Surfactant-free, biodegradable nanoparticles for aerosol therapy based on the branched polyesters, DEAPA-PVAL-g-PLGA

This study describes the development of surfactant-free, biodegradable nanoparticle systems with varying physicochemical properties and their suitability for pulmonary application via nebulization. Nanoparticle suspensions were formulated from the branched polyester, diethylaminopropyl amine-poly(vi...

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Veröffentlicht in:Pharmaceutical research 2003-12, Vol.20 (12), p.2011-2020
Hauptverfasser: DAILEY, L. A, KLEEMANN, E, WITTMAR, M, GESSLER, T, SCHMEHL, T, ROBERTS, C, SEEGER, W, KISSEL, T
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container_end_page 2020
container_issue 12
container_start_page 2011
container_title Pharmaceutical research
container_volume 20
creator DAILEY, L. A
KLEEMANN, E
WITTMAR, M
GESSLER, T
SCHMEHL, T
ROBERTS, C
SEEGER, W
KISSEL, T
description This study describes the development of surfactant-free, biodegradable nanoparticle systems with varying physicochemical properties and their suitability for pulmonary application via nebulization. Nanoparticle suspensions were formulated from the branched polyester, diethylaminopropyl amine-poly(vinyl alcohol)-grafted-poly(lactide-co-glycolide) (DEAPA-PVAL-g-PLGA) alone, as well as with increasing amounts of carboxymethyl cellulose (CMC). Particle size, zeta potential, turbidity, and morphology (atomic force microscopy) were characterized. Three formulations were chosen for further study: Cationic nanoparticles without CMC, cationic nanoparticles with CMC, and anionic nanoparticles with an excess of CMC. Nanoparticle degradation was characterized, as well as stability during nebulization. Nanoparticle-cell interactions were investigated and quantified using confocal laser scanning microscopy and fluorescence spectrometry. Nanoparticles ranged in size from 70-250 nm and displayed zeta potentials of +58.9 to -46.6 mV. Anionic nanoparticles showed the highest stability during nebulization. The degradation rate of each nanoparticle formulation decreased with increasing amounts of CMC. Cell association was highest among cationic nanoparticles (57% and 30%, respectively), although these were not internalized. Despite a lower rate of cell association (3%), anionic nanoparticles were internalized by A549 cells. Surfactant-free nanoparticles from DEAPA-PVAL-g-PLGA are versatile drug delivery systems; however, only the anionic formulations investigated were proven suitable for aerosol therapy.
doi_str_mv 10.1023/B:PHAM.0000008051.94834.10
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A</au><au>KLEEMANN, E</au><au>WITTMAR, M</au><au>GESSLER, T</au><au>SCHMEHL, T</au><au>ROBERTS, C</au><au>SEEGER, W</au><au>KISSEL, T</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Surfactant-free, biodegradable nanoparticles for aerosol therapy based on the branched polyesters, DEAPA-PVAL-g-PLGA</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>2003-12-01</date><risdate>2003</risdate><volume>20</volume><issue>12</issue><spage>2011</spage><epage>2020</epage><pages>2011-2020</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>This study describes the development of surfactant-free, biodegradable nanoparticle systems with varying physicochemical properties and their suitability for pulmonary application via nebulization. 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The degradation rate of each nanoparticle formulation decreased with increasing amounts of CMC. Cell association was highest among cationic nanoparticles (57% and 30%, respectively), although these were not internalized. Despite a lower rate of cell association (3%), anionic nanoparticles were internalized by A549 cells. Surfactant-free nanoparticles from DEAPA-PVAL-g-PLGA are versatile drug delivery systems; however, only the anionic formulations investigated were proven suitable for aerosol therapy.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>14725368</pmid><doi>10.1023/B:PHAM.0000008051.94834.10</doi><tpages>10</tpages></addata></record>
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source MEDLINE; SpringerLink Journals
subjects Aerosols
Alcohol
Biodegradation
Biological and medical sciences
Biotransformation
Carboxymethylcellulose Sodium
Cellulose
Chemistry, Pharmaceutical
Drug Delivery Systems
Drug Stability
General pharmacology
Lactic Acid - chemistry
Medical sciences
Microscopy
Microscopy, Atomic Force
Microscopy, Confocal
Microspheres
Nanoparticles
Nephelometry and Turbidimetry
Particle Size
Pharmaceutic Aids
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyesters - chemistry
Polyglactin 910 - analogs & derivatives
Polyglactin 910 - chemistry
Polyglycolic Acid - chemistry
Polylactic Acid-Polyglycolic Acid Copolymer
Polymers - chemistry
Polyvinyl Alcohol - chemistry
Scientific imaging
Spectrometry, Fluorescence
Surfactants
Suspensions
Toxicity
title Surfactant-free, biodegradable nanoparticles for aerosol therapy based on the branched polyesters, DEAPA-PVAL-g-PLGA
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