Polymeric Drug Delivery II. Polymeric Matrices and Drug Particle Engineering

381 Pages·2006·39.429 MB·English

by  Sönke Svenson (Eds.)

Polymeric Drug Delivery II
g 01
orw0
pubs.acs.6-0924.f
http://k-200
2 | 1/b
12
00
21
uly 6, oi: 10.
6 on J06 | d
30
12
9.163.34.March 9,
by 8ate:
d D
nloadecation
DowPubli

In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
g 01
orw0
pubs.acs.6-0924.f
http://k-200
2 | 1/b
12
00
21
uly 6, oi: 10.
6 on J06 | d
30
12
9.163.34.March 9,
by 8ate:
d D
nloadecation
DowPubli

In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
ACS SYMPOSIUM SERIES 924
Polymeric Drug Delivery II
Polymeric Matrices and Drug
g 01
orw0
pubs.acs.6-0924.f Particle Engineering
http://k-200
2 | 1/b
12
00
21
uly 6, oi: 10. Sönke Svenson, Editor
6 on J06 | d Dendritic Nano Technologies, Inc.
30
12
9.163.34.March 9,
by 8ate:
d D
nloadecation
DowPubli Sponsored by the

ACS Division of Polymeric Materials: Science and
Engineering, Inc.
American Chemical Society, Washington, DC
In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
Library of Congress Cataloging-in-Publication Data
Polymeric drug delivery / Sönke Svenson, editor; sponsored by the ACS Division of
Polymeric Materials; Science and Engineering, Inc.
p. cm.—(ACS symposium series; v. 923-)
"Developed from a symposium sponsored by the Division of Polymeric Materials:
Science and Engineering, Inc., at the 226th National Meeting of the American
Chemical Society, New York, September 7-11, 2003"-—T.p. verso.
g 01 Includes bibliographical references and indexes.
orw0
pubs.acs.6-0924.f CISoBnNte n1t3s:: 9v.7 81-. 0P-a8rt4ic1u2l-a3te9 1d8ru-g0 c(aalrkri.e prsa per)
http://k-200 I. Polymeric drug delivery systems—Congresses. 2. Polymeric drugs—Congresses.
2 | 1/b I. Svenson, Sönke, 1956- II. American Chemical Society. Division of Polymeric
0102 Materials: Science and Engineering, Inc. III. American Chemical Society. Meeting
21
uly 6, oi: 10. RS(220216 thP: 6250P0634 :1 N2 ew2 Y00or5k , N.Y.) IV. Series.
6 on J06 | d 615'.3—dc22 2005053686
30
9.163.34.1March 9, 2 TCfohorep I ynprfaoipgremhrta ut©isoe n2d 0 Si0nci6 etnh Acisems p—eurPbicleiacrnamt iCaonhnee nmmceeiec otasfl PSthaoepc emirei tnfyoim r uPrmin treedqu Liriebmraernyt sM oaft Aermiaelsr,i cAaNn SNIa Ztio3n9a.4l 8S-t1a9n8d4ar. d
by 8ate: Distributed by Oxford University Press
d D
nloadecation This volume: ISBN 13: 978-0-8412-3976-0 ISBN 10: 0-8412-3976-2
DowPubli All Rights Reserved. Reprographic copying beyond that permitted by Sections 107 or 108 of the
U.S. Copyright Act is allowed for internal use only, provided that a per-chapter fee of $33.00 plus
$0.75 per page is paid to the Copyright Clearance Center, Inc., 222 Rosewood Drive, Danvers, MA
01923, USA. Republication or reproduction for sale of pages in this book is permitted only under
license from ACS. Direct these and other permission requests to ACS Copyright Office, Publications
Division, 1155 16th Street, N.W., Washington, DC 20036.
The citation of trade names and/or names of manufacturers in this publication is not to be construed
as an endorsement or as approval by ACS of the commercial products or services referenced herein;
nor should the mere reference herein to any drawing, specification, chemical process, or other data
be regarded as a license or as a conveyance of any right or permission to the holder, reader, or any
other person or corporation, to manufacture, reproduce, use, or sell any patented invention or
copyrighted work that may in any way be related thereto. Registered names, trademarks, etc., used in
this publication, even without specific indication thereof, are not to be considered unprotected by
law.
PRINTED IN THE UNITED STATES OF AMERICA
In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
Foreword
The ACS Symposium Series was first published in 1974 to pro­
vide a mechanism for publishing symposia quickly in book form. The
purpose of the series is to publish timely, comprehensive books devel­
oped from ACS sponsored symposia based on current scientific re­
search. Occasionally, books are developed from symposia sponsored by
g 01 other organizations when the topic is of keen interest to the chemistry
pubs.acs.or6-0924.fw0 taeundtise nisc erB.e evfioerwe eadg froere ianpgp troo ppruiabtlei sahn ad bcooomkp, rtehhee npsriovpeo sceodv etraabglee oafn dc ofno­r
http://k-200 interest to the audience. Some papers may be excluded to better focus
2 | 1/b the book; others may be added to provide comprehensiveness. When
12
00 appropriate, overview or introductory chapters are added. Drafts of
21
6 on July 6, 06 | doi: 10. mchaanputsecrsrA ipastr se a a prreeu elprer-,e repovanirleyewd oeirdni gcpiarnmiaole rr rateo-sr eefaainrdcaylh fapocarcmpeeparttas. nacne d oor rriegjiencatl iorne,v iaenwd
30
9.163.34.1March 9, 2 poaupsleyr sp uabrel isihnecdlu pdaepde irns athree nvoot luamcceesp. teVde. rbatim reproductions of previ­
by 8ate:
nloaded cation D ACS Books Department
DowPubli

In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
Preface
Achieving the therapeutic drug concentration at the desired location
within a body during the required length of time without causing local
over-concentrations and their adverse side effects is the main challenge
g 01 in the development of a successful drug delivery system. Key factors to
s.acs.or924.pr0 btoex cicointys idfeorre d tihna tt hims aetftfeorr)t, artea rdgreutgin bgi, oaavnadi labdirluigty-,r eblieoacseo mpparotifbiliel.i ty T(hoer
b0
pu6- bioavailability of class II and HI drugs (by the Biopharmaceutical
p://200 Classification System of Drugs) is challenged by their poor water
2 | htt1/bk- solubility and poor membrane permeability, respectively. Poor water
12
00 solubility results in the rejection of about 40% of newly developed drugs
21
July 6, doi: 10. beyx htihbeit Pshuabrompaticmeualt icpaelr fIonrdmuasntrcye, wduhei le toa btohuist 2c0h%al leonf gme. arSktertaetde gidesru gtso
4.136 on 9, 2006 | loivpeorscoommees ,t h(isp oplryombleermic )i nmcliucdeel ltehse, udseen dofr ipmaertrisc, uleamr udlrsuigo nc ardrrioeprsl estus,c ha ansd
3.3ch engineered micro- and nanoparticles. These carriers encapsulate a drug,
9.16Mar this way enhancing their water solubility (bioavailability) and reducing
ed by 8n Date: ttrhaenirs potortx icdirtyu gs( entoh anthcee d debsiiorceod mlpoactaibtiiolnit yb)y. Ine itahdedr itpioanss, ivcea rrtiaerrgs etcinagn
do
DownloaPublicati t(hernohuagnhc eldi gpaenrdms ethaabti liintyte arancdt rwetiethn trioecne, pEtoPrRs, tehfafte catr)e oor vbeyr eaxcptirvees steadr gaett itnhge
surface of tumor cells. Alternatively, problem drugs can be encapsulated
into depot matrices, whose release profile, defined by diffusion and
matrix degradation, determines the concentration level of the free drug.
The third strategy does not employ auxiliaries such as carriers or
matrices but focuses on particle engineering. For example, reducing the
size of a drug particle will increase its surface area and enhance its
solubilization rate. All three strategies are explored in university
laboratories as well as by the Pharmaceutical Industry.
Thus the main motivation for organizing the Polymeric Drug
xi.
In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
Delivery: Science and Application symposium during the 226th National
Meeting of the American Chemical Society (ACS) in New York, New
York, in September 2003, was to provide a forum for both communities,
academia and industry, to discuss progress in these three strategic
approaches. Seventy-five well-recognized international experts, equally
representing both communities, had been invited to present their
research being conducted in the United States (57), the United Kingdom
(4), Canada (3), Germany (3), France (3), the Netherlands (3), Italy (1)
and Spain (1). Highlights from this symposium are presented in two
volumes within the ACS Symposium Series: Polymeric Drug Delivery
I:Particulate Drug Carriers (ACS Symposium Series 923) and
Polymeric Drug Delivery ILPolymeric Matrices and Drug Particle
Engineering (ACS Symposium Series 924). To provide an even broader
g 01
s.acs.or924.pr0 oinvcelruvdieedw ,i n tthweo bocooknst.r ibutions from Japanese researchers have been
b0
pu6- The 44 chapters selected for publication within the Symposium
p://200 Series are divided into three main sections. Following an overview, the
2 | htt1/bk- first section describes in twenty chapters the use of carriers such as
12
00 liposomes, micelles, dendrimers, emulsion droplets, nanoparticles, and
21
July 6, doi: 10. yoergaastn icce lmlso ilne cthuel e(st,a rmgaecterdo)m doelelicvuelreys osfu pcoh oarsly pwroatteeirn-ss oalunbdl en udcrulegisc, asmciadlsl,
on 6 | and metal ions for molecular imaging purposes. Different routes of
4.136 9, 200 application are described, including oral and transepithelial delivery
3.3ch (Volume I).
9.16Mar The second section, with 13 chapters, is devoted to the use of
ed by 8n Date: phoydlyrmogeerlisc, amnadt rmiciellsi. roTdhse i n agpepnlei caantdi odnr uogf dpeolilvyemrye,r ass owluetlli otnhes, prneadniocgtieolns,
do
DownloaPublicati ofrfo dmr utga bsloeltusb biyli tFy oinu rpioelry-Tmrearnics fmoramtr iicnefsr,a trheed iin m saigtuin sgt,u adnyd oaf ndtirmugi crreolebaiasle
release coatings are presented.
The third section details in nine chapters the use of supercritical
fluids, controlled precipitation processes, and application of excipients
in particle engineering and size control. The final chapter describes the
preparation of fast dissolving tablets, another approach to increase the
availability of drugs. These two sections, supplemented by an overview
of the topics, are presented in Volume II.
These books are intended for readers in the chemical and
pharmaceutical industry and academia who are interested or involved in
drug delivery research as well as for advanced students who are
interested in this active and rapidly developing research area.
xii
In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
I am using this opportunity to congratulate three presenters at the
symposium and coauthors of this book, whose contributions received
special recognition during the ACS National Meeting. Dr. Theresa
Reineke and her co-worker Yemin Liu (University of Cincinnati),
received the Arthur K. Doolittle Award for Fall 2003 for the best paper
presented at the ACS Division of Polymeric Materials: Science and
Engineering, Inc., (PMSE) meeting for their presentation on "Synthesis
and Characterization of Polyhydroxyamides for DNA Delivery". Dr.
Brian Johnson (Princeton University), received the 2003 ICI Student
Award in Applied Polymer Science for his presentation on
"Nanoprecipitation of Organic Actives Using Mixing and Block
Copolymer Stabilization".
I deeply appreciate the willingness of the authors to contribute to
g 01
s.acs.or924.pr0 tahpips reicmiaptoer ttahnet hoevlpe rovfi mewa noyf rdersuega rcdheelrisv, erwyh toe chhanvoe ldoegvieost.e dI tahlesior tgimreea ttloy
pub6-0 this project by reviewing these contributions, ensuring clarity and
p://200 technical accuracy of the manuscripts. I thank the PMSE for the
2 | htt1/bk- opportunity to hold the symposium as a part of their program and
12 especially Ms. Eileen Ernst, the PMSE Administrative Assistant and
00
21
uly 6, oi: 10. "aFbslotrraecntcse aNndi gphrteinpgrianltes" tion tom eth, ef osr yhseter mi.n vI aalupapbrelec ihaetelp thwei thp aptileanccine g aanlld
Jd
on 6 | support of the ACS Symposium Series acquisitions and production team
4.136 9, 200 during the production of these books.
3.3ch Last but not least I thank the ACS Corporation Associates (CA) as
9.16Mar the "gold sponsor"; The Dow Chemical Company as the "silver
ed by 8n Date: Psphoanrmsoarc"e; utaincda lsE, lIannc .;N JaonhonSsyons teamnds ;J oEhpnisco nT, hCeernapteeru ftoicr sB, ioInmc.a;t eGriuailslf aonrdd
do
DownloaPublicati Aspdovnasnocresd" foTre tchheniro lfoingaiensc;i ala nsdu ppTohrat r ofT ethceh nsoylmogpioessi, umIn. cI.t waso ul"db rhoanvzee
been impossible to assemble this outstanding group of researchers
without these contributions.
Sönke Svenson
Dendritic NanoTechnologies, Inc.
2625 Denison Drive
Mount Pleasant, MI 48858
[phone] (telephone)
[phone] (fax)
[email protected] (email)
xiii
In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.
g 01
s.acs.or924.pr0
b0
pu6-
p://200
2 | htt1/bk-
12
00
21
uly 6, oi: 10.
Jd
on 6 |
4.136 9, 200
3.3ch
9.16Mar
ed by 8n Date:
do
DownloaPublicati

In Polymeric Drug Delivery II; Svenson, S.;
ACS Symposium Series; American Chemical Society: Washington, DC, 2006.