This document discusses novel drug delivery systems (NDDS), including liposomes, micelles, nanoparticles, and phytosomes. NDDS are formulations that transport pharmaceutical compounds in the body to achieve therapeutic effects in a safer, more effective manner than conventional methods. Liposomes, micelles, nanoparticles, and phytosomes are described as types of NDDS that can encapsulate or absorb drugs to improve delivery properties, stability, and bioavailability. Specific examples are provided of using liposomes to deliver anticancer drugs, herbal compounds, and antifungal agents.
2. What is
NDDS?
Novel Drug delivery System (NDDS) refers to
the approaches, formulations, technologies,
and systems for transporting a
pharmaceutical compound in the body as
needed to safely achieve its desired
therapeutic effects
NDDS is a system for delivery of drug other
than conventional drug delivery system.
NDDS is acombination of advance technique
and new dosage forms which are far better
than conventional dosage forms
3. Drug delivery Carrier:
ā¢ drug carrier systems such as micelles,
liposomes, as well as nanoparticle
dispersions consisting of small particles of
10ā400 nm diameter show great promise
as drug delivery systems.
ā¢ the goal is to obtain systems with
optimized drug loading and release
properties, long shelf-life and low toxicity
4. Liposomes
ļLiposomes are a form of vesicles that consist either of
many or just one phospholipid bilayers, the particle
size of liposomes varies from 20nm to 10Ī¼m.
ā¢ small unilamellar vesicles(SUV) varies from
0.02ā0.05Ī¼m
ā¢ large unilamellar vesicles (LUV) are more than
0.06Ī¼m
ā¢ multi lamellar vesicles (MLV) size is in between and
0.5Ī¼m.
ļThe polar core enables polar drug molecules to be
encapsulated. Amphiphilic and lipophilic molecules
are solubilized within the phospholipid bilayer
according to their affinity towards the phospholipids.
5. ā¢ Channel proteins can be incorporated without loss of their activity within the
hydrophobic membranes, acting as a size-selective filter, only allowing passive
diffusion of small solutes such as ions, nutrients and antibiotics. Thus, drugs that are
encapsulated are effectively protected from premature degradation by proteolytic
enzymes. The drug molecule is able to diffuse through the channel.
6. ā¢ Liposomes have a short biologicalālife
in blood circulation. The circulation
time of liposomes in the blood stream
can be increased by attaching them to
polyethylene glycol (PEG)āunits. The
presence of PEG on the surface of the
liposomal carrier reduce mononuclear
phagocyte system uptake
ā¢ The two important methods used for
preparing liposomal drug delivery
systems are, Simple hydration method
and emulsion method
7. Liposome in Anticancer drugs:
ā¢ liposomes exhibit extravasation and
accumulation at the site of solid tumors due
to increased endothelial permeability and
reduced lymphatic drainage in these tissues.
ā¢ Liposomal delivery improve the therapeutic
efficacy of anticancer drugs and reduce or
modulate their toxicity profile.
ā¢ For example, long circulating PEG-coated
liposomal formulation of doxorubicin -DoxilĀ®
doxorubicin
8. Liposome in herbal formulation:
ā¢ Liposomes have been used to change the
pharmacokinetics profile of not only drugs,
but herbs, vitamins and enzymes.
ā¢ Milk thistle (Silybum marianum) is one of
the few herbal drugs whose excellent
pharmacological profile and itās
hepatoprotective , but it is poorly absorbed
(20ā50%) from the gastrointestinal tract , so
itās formulated in liposomal form to enhance
the bioavailability
9. Liposome in Antifungal agents :
Liposomal Amphotericin B (LAmB) ā PhsomeĀ®
ā¢ It is contains amphotericin B , It is a true liposome
composed of unilamellar lipid vesicles
ā¢ LāAmB has high plasma concentration and longer
circulation time than other lipid formulations.
ā¢ L-AmB show less nephrotoxicity compared to regular
Amphotericin B
10. Micelles
ā¢ Micelles formed by self-assembly of amphiphilic block
copolymers (5-50 nm) in aqueous solutions
ā¢ the hydrophilic blocks can form hydrogen bonds with
the aqueous surroundings and form a tight shell around
the micellar core.
ā¢ the contents of the hydrophobic core are effectively
protected against hydrolysis and enzymatic
degradation.
ā¢ Micelles are used for drug delivery applications because
of their chemical composition, total molecular weight
and block length ratios can be easily changed, which
allows control of the size and morphology of the
micelles.
11. ā¢ Functionalization of block
copolymers with cross linkable
groups can increase the stability of
micelles and improve their
temporal control.
ā¢ Substitution of block copolymer
micelles with specific ligands is a
very promising strategy to a broader
range of sites of activity with a much
higher selectivity.
12. Lipoproteins
ā¢ Lipoproteins are biological lipid carriers
play important role in transport of fats
within the body. These are natural
nanoparticles which serve as drug-
delivery vehicles due to their small size,
long residence time in the circulation.
ā¢ Lipoproteins carry high drug payload
and are used as delivery vehicles for
transportation of chemotherapeutic
agents.
13. Targeted drug delivery system in cancer treatment:
ļA targeted drug delivery system enhance the therapeutic index of
anticancer agents, either by increasing the drug concentration in
tumor cells or by decreasing the exposure in normal host tissues.
ļThe Ways to use : physical and biological targeting strategies.
ā¢ Physical targeting:
is based on delivering anticancer agents directly to tumor tissue by
physical implantation or injections of the agents precisely at the tumor
site.
ā¢ Biological targeting :
anticancer moiety can be delivered by specific carriers such as
lipoproteins.
14. Low density lipoprotein for targeted delivery
of anticancer
ā¢ Growing cells need cholesterol to construct cell membranes. They
acquire cholesterol via de novo synthesis and high affinity receptor-
mediated uptake of low-density lipoprotein (LDL).
ā¢ Many types of tumor cells display higher level of receptor mediated
LDL uptakes compared to normal tissues. LDL has therefore been
proposed as a potential carrier for chemotherapeutic agents.
ā¢ conjugation of an antitumor moiety with cholesterol facilitates the
loading of these compounds into LDL.and
ā¢ utilize the elevated LDL receptor expression on tumor cells for
targeted drug delivery.
15. Nanoparticles
ā¢ They are in the solid state and are either amorphous or crystalline.
(including nanospheres and nanocapsules of size 10-200 nm)
ā¢ They are able to adsorb and/or encapsulate a drug, thus protecting it
against chemical and enzymatic degradation.
ā¢ Nanocapsules are vesicular systems in which the drug is confined to a
cavity surrounded by a unique polymer membrane.
ā¢ Nanospheres are matrix systems in which the drug is physically and
uniformly dispersed.
16. Classification of nanomaterials:
ā¢ Nanotubes- They are hallowing cylinders
made of carbon atoms.
ā¢ Nanowires- Glowing silica nano wire is
wraped around a single stand of human hair.
ā¢ Nanocantilever- The honey comb mesh
behind this tiny carbon cantilever is surface
of flyās eye. Cantilevers are beams anchored
at only one end.
ā¢ Nanoshells- are hollow silica spheres
covered with gold.
ā¢ Quantum dots- are miniscule semiconductor
particles that can serve as sign pots of
certain type of cells or molecules in the
body.
17. ā¢ Nano pores- have cancer research and
treatment applications. Engineered into
particles, they are holes that are so tiny that
DNA molecules can pass through them one
strand at a time allowing for highly precise and
efficient DNA sequencing.
ā¢ Gold nanoparticles- represent a novel
technology in the field of particle-based tumor-
targeted drug delivery.
ā¢ Bucky balls- Bucky ball is common for a
molecule called buckminsterfullerene, which is
made of 60 carbon atoms formed in shape of
hollow ball discovered in 1985.
ā¢ Dendrimers- are nanometer-sized, highly
branched and monodisperse macromolecules
with symmetrical architecture.
18. Phytosomes :
ā¢ The phytochemical and
phytopharmacological sciences established
the compositions, biological activities and
health promoting benefits of numerous
plant products.
ā¢ Phytosomes are more bioavailable as
compared to conventional herbal extracts
owing to their enhanced capacity to cross
the lipoidal biomembrane and finally
reaching the systemic circulation.