INTRODUCTION TO

DRUG DELIVERY

Dr. Wan Maznah Binti Wan Ishak

 TOPIC OUTCOMES

A Overview of drug delivery systems

Advantages pf pharmaceutical
B
dosage forms

Formulation development of
C
different dosage forms
OVERVIEW OF
DRUG DELIVERY SYSTEM
 Drug Delivery Systems (DDS)
• DDSs are polymeric or lipid carrier systems that transport drug to their targets or
receptor sites that
➢ Provides their maximum therapeutic activity
➢ Prevent their degradation or inactivation during transit to the target sites
➢ Protect body from adverse reactions due to inappropriate disposition.

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 Drug Delivery Systems (DDS)
• The goal of a drug delivery system is
➢ to release the drugs simultaneously and
provide maximal safety, effectiveness and
reliability

• Ideally, a DDS could deliver the correct amount of

drug to the site of action at the correct rate and
timing in order to maximize the desired
therapeutic response

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 Drug Delivery Systems (DDS)
• The DDS should aim to provide drug
concentration at the site of action above the
minimal effective concentration yet below the
maximal tolerated plasma concentration
(minimal toxic concentration)
• Factors that control drug concentration
➢ Route of administration
➢ Frequency of administration
➢ Metabolism of drug
➢ Drug clearance
➢ Dosage form design of drug

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 Classification of DDS

Route of
Physical State
Administration

Rate of Drug
Release
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Classification of DDSs
Physical state
✓Gaseous (eg anesthetics)
✓Liquid (eg: solutions,
emulsions and suspensions)
✓Semisolid (eg: creams,
ointments and gels)
✓Solid (eg: tablets and
capsules)
 Classification of DDSs
Site/Route of Administration
Peroral
Injection/ Transmucosal
Topical (through the
Infusion
mouth)
▪ Intravenous ▪ Nasal
▪ Intramuscular ▪ Buccal
▪ Intradermal ▪ Sublingual
▪ Intraperitoneal
▪ Subcutaneous
Classification of DDSs
Rate of Drug
Release

Immediate Modified
Release Release

Delayed Sustained
Release Release

Controlled Targeted
Release Release
 Rate of Drug Release
Immediate Release
• The drug is released immediately after
administration
• Designed to give a fast onset of drug action
• The most common from solid dosage forms such as
disintegrating tablets, chewable, effervescent,
sublingual and buccal tablet as well as liquid dosage
form
• These tablets often referred as plain or conventional
tablets
• Factors influencing drug delivery in solid dosage
forms
➢ Drug solubility
➢ Drug disintegration and dissolution
➢ Drug absorption across membrane permeability

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 Rate of Drug Release
Immediate Release
• Epithelia presents a physical and biochemical
barrier to drug absorption
• Drugs must be in solution before they can cross
epithelia, so rate of absorption is controlled by
how fast the drug dissolves in the fluids at the
absorption site described as dissolution rate
limited.
• Therefore, solubility of drug is an important
physicochemical property affecting drug
absorption

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 Rate of Drug Release
Modified Release
• Drugs release that occurs sometime after administration or for sustained period
or to a specific target in the body
• These systems tend to be used to improve therapeutic outcome of the drug
intervention to improve patient adherence
• Modification of the time course and site of drug release is commonly achieved
by solid dosage form

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 Rate of Drug Release
i) Delayed Release
• The drug is not released immediately after
administration but sometime after administration
• Typical delayed release dosage forms are enteric-
coated tablets which delay drug release until
reach at the small intestine or the colon
• Upon reaching these sites, drug release should be
rapid and drug concentration vs time profiles
often similar to that of an immediate release
dosage form but the time between administration
of DDS and the drug release is delayed

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 Rate of Drug Release
ii) Sustained Release
• The drug is released over a prolonged period
of time
• The drug is release slower than IR delivery, so
that the therapeutic plasma levels are
maintained over a prolonged period of time
(typically 8-12 h)
• Typical sustained dosage forms are polymer-
coated pellets and matrix tablets

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 Rate of Drug Release
iii) Controlled Release
• The drug is released at a predetermined rate for a prolonged period of time, so
effective drug plasma levels are maintained and controlled over an extended
period of time
• In contrast to SR dosage forms, CR delivery systems aim to control both the
drug release from the dosage form and also the subsequent plasma levels,
therefore plasma levels are solely determined by the drug release kinetics from
the DDS
• Eg oral osmotic system

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 Rate of Drug Release
iv) Targeted Release
• Attempted to deliver the drug to a specific target where the drug release is
triggered
• For eg, through a time delay or as a result in a change in the environment
surrounding the MR system (eg change in pH)
• This can enhance drug efficiency and reduced toxicity

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Rate of Drug Release

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 ROUTE OF
ADMINISTRATION FOR
DRUG DELIVERY
Oral Drug Delivery
• The preferred route of administration for pharmaceutical product has been oral
ingestion
• As a drug passes through GIT, it encounters different environments with respect
to pH, enzymes, electrolytes, fluidity and surface features, all of which influence
drug absorption
• pH at various sites in GIT
• Stomach (pH 2-4)
• Duodenum (pH 5.5)
• Small intestines (pH 6-7)
• Distal ileum (pH 7-8)
• Colon (pH 5.6)

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Buccal and Sublingual Drug Delivery
• Buccal and sublingual mucosae in the oral cavity provide an excellent alternative
for the delivery of certain drugs
• Oral transmucosal absorption is rapid because of the rich vascular supply of the
mucosa
• These routes provide improved delivery for certain drugs that are inactivated by
first-pass intestinal/hepatic metabolism or proteolytic enzymes in GIT

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Buccal and Sublingual Drug Delivery
• Sublingual mucosa is
✓ relatively permeable
✓ suitable for delivery of low-molecular weight lipophilic drugs
✓ rapid onset of action is required
✓ Infrequent dosing is required
• Sublingual DDS are generally of two different designs
• Rapidly disintegrating tablets
• Soft gelatin capsules filled with a drug in solution
• Such systems create a very high drug concentration in the sublingual region
before they are systemically absorbed across the mucosa

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Buccal and Sublingual Drug Delivery
• Buccal mucosa
✓ less permeable than sublingual area
✓ not able to provide rapid absorption properties
• The buccal mucosa suitable for sustained-delivery applications
• Buccal DDS usually include permeability enhancer to increase the flux of drugs
through the mucosa
• Bioadhesive polymers extensively employed in buccal DDS to reduce drug
retention at the site of absorption

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Nasal Drug Delivery
• Nasal DDS traditionally used for locally acting drug
• Major advantages of nasal administration
➢ fast absorption
➢ rapid onset of action
➢ avoidance of hepatic and intestinal first-pass effects
• Dosage forms for nasal absorption must deposit and remain in the nasal cavity
long enough to allow effective absorption

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Nasal Drug Delivery
• Eg: nasal sprays and nasal drops
• Nasal spray deposits drug in the proximal part of the nasal atrium
• Nasal drops are dispersed throughout the nasal cavity
• A nasal spray requires that the particles have a diameter larger than 4 µm to be
retained in the nose and to minimize their passage into the lungs

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Pulmonary Drug Delivery
• This route of administration is useful for treating pulmonary conditions and for
drug delivery to other organs via the circulatory systems
• Lipid-soluble molecules are absorbed rapidly from the respiratory tract thus
increasing number of drugs are being administered by this route including
bronchodilators, corticosteroids, antibiotics, antifungal agent etc
• Because lung has a large surface area and a highly permeable membrane, the
lung is an ideal site for absorption of macromolecules such as proteins, peptides,
oligonucleotides and genes

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Ocular Drug Delivery
• Drugs are topically applied to the eyes in the form of drops or ointments for local
action
• Following topical administration, a drug is eliminated from the eye by
nasolacrimal drainage, tear turnover, productive corneal absorption and
nonproductive conjunctival uptake
• For drugs administered through topical route, cornea is the main barrier to drug
absorption
• Ocular drug absorption depends on both drug ionization and tear turnover

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 Ocular Drug Delivery
• Cornea has three parts
▪ Epithelium
▪ Endothelium
▪ Stroma
• Both endothelium and epithelium have high lipid
content, thus are penetrated by drug in their
unionized lipid soluble forms
• Stroma lying between these two structures has a
high-water content, thus drugs must be both lipid
soluble and water soluble to some extent

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Rectal Drug Delivery
• Rectal administration provides rapid absorption and is an alternative when oral
administration is inconvenient because of inability to swallow or because of GIT
side effects such as nausea, vomiting and irritation
• Rectal administration has the advantage of minimizing or avoiding hepatic first-
pass metabolism
• However, rectal route is inconvenient and has irregular drug absorption
• Moreover, rectal administration should be avoided in immunosuppressed
patients in whom even minimal trauma could be led to the formation of an
abscess

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Vaginal Drug Delivery
• Vaginal epithelium is permeable to a wide range of substances including steroids,
prostaglandins, antibiotics and estrogen
• Most steroids are readily absorbed by vaginal epithelium leading to their higher
bioavailability because of reduced first-pass metabolism
• Vaginal ointments and creams contain drugs such as anti-infectives, estrogenic
hormone substrates and contraceptive agents

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