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Nano Physical Pharmaceutics of Micelle-Based Systems
copolymers. Cui et al. have synthesized a high-molecular polymer
mPEG-S-S-C16 with redox properties and used it to load the
chemotherapy drug DOX. In vitro experiments show that under
disintegrated, and the wrapped DOX can be quickly released, and
2.5.6.3 Temperature-responsive micelles
Temperature is one of the most common sources of stimulation.
Temperature-responsive polymeric micelles are assembled from
copolymers with temperature-responsive blocks, where the
aqueous properties of such copolymers change drastically at a
certain temperature and the corresponding micelles release the
drug through phase inversion. The temperature at which
the transition occurs is referred to as lower critical solution
temperature (LCST) or upper critical solution temperature (UCST)
of the polymer. When the temperature is below LCST or above
UCST, hydrogen bonds are formed between polymer and water and
dissolve. When the temperature is above LCST or below UCST, the
hydrogen bonds between water and polymer chains are broken
and polymer precipitates. Currently, the most widely used
temperature-responsive polymer is PNIPAAm when LCST is
around 32 °C. In addition, Pluronics and P(HPMAm-Lacn) are
thermo-responsive poly(N-isopropylacrylamide-b-lauryl acrylate)
(PNIPAAm-b-PLA) with tailored molecular weight through
reversible addition-fragmentation chain-transfer (RAFT)
polymerization to prepare drug-loaded smart micelle. The micelle
experienced phase transition when the temperature rise up above
the LCST and showed a sustained drug release rate [54].
2.5.6.4 Photo-responsive micelles
Photo-responsive micelles usually undergo structural
mainly through photo-induced transition of hydrophobicity–
hydrophilicity or photo-cleavage reaction [55, 56]. Photochromic
moieties such as coumarin, azobenzene, spiropyran, and 2-diazo-
Summary and Perspective
85
1,2-naphthoquinone are commonly introduced to construct
photo-responsive block polymers. For example, The conformation
of azobenzene groups and its derivatives changes from the
apolar trans form to the polar cis form upon light irradiation
(340–380 nm), then reforms to the orginal state after being
exposed to irradiation at 420–490 nm or put into the dark.
Compared with the cis-azo bond (dipole moment, μ = 3D), the
trans-azo bond has a smaller polarity (dipole moment, μ = 0D)
and stronger hydrophobicity, which may be utilized to control the
assembly and disruption of azo-containing polymeric micelles in
repeated cycles and facilitate drug release. Spiropyran is another
promising photoisomerization group which can exist in two
states, the hydrophilic zwitterionic merocyanine state and the
hydrophobic SP state. These two states can transform into each
other through a reversible isomerization either upon visible
light (620 nm) irradiation (from hydrophilic to hydrophobic) or
the UV (365 nm) irradiation (from hydrophobic to hydrophilic).
Block copolymer with spiropyran showed improved light
hydrophilic and hydrophobic state compared with azo moieties.
2.6 Summary and Perspective
Polymeric micelles have shown various advantages as nanocarriers
for drug delivery. They can realize the solubilization of waterinsoluble drugs through hydrophobic interactions, and achieve
enrichment in tumor tissues through enhanced permeability
in vitro and in
vivo environments, and the complex composition of our internal
environment (e.g., blood) encountered in practical applications,
there are multiple interactions between micelles and biological
macromolecules, which makes the precise and rational design
of micelles a great challenge. At the same time, the special
pathological conditions of tumor microenvironment have stricter
requirements on the targeting and nanomedicine. Only when our
understanding of disease physiology is matched by advances in
86
Nano Physical Pharmaceutics of Micelle-Based Systems
materials science, will it be possible to achieve larger breakthroughs
This chapter attempts to link the physical and chemical
parameters of micelles with interactions in vivo, for example, how
to regulate the particle size and zeta potential of the corresponding
the chemical structure of amphiphilic polymers. It aims to provide
theoretical basis and guidance for the precise design of micelles to
for tumors.
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Chapter 3
Nano Physical Pharmaceutics of
Liposome-Based System
Nian Huang,
a
Mengxin Zhao,a Jian Wang,b and Wei Li
a
a
Department of Nanomedicine, Naval Medical University,
Shanghai 200433, China
National Advanced Medical Engineering Research Center,
Shanghai 201203, China
liwei_dds@163.com
3.1 Classification of Liposome
Nano Physical Pharmaceutics
Edited by Wei Li
Copyright © 2025 Jenny Stanford Publishing Pte. Ltd.
ISBN 978-981-4968-52-2 (Hardcover), 978-1-003-51393-3 (eBook)
www.jennystanford.com
92
Nano Physical Pharmaceutics of Liposome-Based System
Figure 3.1 Schemac diagram of the structures of liposomes with dierent
structures.
3.2 Preparation of Liposomes
3.2.1 Thin-Film Hydraon Method
I
Preparation of Liposomes
93
3.2.2 Reverse-Phase Evaporation Method
3.2.3 Injection Method