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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5907_Библиотеки_им_академика_М_И_Перельмана.pdf
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Nano Physical Pharmaceucs of Microsphere Delivery System
drug-carrying microspheres with high embedding rate and
high drug activity. Using a nearly monodisperse high molar
mass poly(N-isopropylacrylamide) (PNIPAM) sample, Wu et
al. successfully changed the conformation of a single PNIPAM
chain from curl to a fully collapsed stable single-chain globule in
extremely dilute aqueous solution, which enabled us to study
the transition from globule to curl of a single homopolymer chain
later study of the stability of microspheres in solution. Qi et al. [64]
prepared uniform-sized PLGA microspheres by Shirasu porous
exenatide, a drug for treating Type 2 diabetes. The experimental
results showed that the hypoglycemic rate of the exenatide
blood glucose returned to the level of the control group (normal
saline group) after the 14th day of drug administration was
took thymosin as the model drug,
optimized the concentration of internal aqueous phase, oil phase
aqueous phase pH, and prepared thymosin loaded microspheres
with an average particle size of 24 µm and uniform particle size
combined with solvent evaporation method, and the embedding
investigated. The results showed that with the increase of
the molecular weight of PLGA, the burst rate of microspheres
decreased, and the whole release process was closer to zeroorder release. And because the preparation process of membrane
Protein drug sustained-release microspheres. Protein drugs
have high molecular weight, complex structure, easy denaturation
and inactivation under severe preparation conditions, and poor
can solve this problem. Zhang et al. [66] used insulin as a model
NPP of Microspheres
225
curing process. The oral calcium alginate chitosan microspheres
can mildly prepare lotion with uniform size, so as to retain the
gastrointestinal tract. In the experiment of diabetes rats, the
prepared insulin-loaded oral microspheres have a continuous
Small molecule drug sustained-release microspheres.
easy to escape quickly during the preparation of microspheres
due to their small molecular weight, which leads to a decrease
in the entrapment rate. To solve this problem, the researchers
obtained emulsion droplets with uniform particle size through
ripening in the curing process, and ensuring high embedding rate
(RVC) as the model drug and prepared a uniform drug-loaded
terminal groups (hydroxyl, carboxyl, ester) on drug loading were
investigated on a controlled basis. The hydroxyl-terminated
ropivacaine microspheres exhibit the best long-term analgesic
6.4.5.2 Application of uniform drug-loaded microspheres in
vaccine preparation
application and charge. The aspect of protection and avoidance
extent of the manufacturing of antibody responses are intently
linked to mode of application. Biodegradable delivery technology
for vaccines which are administered by the intravenous path
may resolve the shortcomings of the same conventional vaccines.
226
Nano Physical Pharmaceucs of Microsphere Delivery System
technology. The water phase is an antigen solution and the
lotion preparations with uniform particle size have a stronger
immune response than preparations with wide particle size
distribution.
6.4.5.3 Application of uniform drug-loaded microspheres in
the treatment of malignant tumors
and bioavailability in the human body. Therefore, large doses
are required to increase the probability of reaching the tumor
site, as shown in Fig. 6.6. Based on the enhanced capability
passively targeted. Therefore, nanosphere (NP) preparations are
double emulsion method combined with rapid membrane
homogeneous chitosan nanospheres (CNPs) with a particle size
technology, and realized co-encapsulation of doxorubicin (DOX),
PTX and Fe3O4 nanocrystals by combining O/W/O double
The CNPs with uniform particle size are loaded with hydrophobic
taxol, doxorubicin and iron oxide nanocrystals Fe3O4 at the same
3O4 and
killing role. The actual results showed that the three-week
which was far higher than other control groups, showing a good
nanospheres was used to introduce a polyethylene glycol
Summary and Perspective
227
targeting tumor cells to prepare a paclitaxel nano drug delivery
carrier (RGDPEG-CNP: PTX) with both stealth and targeting
capabilities. The experimental results show that the drug delivery
preparation with uniform size nanospheres can improve the
Figure 6.6 Schematic of the general in vivo fate of the microsphere from
injection site to tumor.
6.5 Summary and Perspective
as changes in the living environment, the aging society, the
development of medicine, cognitive concepts and so on, the disease
tumors, cardiovascular diseases, diabetes and mental diseases have
increased rapidly, which will greatly increase the consumption
of medical resources. Microspheres have the advantages of
demand will be on the rise.
One of the important directions for the development of drug
dosage forms is to improve the targeting of drugs. At present,
there are new and gratifying achievements in the research of drug
microspheres targeting, such as nano-microspheres, magnetic
228
Nano Physical Pharmaceucs of Microsphere Delivery System
microspheres, bioadhesion microspheres and antibody-mediated
microspheres. Nano-microspheres are easier to pass through
the gastric mucosa, intestinal mucosa, nasal mucosa and even the
being paid to them at present. The magnetic microspheres
prepared by magnetic properties have magnetic responsiveness,
Bioadhesive microspheres prepared by using adhesive materials
such as deacetylated chitosan and polycarboxyethylene can
improve the absorption of drugs at the biological mucosa.
Absorption accelerators such as microspheres co-carrier
lysophospholipid or protease inhibitors are used to improve the
of antigen-antibody is used to prepare antibody microspheres,
which can improve the targeting of drugs. In addition, the
development and application of new natural polymer materials
progress of microsphere preparations and provides corresponding
theoretical guidance and basis for related work in the future.
Hopefully, with a deeper understanding of microspheres, new
approaches will be developed to conquer the obstacles in the
preparation and application process.
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222
226
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see
see