Principles of Drug Delivery

System
Prof. Usman Sumo Friend Tambunan
Vincent Jonathan Fleming
Bioinformatics Research Group – Universitas Indonesia
Discovery of Morphine
• Opium plant (Papaver somniferum) was used in ancient
civilizations (4000-1000 BCE) for various medicinal
purposes and in religious ceremonies
• Opium is produced by drying the latex that exudes from
the capsules of the poppy.
Discovery of Morphine

• Around 1805-1820, a number of individuals simultaneously

reported the isolation of a crystalline, alkaline material
from the poppy latex.
• Friedrich Wilhelm Serturner (1783-1841) showed in 1811
that administration to dogs made the animals sleepy.
Discovery of Morphine
• The true benefit of morphine as a
pain-relieving agent only became
apparent after the invention of
the hypodermic syringe by
Alexander Wood in 1853
• Morphine found great utility in the
civil war, but, since ideal dosing
was not established, also caused
many deaths
• The chemical structure of
morphine was not established till
1923, when J. Masson Gulland
and Robert Robinson succeeded in
deciphering it
Discovery of Penicillin
• In 1928, Alexander Fleming, a
bacteriologist at St. Mary’s Hospital, had
returned from a vacation when, while
talking to a colleague, he noticed a zone
around an invading fungus on an agar
plate in which the bacteria did not grow.
• After isolating the mold and identifying it
as belonging to the Penicillium genus,
Fleming obtained an extract from the
mold, naming its active agent penicillin
• He determined that penicillin had an
antibacterial effect on staphylococci and
other gram-positive pathogens.
Drug Delivery
• The appropriate administration of drugs through
various routes in the body for the purpose of
improving health
• It is highly interdisciplinary
• It has recently evolved to take into consideration
a) Drug physico-chemical properties
b) Body effects and interactions
c) Improvement of drug effect
d) Patient comfort and well being
Oral
• This is the oldest route which has been used for
conventional and novel drug delivery. The main two
reasons for considering this route is the highly
preferred one are ease of administration and the
highly accepted and/ or comfortable for the patients
• Traditional oral delivery systems
Tablets
Capsules
Soft gelatin capsules
Suspensions
Elixirs
Oral
Advantages of Oral Delivery:
• Convenience in Administration
• Non invasive
• Accurate and measured dose
• Unit Dosage form
• Higher compliance
• Cheap for the patient

Disadvantages of Oral Delivery

• Unconscious patients can not take dose
• Low permeability
• Degradation by Gastro-Intestinal enzymes
• First pass metabolism
• Irregular absorption
Buccal/Sublingual
• Tablets or chewing gums are placed under tongue
(sublingual) and between cheeks (buccal)
• Advantages:
By-pass First pass metabolism
Rapid absorption
Low enzymatic activity
• Disadvantages
Discomfort during dissolution
Probability of swallowing- lost of effect
Small doses
Rectal
• Suppositories are placed inside rectum and it melts
at body temperature to give quick effect.
• Advantages:
By-pass first pass metabolism
Useful for children
• Disadvantages
Absorption depends on disease state
Degradation by bacterial flora
Uncomfortable
Intravenous
• Drug in liquid form is administered directly into blood
by injecting in vein with the help of sterile injector.
• Advantages:
Drug 100% bioavailable
Rapid response
Can administer drugs degradable in stomach
By-passes First Pass Metabolism
• Disadvantages
Invasive
Trained personnel
Possible toxicity due to incorrect dosing
Sterility
Subcutaneous
• Liquid drug is administered in subcutaneous tissue
by injecting with injector
• Advantages:
Patient self-administration
Slow, complete absorption
By-pass FPM when placed at lower part of rectum
• Disadvantages
Invasive
Irritation
Inflammation
Maximum dose volume of 2mL
Intramuscular
• The liquid drug is administered in the muscle tissue
by injecting with injector
• Advantages:
Drug is absorbed slowly, so prolong effect
Larger volume than subcutaneous
By-pass first pass metabolism
• Disadvantages
Invasive – patient discomfort
Irritation
Inflammation
May require some training
Transdermal
• The medical treatment will apply on the body
surfaces such as the skin and / or mucous
membrane
• This route of administration significantly associated
with local effect rather than systemic effect.
• This route will transfer the active ingredients
directly to the systematic circulation without
gastrointestinal and/ or liver metabolism
Transdermal
Inhalation
• The medical treatment will directly reach the lungs,
by this way this route considers the route of choice
to avoid systemic effect i.e., increase the
bioavailability of the drug in the system
• This route consider as the first choice in the
treatment of respiratory diseases
Novel Drug Delivery System (NDDS)
• It is a combination of advance technique and new
dosage forms which are far better than conventional
dosage forms and involves medicinal devices
• It improves drug potency, control drug release to give
a sustained therapeutic effect, provide greater safety
and target a drug specifically to a desired tissue.
Advantages of NDDS
• Optimum dose at the right time and right location.
• Efficient use of expensive drugs, excipients and
reduction in production cost.
• Beneficial to patients, better therapy, improved
comfort and standard of living
Modes of NDDS
Targeted Drug Delivery System: The drug is delivered in such a way that
drug is only active in the target area of the body (cancerous tissues) in
which drug is released over a period of time in a controlled manner. e.g.,
Colon targeted drugs

Controlled Drug Delivery System: Release of drug is for long periods. In this
the rate or speed at which the drug is released is controlled by modification
in formulation. e.g. Nifidipine

Modulated Drug Delivery System: Here the rate of drug release is controlled
and modulated by devices such as nebulizer, MDI (metered dose inhaler),
etc
Thank you for
Listening
usman@ui.ac.id
vincent.jonathan@ui.ac.id