="SPA"><s0>Sistema nervosio central patología</s0>
<s5>41</s5>
</fC07>
<fC07 i1="06" i2="X" l="FRE"><s0>Pathologie du   système nerveux</s0>
<s5>42</s5>
</fC07>
<fC07 i1="06" i2="X" l="ENG"><s0>Nervous system diseases</s0>
<s5>42</s5>
</fC07>
<fC07 i1="06" i2="X" l="SPA"><s0>Sistema nervioso patología</s0>
<s5>42</s5>
</fC07>
<fC07 i1="07" i2="X" l="FRE"><s0>Agoniste</s0>
<s5>43</s5>
</fC07>
<fC07 i1="07" i2="X" l="ENG"><s0>Agonist</s0>
<s5>43</s5>
</fC07>
<fC07 i1="07" i2="X" l="SPA"><s0>Agonista</s0>
<s5>43</s5>
</fC07>
<fC07 i1="08" i2="X" l="FRE"><s0>Récepteur dopaminergique D2</s0>
<s5>44</s5>
</fC07>
<fC07 i1="08" i2="X" l="ENG"><s0>D2 Dopamine receptor</s0>
<s5>44</s5>
</fC07>
<fC07 i1="08" i2="X" l="SPA"><s0>Receptor dopaminérgico D2</s0>
<s5>44</s5>
</fC07>
<fC07 i1="09" i2="X" l="FRE"><s0>Antioxydant</s0>
<s5>45</s5>
</fC07>
<fC07 i1="09" i2="X" l="ENG"><s0>Antioxidant</s0>
<s5>45</s5>
</fC07>
<fC07 i1="09" i2="X" l="SPA"><s0>Antioxidante</s0>
<s5>45</s5>
</fC07>
<fN21><s1>157</s1>
</fN21>
<fN44 i1="01"><s1>OTO</s1>
</fN44>
<fN82><s1>OTO</s1>
</fN82>
</pA>
</standard>
<server><NO>PASCAL 11-0233851 INIST</NO>
<ET>Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug</ET>
<AU>D'AURIZIO (E.); VAN NOSTRUM (C. F.); VAN STEENBERGEN (M. J.); SOZIO (P.); SIEPMANN (F.); SIEPMANN (J.); HENNINK (W. E.); DI STEFANO (A.)</AU>
<AF>Department of Pharmaceutical Sciences, "G. DAnnunzio" University, Via dei Vestini 31/66100 Chieti/Italie (1 aut., 4 aut., 8 aut.); Department of Pharmaceutics, Utrecht Institute for Pharmaceutical Sciences (UIPS), Utrecht University, P.O. Box 80082/3508 TB Utrecht/Pays-Bas (2 aut., 3 aut., 7 aut.); INSERM U 1008, Controlled Drug Delivery Systems and Biomaterials, College of Pharmacy, University Lille Nord de France/Lille/France (5 aut., 6 aut.)</AF>
<DT>Publication en série; Niveau analytique</DT>
<SO>International journal of pharmaceutics; ISSN 0378-5173; Coden IJPHDE; Pays-Bas; Da. 2011; Vol. 409; No. 1-2; Pp. 289-296; Bibl. 3/4 p.</SO>
<LA>Anglais</LA>
<EA>L-Dopa-α-lipoic acid (LD-LA) is a new multifunctional prodrug for the treatment of Parkinson's disease. In human plasma, LD-LA catechol esters and amide bonds are chemically and enzymatically cleaved, respectively, resulting in a half-life time of about fifty minutes. In the present work, the unstable LD-LA was entrapped into biodegradable poly(lactic-co-glycolic acid) (PLGA) microspheres designed as depot systems to protect this prodrug against degradation and to obtain a sustained release of the intact compound. The microspheres were prepared by an oil-in-water emulsion/solvent evaporation technique and the effect of formulation and processing parameters (polymer concentration in the organic solvent, volumes ratio of the phases, rate of the organic solvent evaporation) on microspheres characteristics (size, loading, morphology, release) was investigated. Also emphasis was given on the stability of the drug before and after release as well as on the underlying mass transport mechanisms controlling LD-LA release. Interestingly, when encapsulated in appropriate conditions into PLGA microspheres, the labile prodrug was stabilized and released via Fickian diffusion up to more than one week.</EA>
<CC>002B02A03</CC>
<FD>Préparation; Caractérisation; Copolymère; Lactique acide copolymère; Glycolique acide copolymère; Microsphère; Antiparkinsonien; Promédicament; Maladie de Parkinson; Lévodopa; Acide 1,2-dithiolane-3-valérique; Hydrolyse; Cinétique; Lactique acide polymère; Glycolique acide polymère; Libération; Technologie pharmaceutique; Lactone copolymère; Lactone polymère; Polymère aliphatique</FD>
<FG>Microparticule; Pathologie de l'encéphale; Syndrome extrapyramidal; Maladie dégénérative; Pathologie du   système nerveux central; Pathologie du   système nerveux; Agoniste; Récepteur dopaminergique D2; Antioxydant</FG>
<ED>Preparation; Characterization; Copolymer; Lactic acid copolymer; Glycolic acid copolymer; Microsphere; Antiparkinson agent; Prodrug; Parkinson disease; Levodopa; Thioctic acid; Hydrolysis; Kinetics; Lactic acid polymer; Glycolic acid polymer; Release; Pharmaceutical technology; Lactone copolymer; Lactone polymer; Aliphatic polymer</ED>
<EG>Microparticle; Cerebral disorder; Extrapyramidal syndrome; Degenerative disease; Central nervous system disease; Nervous system diseases; Agonist; D2 Dopamine receptor; Antioxidant</EG>
<SD>Preparación; Caracterización; Copolímero; Láctico ácido copolímero; Glicolico acido copolimero; Microsfera; Antiparkinsoniano; Promedicamento; Parkinson enfermedad; Levodopa; Tióctico ácido; Hidrólisis; Cinética; Láctico ácido polímero; Glicólico ácido polímero; Liberación; Tecnología farmacéutica; Lactona copolímero; Lactona polímero; Polímero alifático</SD>
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<ID>11-0233851</ID>
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La maladie de Parkinson en France (serveur d'exploration)

Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug

Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug

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