Liposome-Based Drug Delivery Systems

499 Pages·2021·12.783 MB·English

by  Wan-Liang Lu, Xian-Rong Qi

Biomaterial Engineering
Series Editor: Youqing Shen
Wan-Liang Lu
Xian-Rong Qi
Editors
Liposome-Based
Drug Delivery
Systems
Biomaterial Engineering
SeriesEditor
YouqingShen
CollegeofChemicalandBiologicalEngineering
ZhejiangUniversity
Hangzhou,China
Theuseofhumanbodycompatiblematerialsformedicaldiagnosis,treatment,and
surgery is always critical in enhancing life-saving therapies and quality of life of
patients. With the massive research efforts in this field in both universities and
industries, there is a continuous growth in our knowledge/technique in design and
useofsuchbiomaterialstoeffectivelydeliverspecifictherapeutics,includingDNA,
protein, and contrast reagents, to the targeted cells and organs for treatment or
diagnosis; to repair or replace tissues; or even to construct artificial organs like
cartilages, bones, and skins to regain the body functions. The inherent interdisci-
plinarynatureofbiomaterialsmakesresearchersoftenusemethodstoprepareawide
range of materialsand various bioassays to evaluatetheir diverse bio-related prop-
erties. However, it is generally very difficult to find and tell reliable sources and
detailed know-how for the needed methods and protocols, which are buried in the
vastliteratureandonlydescribedingenerallackofdetails.Onestillhastofindthe
bestbytrialanderror.
The aim of this series is to provide a complete reference for researchers, engi-
neers, and graduate students who are engaged in R&D of biomaterials. It provides
newcomers the fundamental concepts and overall status of the areas they work on
and provides researchers comprehensive, in-depth, and authoritative information
including preparation/fabrication protocols of most biomaterials and bioassay pro-
tocolsaswellasawidevarietyofadvancedexperimentalmethodsusedinpractice,
numerousexamples,andpracticalapplications.
Moreinformationaboutthisseriesathttp://www.springer.com/series/13484
(cid:129)
Wan-Liang Lu Xian-Rong Qi
Editors
Liposome-Based Drug
Delivery Systems
With158Figuresand17Tables
Editors
Wan-LiangLu Xian-RongQi
BeijingKeyLaboratoryofMolecular DepartmentofPharmaceutics
PharmaceuticsandNewDrugSystem SchoolofPharmaceuticalScience
Beijing,China PekingUniversity
Beijing,China
BeijingKeyLaboratoryofMolecular
PharmaceuticsandNewDrugSystem
Beijing,China
ISSN2523-8809 ISSN2523-8817(electronic)
ISBN978-3-662-49318-2 ISBN978-3-662-49320-5(eBook)
ISBN978-3-662-49319-9(printandelectronicbundle)
https://doi.org/10.1007/978-3-662-49320-5
©Springer-VerlagGmbHGermany,partofSpringerNature2021
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Series Preface
Theuseofhumanbodycompatiblematerialsformedicaldiagnosis,treatment,and
surgery is always critical in enhancing life-saving therapies and quality of life of
patients. With the massive research efforts in this field in both universities and
industries, there is a continuous growth in our knowledge/technique in design and
useofsuchbiomaterialstoeffectivelydeliverspecifictherapeutics,includingDNA,
protein, and contrast reagents, to the targeted cells and organs for treatment or
diagnosis; to repair or replace tissues; or even to construct artificial organs like
cartilages, bones, and skins to regain the body functions. The inherent interdisci-
plinarynatureofbiomaterialsmakesresearchersoftenusemethodstoprepareawide
range of materialsand various bioassays to evaluatetheir diverse bio-related prop-
erties. However, it is generally very difficult to find and tell reliable sources and
detailed know-how for the needed methods and protocols, which are buried in the
vastliteratureandonlydescribedingenerallackofdetails.Onestillhastofindthe
bestbytrialanderror.
The aim of this series is to provide a complete reference for researchers, engi-
neers, and graduate students who are engaged in R&D of biomaterials. It provides
newcomers the fundamental concepts and overall status of the areas they work on
and provides researchers comprehensive, in-depth, and authoritative information
including preparation/fabrication protocols of most biomaterials and bioassay pro-
tocolsaswellasawidevarietyofadvancedexperimentalmethodsusedinpractice,
numerousexamples,andpracticalapplications.
This reference work, tentatively composed of 10 volumes, covers the most
popular topics of biomaterials, from drug delivery to gene and protein delivery,
from biomedical biodetection to diagnosis, from cardiovascular diseases to tissue
engineering.Thecontentiscreatedbyleadingscientistsineachfieldandwillevolve
constantly,thusitpresentsbothhigh-qualityandup-to-datescientificandtechnical
information.
June,2021 YouqingShen
v
Volume Preface
Liposomes are the sealed vesicles that are generally formed by phospholipids,
cholesterol, and other materials. Liposomes are not only a convenient platform for
studyingmembranekineticsanddrugorbiomoleculetransport,butalsoapotential
drugdeliverycarriersystem.Liposomeshaveauniqueroleinovercomingbiological
barriers and carrying biological drugs. As a drug carrier, liposomes have a broad
prospect in basic research and clinical application, such as delivering anticancer
agents,anti-parasitedrugs,hormones,andgenes.
This volume mainly describes the protocols for fabrication of liposomal drug
delivery system, and consists of two parts. The first part emphasizes the basic
protocols and concepts for fabrication of drug-loaded liposomes. For new investi-
gators, laying the groundwork is the first step. This part focuses on the fabrication
detailsinliposomesformulations,whicharetheso-calledsmalltrickswhileusually
notdisclosedinmostpublishedresearcharticles.However,theseprocessingdetails
are crucial for the preparation of liposomes. And the second part focuses on the
strategies in modified and/or functionalized liposomes to adapt to pathophysiolog-
icalenvironment,aswellastheirapplicationintreatingdiseases.Asnewanalytical
andsynthetictechnologiesbecomeavailable,andimprovedunderstandingofpath-
ophysiology,variousfunctionalizeddrugliposomesaredevelopedtofittherequire-
ments of different therapeutic purposes, exhibiting a broad range of applications.
Accordingly,theobjectivesofthispartareaimedatdeeplyunearthingtheformula-
tion of drug-loaded liposomes, describing the detailed operation of liposomal for-
mulation, and further demonstrating their potential applications. Therefore, this
volume shows the features of experimental report or protocol for proving a guide
to scientists, research students, and young investigators in pharmaceutical
enterprises.
Editorialmembersofthisvolumeinvolverenownedexpertsandyoungscholars
in the research field of liposomes, and some graduate students who have research
experience in liposomes field also participate in the editing work. They are mainly
fromPekingUniversity,FudanUniversity,SichuanUniversity,ChinaPharmaceuti-
calUniversity,ShenyangPharmaceuticalUniversity,SecondMilitaryMedicalUni-
versity, Hebei Medical University, Beijing Institute of Petrochemical Technology,
Shihezi University, Liaoning University of Traditional Chinese Medicine, Shanxi
UniversityofTraditionalChineseMedicine,JilinMedicalUniversity,Universityof
vii
viii VolumePreface
North Carolina at Chapel Hill, University of Nebraska Medical Center, and Chap-
manUniversity,aswellastheiraffiliatedhospitals.
This volume is included in the reference series – Biomaterial Engineering,
proposed by Prof. Youqing Shen. The volume is expected to be used by graduate
students,postdoctoralresearchers,andresearchersusinglipid-basedsystemsinthe
fields of drug delivery, physical chemistry, and cellular and molecular biology. We
aregratefultoalltheauthorsfortheircontributions.Wearealsoverygratefultothe
serieseditor,Dr.JubyGeorge,andtheoutstandingstaffatSpringerNaturefortheir
support,help,andencouragement.
SchoolofPharmaceuticalSciences Wan-LiangLu
PekingUniversity Xian-RongQi
June,2021
Contents
PartI GeneralProtocolsforFabricationofDrugLiposomes ...... 1
1 LiposomesinDrugDelivery:StatusandAdvances ............ 3
Ying-JieHu,Rui-JunJu,FanZeng,Xian-RongQi,andWan-LiangLu
2 PreparationofDrugLiposomesbyThin-FilmHydrationand
Homogenization ....................................... 25
BaiXiangandDe-YingCao
3 PreparationofDrugLiposomesbyReverse-PhaseEvaporation ... 37
Nian-QiuShiandXian-RongQi
4 PreparationandCharacterizationofDrugLiposomesby
pH-GradientMethod .................................... 47
Nian-QiuShi,Xian-RongQi,andBaiXiang
5 PreparationandCharacterizationofDrugLiposomesby
AmmoniumSulfateGradient ............................. 59
Rui-JunJuandXue-TaoLi
6 PreparationofDrugLiposomesbyEDTAGradientMethods .... 79
YanzhiSongandYihuiDeng
7 Lipid-CoatedCisplatinNanoparticlesforInsoluble
DrugLoading ......................................... 97
YangLiuandLeafHuang
8 PurificationMethodofDrug-LoadedLiposome ............... 111
MengLinandXian-RongQi
9 QualityEvaluationofDrug-LoadedLiposomes ............... 123
MengLin,RudongWang,andXian-RongQi
ix
x Contents
PartII FunctionalizedLiposome-BasedDrugDeliverySystems
andPotentialApplication .................................. 141
10 CouplingMethodsofAntibodiesandLigandsforLiposomes .... 143
MingChen,Qiu-RanMa,andWan-LiangLu
11 PreparationandEvaluationofFolateReceptorMediated
TargetingLiposomes .................................... 167
WeiGao
12 PreparationofCellPenetratingPeptides-MediatedTargeting
DrugLiposomes ....................................... 179
YangWangandQinHe
13 PreparationofMultifunctionalPaclitaxelLiposomesfor
TreatmentofBrainGlioma ............................... 193
Xiu-YingLi
14 PreparationandEvaluationofIntegrinReceptor-Mediated
TargetingDrugLiposomes ............................... 213
FeiWang,GangWei,andWeiyueLu
15 PreparationofFunctionalVincristineLiposomesforTreatment
ofInvasiveBreastCancer ................................ 239
FanZeng
16 PreparationandCharacterizationofDNALiposomesVaccine ... 259
Ya-FeiDu,MingChen,Jia-RuiXu,QianLuo,andWan-LiangLu
17 PreparationandEvaluationofBiomineral-BindingAntibiotic
Liposomes ............................................ 277
Xin-MingLiu,KeRen,GeoffreyWu,andDongWang
18 Dual-ModifiedsiRNA-LoadedLiposomesforProstateCancer
Therapy .............................................. 293
BaiXiangandDe-YingCao
19 FabricationandEvaluationofDualPeptides-ModifiedLiposomes
CoencapsulatingsiRNAandDocetaxel ...................... 309
ZhenzhenYangandBaiXiang
20 PreparationandEvaluationofRivastigmineLiposomesfor
IntranasalDelivery ..................................... 325
ZhenzhenYang
21 Dequalinium-MediatedMitochondria-TargetingDrugLiposomes
fortheTreatmentofDrug-ResistantLungCancer ............ 345
XueYing