NEW DRUG DELIVERY SYSTEMS

Dr M.BHEEMESH

PG IN PHARMACOLOGY
 INTRODUCING A NEW DRUG TO
MARKET COSTS AN AVERAGE
US$ 897 MILLLON/4485 CRORES

PROCESS FOR APPROVAL MAY TAKE

UP TO 15 YEARS
SO ALREADY EXISTING TIME TESTED
DRUGS ARE EFFECTIVELY USED BY
INTERDISCIPLINARY APPROACHES
TO INCREASE THERE EFFICACY
 ADVANTAGES:

INCREASE DRUG BIO AVAILABULITY IN

REQUIRED ZONE

PREVENT/MINIMISE HARMFULL SIDE

EFFECTS

MINIMISE DRUG DEGRADATION AND

LOSS
 1.ENTERAL ROUTES:
ORAL, SUB LINGUAL,RECTAL

2.PARENTERAL ROUTES:
I.V,I.M,INRADERMAL,SUB
CUTANEOUS,INHALATIONAL

3.TOPICAL ROUTES:
TRANSDERMAL,CONJUNCTIVAL,
VAGINAL AND URETHRAL
MATRIX TABLET
 Matrix tablet

DRUG IS IN CORPORATED IN A
LATTICE or INERT MESHWORK

ADVANTAGE: SINGLE DAILY SUSTAINED

RELEASE OF THE DRUG
 PRODRUG

INACTIVE CHEMICAL COMPOUNDS AFTER

ADMINISTRATION UNDERGOES BIOTRANSFORMATION TO
PHARMACOLOGICALLY ACTIVE COMPOUNDS
LEVODOPA •DOPAMINE

TALAMPICILLIN •AMPICILLIN
TRANS DERMAL DRUG DELIVERY
 TRANS DERMAL DRUG DELIVERY

THESE ARE ADHESIVE PATCHES

CONTAING DRUG WHICH PASSIVELY
DIFFUSES THROUGH THE SKIN

CURRENTLY USED DRUGS ARE:

NITROGLYCERINE,
CONTRACEPTIVES etc
 ADVANTAGES DIS-ADVANTAGES

• CONTINUOUS • DRUG DELIVERY IS

DRUG DELIVERY PASSIVE
• NO PAIN • LARGE MOLECULAR
• NO MISSING OF WEIGHT DRUGS ARE
DOSE NOT DELIVERED
Newer `ACTIVE’ technologies in
Transdermal drug delivery

1,IONTOPORESIS
2,LASER ASSISTED
TRANSDERMAL DRUG DELIVERY
IONTOPORESIS
ADVANTAGE: DRUG DELIVERED
CAN BE MEASURED

DIS ADVANTAGE: CAN`T

DELIVER LARGE MOLECULAR
WEIGHT DRUGS
LASER ASSISTED TRANSDERMAL DRUG
DELIVERY
PORES ARE MADE ON SKIN USING LASER
LARGE MOLECULAR WEIGHT DRUGS CAN BE
DELIVERED THROUGH SKIN PERFORATIONS
MICRO ELECTRICAL MECHANICAL SYSTEM
[MEMS] SYRINGE

FREEZE-DRIED
DRUG STORED IN
ITS SILICON RUBBER
RESERVOIR
• ADVANTAGES • DIS ADVANTAGES

• LESS PAIN
• NO NERVE DAMAGE • HIGH COST
• NO INJECTION
ABSCESS
PEN JET
IT’S A NEW METHOD OF
DELIVERING DRUG IN TO
SUBCUTANEOUS PLANE
MECHANISM:USING COMPRESSED
GAS DRUG IS FORCED TO PASS
THROUGH THE SKIN.
NON-INVASIVE
ADV:1

2,POWDERS AND LIQUIDS CAN BE USED

 NASAL DRUG DELIVERY

LOCAL: ANTIHISTAMINICS

SYSTEMIC:DESMOPRESSIN FOR
DIABETES INSIPIDUS
NASOCOBAL FOR PERNICIOUS ANEMIA
Site of drug
spray &
absorption
ADVANTAGES

By passes liver first pass

metabolism
 POLYMER DELIVERY SYSTEM

DRUG IS ENTRAPED IN SOLID

POLYMER LIKE SILICONE RUBBER
WHICH IS IMPLANTED or INJECTED
IN BODY

E.g.: norplant
progestasert
 NORPLANT

LEVONORGESTROL
SUBDERMALLY
IMPLANTED PROVIDES
CONTRACEPTIVE
PROTECTION
FOR
5 Years
 PROGESTASERT

INTRA UTERINE
CONTRACEPTIVE DEVICE

CONTROL RELEASE OF
PROGESTERONE FOR A
YEAR
ADVANTAGES

NO MISSING OF DOSE

DIS ADVANTAGES

ECTOPIC PREGNANCY
CHANCE OF P.I.D
 OCUSERT

PLACED UNDER
THE EYELID

DELIVERS A
STEADY FLOW
ROUND THE
CLOCK FOR 7
Days

PILOCARPINE
 DIS ADVANTAGE:
LIMITED SUCCESS DUE TO HIGH
IRRITATION AND COMPLICATED
APPLICATION
 DRUG-ELUTING STENTS

A METALLIC DEVICE
CONTAINS A DRUG
GRADUALLY RELEASED
OVER 14-30 DAYS

DRUGES USED:
•SIROLIMUS
•PACLITAXEL
SIROLIMUS HELPS IN PREVENTING
RE -STENOSIS
TARGETED DRUG DELIVERY SYSTEM

1,LIPOSOMES
2,MONOCLONAL ANTIBODIES
3,NANO TECHNOLOGY MEDIATED
DRUG DELIVERY
 LIPOSOMES

LIPOSOMES ARE A
FORM OF VESICLES

-Dr ALEC D BANGHAM

LIPOS-FAT, SOME-BODIES
Multi vesicular liposome
STEALTH LIPOSOME
DRUGS DELIVERED THROUGH
LIPOSOMES:

AMPHOTERICIN B

DAUNORUBICIN

DOXORUBICIN
 MONOCLONAL ANTIBODIES [M A B]

Also known as MAGIC BULLET

INVENTED BY KOHLER and MILSTEIN IN 1975

GOT NOBEL PRIZE IN 1984

Definition:

MABs ARE A CLASS OF HIGHLY

SPECIFIC ANTIBODIES PRODUCED
BY THE CLONES OF A SINGLE
HYBRID CELL FORMED IN THE
LABORATORY BY THE FUSION OF
B-LYMPHOCYTES WITH A TUMOUR
CELL.
 Adapted from Milstein (1980) Scientific American, Oct. p.58

Antigen 31 2 4
1 m
3 m
BA
LB / 2 m Spleen cells
4 m
c

Immunization
+
B cell Myeloma
1
2 3 Cell fusion
1 2 3 4
4

x 1 2 3 4
31 2 4

Monoclonal
antibodies
Antiseum
Pure single Ab
A mixture of all Ab If a single
Each B cellB produces
cell was picked
only oneup kind
and cultured,
of antibody,
then
which
it willbinds
produce
to itsonly
specific
one kind
antigen.
of antibody.
After
Myeloma
IfEach
B cell
immunization,
hybridoma
is cell
fusedcanwith
line
bethe
can
myeloma,
cultured
mouse
produce
inspleen
the
thepure
fused
testcontains
single
tube,
cell might
antibody,
but
B cells
can benot
cultured
producing
called
produce
monoclonal
andspecific
useful
produce
antibody.
antibodies.
antibody.
antibody.
Conventional
But B cell canantiserum
not surviveis well
the mixture
in the culture.
of all antibodies produced by B cells from spleen.
 MABs ARE PRODUCED
1]IN ANIMALS
2] IN CELL-CULTURE
3]BATCH TISSUE-CULTURE
METHODS
4]BY IN VITRO TECHNIQUES

IN VITRO TECHNIQUES ARE USED

IN MORE THAN 90% OF CASES
MABs ARE CLASSIFIED INTO GENERATIONS AS PER
THEIR EVOLUTION AND IMMUNOGENICITY

1. FIRST GENERATION MABs:

DEVELOP FROM MURINE , RABBIT, RATS.
DISADVANTAGES : Abs TO THESE
FOREIGN ANTIGENS
HAMA-HUMAN ANTI-MOUSE ANTIBODIES
HARA-HUMAN ANTI-RABBIT ANTIBODIES
 2] SECOND GENERATION Mabs

RECOMBINANT DNA technology [OR]

GENETIC ENGINEERING is used to
construct hybrids composed of human anti
body regions linked with primate or
murine back bone.
 MONOCLONAL ANTI BODIES

1,FIRST GENERATION Abs 2,SECOND GENERATION Abs

1,chimeric Abs e.g : infliximab,rituximab

2,humanised Abs e.g:daclizumab,trastuzumab

3,primatized Abs

4,genetically engineered Abs e.g. ALEMTUZUMAB

MECHANISM OF TRASTUZUMAB ACTION
 DIS ADVANTAGES

1] COST IS VERY HIGH

2] PHARMACO VIGILANCE
STUDIES REVEALED THAT
RITUXIMAB IS CAUSING
PROGRESSIVE
MYELOENCEPHALOPATHY.
 NANO TECHNOLOGY

Definition:

The study and manufacture of devices of

molecular dimensions, in the range of
nanometers or one-billionth of a meter
 APPLICATIONS OF NANO TECHNOLOGY

Diagnostic
- Imaging
- Quantum dots
- Microscopic sampling

Therapeutic
- Delivering medication to the exact location
- Treatment of cancer
- Repair of damaged tissues
 TREATMENT OF CANCER WITH
MAGNETIC NANO PARTICLES

NANO PARTICLE OF SIZE 20 nm

500 times smaller than R.B.C cell
1 ml OF NANO SOLUTION CONTAINS 1TRILLION
NANO PARTICLES
GLIO BLASTOMA
ALTERNATIVE MAGNETIC FIELD 1000/SEC
FUTURE TRENDS
“A microscopic
machine roaming
through the
bloodstream,
injecting or taking
samples for
identification and
determining the
concentrations of
different
compounds"
Mechanical
drilling of a
small tumor
mass by a
nanorobot
 Dental
Robots

Four remote-controlled nanorobots examine

and clean the subocclusal surfaces of a
patient's teeth, near the gumline.
Medical
nanodevices
could augment
the immune
system by finding
and disabling
unwanted
bacteria and
viruses.
A NANOROBOT NIBBLING ON AN ATHEROSCLEROTIC DEPOSIT IN A
BLOOD VESSEL
VIRUS FINDER
CLOT-INDUCING MEDICAL NANOROBOTS ARE SHOWN IN
VARIOUS STAGES OF CLOT-NETTING DEPLOYMENT.
AN ARRAY OF NINE CLOT-INDUCING MEDICAL NANOROBOTS ARE
SHOWN WITH THEIR CLOT-NETTING FULLY DEPLOYED AND
INTERLACED.
MEDICAL NANOROBOTS WITH FULLY DEPLOYED NETTING ARE
SHOWN EMBEDDED IN A PATCHLIKE GROWING CLOT WITH RED
CELLS AND FIBRIN STRANDS INVOLVED.
CLOT-INDUCING MEDICAL NANOROBOTS WITH FULLY-DEPLOYED
NETTING ARE SHOWN EMBEDDED IN A PATCHLIKE GROWING CLOT
WITH RED CELLS AND FIBRIN STRANDS INVOLVED (A CLOSER LOOK)
ROUGH ESTIMATES SAYS THAT THIS
WILL BE ACHIEVED IN ABOUT
10-20YEARS

DISADVANTAGES OF NEW DRUG

DELIVERY SYSTEMS
COST IS VERY HIGH
 CONCLUSION
EVEN THOUGH THE COST OF THESE
METHODS ARE PROHIBITIVELY HIGH,
THEY STILL OFFER MANY
ADVANTAGES

ALL THE NEWER METHODS HAVE

THE POTENTIAL TO FULFILL THE
CURRENT MEDICAL NEEDS AND
THUS ARE THE METHODS FOR
IMMEDIATE FUTURE
 REFERENCES

PRINCIPLES OF PHARMACOLOGY
H.L SHARMA,K.K SHARMA

INDIAN JOURNAL OF PHARMACOLOGY VOL-39

WWW.ENCAPSULA.COM