various applications of nanoparticles as drug delivery systems

1. Nanotechnology based drug
delivery
By: Abeer abd- elrahman
B.SC of pharmacy

2. • Nano medicine had viewed
countless breakthroughs in drug
delivery implementations.
• Nanoparticles are defined as
particulate distribution or solid
particles with a size in the range
of 10-100 nm.
• Controlled nano drug delivery
seeks the development of
suitable drug carriers that can
transmit a sufficient dose of drug
to diseased lesions.

3. • Various nanostructures including liposomes,
polymers, dendrimers, micelles and magnetic
nanoparticles have been tested as carriers in
drug delivery.

4. • Nanoparticles can be prepared from different
types of materials such as proteins,
polysaccharides and synthetic polymers
• The selection of matrix depends on many
factors including requisite size of
nanoparticles, underlying properties of the
drug such as solubility, stability, surface
characteristics (charge and permeability),
degree of biodegradability, biocompatibility
and toxicity, drug delivery profile desired,
antigenicity of the final product.

5. • To overcome the limitations and drawbacks of
conventional drug administration like limited
effectiveness, poor biodistribution, toxicity
and lack of sensitivity, controlled drug delivery
system is utilized.
• In controlled drug delivery systems, the drug is
transported at the place of action, increasing
its influence on the vital tissues and
minimizing its undesirable side effects.

6. Figure showing aspects of controlled drug delivery applications

7. • The poor solubility of drug is a major problem
which limits the development of highly potent
pharmaceutics.
• nanotechnology based drug delivery system has
potential to overcome the poor aqueous
solubility and poor enzymatic/metabolic stability
of drugs associated with the oral route of
administration.

8. • nanoparticles improve delivery of poorly
water soluble drugs in water by delivering
drug of small particle size allowing faster
dissolution in blood stream leading to
targeted drug delivery in a cell- or tissue-
specific manner.

9. • Highly lipophilic
drugs can also be
employed inside
the hydrophobic
core of
biocompatible
polymer or
surfactant.

10. • A) blood-brain-barrier (BBB):
• nanoparticles can be employed in delivering
therapeutic agents in brain tumor as they can
cross blood brain barrier through opening of
tight junctions eg. (hyper-osmotic mannitol).
• Tween-80 coated nanoparticles have been
shown to cross the blood-brain barrier.

11. • B) enzymatic degradation in GIT:
• Three main factors have been reprted to
destabilize oral delivery.
• These include bile salts, pH, pancreatic and
gastric enzymes (which would mainly impaire
delivery of protein based drugs like insulin).

12. • To protect the drug from these harsh
condition drug is better coated with a
biocompatible carrier eg. (liposome, poly
saccharide …,etc).

13. • For example, using liposomes as a suspension
or solubilizing agent for highly lipophilic drugs
to be delivered as micro-emulsion in soft gel
capsule for oral dosage.

14. • C) immunogenic clearance:
• When nanoparticles are adminstered
intravenously, they are treated as foreign
particles by the body immune systems, and
they are phagocytosed from the circulation.
• The surface lipophilicity of nanoparticles
decides the amount of adsorbed blood
components as proteins (opsonins) in
circulating blood influence the in vivo fate of
nanoparticles.

15. • Binding of these opsonins on the surface of
nanoparticles called opsonization, which acts
as a bridge between nanoparticles and
phagocytes.

16. • in order to prevent drugs from getting ingested by
phagocytes, the surfaces of the nanocarriers are
typically coated with the biocompatible synthetic
polymer poly(ethylene glycol) (PEG) which is called
stealth effect.
• So these nano carriers prolonged the retention
time of drug (T1/2 in circulation) and decreased its
clearance by spleen,…etc.

18. • controlled drug delivery system enhances drug
concentration in diseased tissues, therefore,
lower doses of drugs are required so it improved
efficacy, reduced toxicity and improved patient
compliance and convenience.

19. • serious side effects associated with
medications as chemotherapeutic agents like
bone marrow inhibition, destruction of gut
mucosa,..etc are sometimes more dangerous
than the disease itself.

20. • Cell-specific targeting is generally achieved by
attaching drugs to individually designed nano
carriers.
• There are two main mechanisms of targeted
drug delivery:
A) passive targeting. B) active targeting.

21. A) Passive targeting:
• passive targeting is achieved through a process
called enhanced permeability and retention
(EPR) effect.
• As tumor cells tend to grow quickly, they must
stimulate the production of blood vessels.
• These newly formed tumor vessels are usually
abnormal in form and architecture.

22. They are poorly aligned defective
endothelial cells with wide
fenestrations, lacking a smooth muscle
layer, or innervation with a wider
lumen, and impaired functional
receptors for angiotensin II.

23. • The enhanced permeability and retention
(EPR) effect is a controversial concept by
which molecules of certain sizes (typically
liposomes or nanoparticle) tend to
accumulate in tumor tissue much more than
they do in normal tissues.

24. • tumor tissues usually lack effective lymphatic
drainage.
• All of these factors lead to specific
accumulation and prolonged retention of the
nano particulate drug.

25. B) Active targeting:
• Active targeting can be referred to as
receptor mediated drug delivery.
• In the most basic sense, drug design involves
the design of molecules that are
complementary in shape and charge to the
biomolecular (cell receptor) target with which
they interact and therefore will bind to it.

26. • the ligand is usually a molecule which
produces a signal by binding to a site on a
target receptor.
• Ligand binding to a receptor protein is named
“docking”.
• Ligands might be antibodies, polypeptides,
oligosaccharides (carbohydrates), viral
proteins, fusogenic residues, and molecules of
endogenous origin.

27. • Ligand-mediated active targeting has emerged
as a novel strategy in targeting diseased tissue
leaving the normal.
• the receptors act as molecular targets or
portals, and ligands being added to the
surface of nanoparticles, with receptor
specificity and selectivity, are trafficked en
route to the target site.

29. • features of using nanoparticles as drug
delivery systems include easy manipulation of
particle size and its surface characteristics to
achieve both active and passive drug
targeting, controlled and sustained discharge
of the drug both during the transportation
and at the target site increasing drug’s
therapeutic efficacy and reducing side effects.

30. • Nanoparticles also aid in carrying large
payloads, such as designing a delivery system
containing multiple components as:
a) Combined therapeutic agent:
Sometimes there is a need for combined
formulations having more than one active
ingredients for treatment of some diseases as
tuberculosis, H. pylori, psoriasis,…etc.
Some times there are troubles in combining these
active ingredients due to incompatibility or
stability problems.

31. • multiple-block nanoparticle formulations are
also beneficial in where there is a need to
combine hydrophilic/lipophilic drugs.
• Herein, we use for example, liposome with its
non-polar tails forming a hydrophobic core
where the lipophilic drug is entrapped and a
hydrophilic drug can be attached to the
surface.

32. b) imaging agents:
• imaging agents can also be incorporated within
the nanoparticles that allow visualization of the
site of drug delivery or to monitor the in vivo
efficacy of the therapeutic agent .
• in the recent years nanoparticles gained attention
in the application of imaging procceses as
magnetic resonance imaging MRI, computed
tomoghraphy, flourescence imaging,…etc.

33. • Nanoparticles (NPs), in contrast to molecular
probes, often are less cytotoxic and do not
suffer from nonspecific binding by cellular
biomacromolecules or unwanted
sequestration.
• Nanoparticles have several advantages over
small molecule traditional imaging agents,
such as long blood-pool residence times, and
the potential for cell tracking and targeted
imaging applications.

35. c) ligand for targeting specific receptor on a
diseased tissue as discussed before.

36. • nanoparticles are promising for delivering
compounds to improve the pharmacological and
therapeutic properties of conventional drugs.
• Incorporating drug molecules in nanocarriers
provides massive advantages like better bio-
distribution of active compounds, protection
against degradation, improved drug attachment,
passage, targeting, expulsion and communication
with biological barriers.
• It is hoped that nanoparticle-mediated drug
delivery systems will revolutionize and prove to
be the milestone in the biomedical field.

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