Novel Drug

Delivery System

SAYANI BHATTACHARYYA
Syllabus
Ø Unit -I 10 hours
o Controlled drug delivery systems: Introduction, terminology/definitions and rationale, advantages, disadvantages, selection of drug
candidates. Approaches to design controlled release formulations based on diffusion, dissolution and ion exchange principles.
Physicochemical and biological properties of drugs relevant to controlled release formulations Polymers: Introduction, classification,
properties, advantages and application of polymers in formulation of controlled release drug delivery systems.
Ø Unit-II 10 Hours
o Microencapsulation: Definition, advantages and disadvantages, microspheres /microcapsules, microparticles, methods of
microencapsulation, applications
o Mucosal Drug Delivery system: Introduction, Principles of bioadhesion / mucoadhesion, concepts, advantages and disadvantages,
transmucosal permeability and formulation considerations of buccal delivery systems
o Implantable Drug Delivery Systems: Introduction, advantages and disadvantages, concept of implants and osmotic pump
Ø Unit-III 10 Hours
o Transdermal Drug Delivery Systems: Introduction, Permeation through skin, factors affecting permeation, permeation enhancers,
basic components of TDDS, formulation approaches
o Gastroretentive drug delivery systems: Introduction, advantages, disadvantages, approaches for GRDDS – Floating, high density
systems, inflatable and gastroadhesive systems and their applications
o Nasopulmonary drug delivery system: Introduction to Nasal and Pulmonary routes of drug delivery, Formulation of Inhalers (dry
powder and metered dose), nasal sprays, nebulizers
Ø Unit-IV 08 Hours
o Nanotechnology and its Concepts: Concepts and approaches for targeted drug delivery systems, advantages and disadvantages, introduction to liposomes, niosomes,
nanoparticles, monoclonal antibodies and their applications
Ø Unit-V 07 Hours
o Ocular Drug Delivery Systems: Introduction, intra ocular barriers and methods to overcome –Preliminary study, ocular formulations and ocuserts
o Intrauterine Drug Delivery Systems: Introduction, advantages and disadvantages, development of intra uterine devices (IUDs) and applications
First sessional syllabus
Ø Unit -I 10 hours
o Controlled drug delivery systems: Introduction, terminology/definitions and rationale, advantages, disadvantages,
selection of drug candidates. Approaches to design controlled release formulations based on diffusion, dissolution and
ion exchange principles. Physicochemical and biological properties of drugs relevant to controlled release formulations
Polymers: Introduction, classification, properties, advantages and application of polymers in formulation of controlled
release drug delivery systems.
Ø Unit-II 10 Hours
o Microencapsulation: Definition, advantages and disadvantages, microspheres /microcapsules, microparticles, methods
of microencapsulation, applications
o Mucosal Drug Delivery system: Introduction, Principles of bioadhesion / mucoadhesion, concepts, advantages and
disadvantages, transmucosal permeability and formulation considerations of buccal deliverysystems
o Implantable Drug Delivery Systems: Introduction, advantages and disadvantages, concept of implants and osmotic
pump
Ø Unit-III 3 Hours
o Transdermal Drug Delivery Systems: Introduction, Permeation through skin, factors affecting permeation, permeation
enhancers, basic components of TDDS, formulationapproaches
Chapter Controlled drug
delivery systems:
ØIntroduction, terminology/definitions and rationale, advantages,
disadvantages, selection of drug candidates.
ØApproaches to design controlled release formulations based on
diffusion, dissolution and ion exchange principles.
Ø Physicochemical and biological properties of drugs relevant to
controlled release formulations
ØPolymers: Introduction, classification, properties, advantages and
application of polymers in formulation of controlled release drug
delivery systems.
Drug Delivery
Drug delivery - the method or process of administering
pharmaceutical compound to achieve a therapeutic effect in humans
or animals.

Most common methods of delivery include

◦ peroral (through the mouth) [preferred non-invasive ]
◦ topical (skin),
◦ transmucosal (nasal, buccal, sublingual, vaginal, ocular and rectal) and
◦ inhalation routes.
Drug Delivery
Many medications
◦ such as peptide and protein, antibody, vaccine and gene based drugs, in
general may not be administered using these routes (using conventional
DDS) because they might be susceptible to enzymatic degradation or can
not be absorbed into the systemic circulation efficiently due to molecular
size and charge issues to be therapeutically effective.

Protein and peptide drugs have to be delivered by injection.

Why do we need NDDS?
The conventional dosage forms provide drug
release immediately and it causes fluctuation of
drug level in blood depending upon dosage form.

Therefore to maintain the drug concentration

within therapeutically effective range needs novel
drug delivery system.
Plasma concentration vs time
profile
REASONS FOR DEVELOPING
NDDS
Repatenting successful drugs by applying new techniques & concepts in
the from of NDDS
↑ expenses for developing New Drug Candidates (NDC cost ≈ $2 billion;
NDDS ≈ $20O Million)
To deliver novel, genetically engineered pharmaceuticals
(peptides/proteins/genes) to their site of action without significant
immunogenic / biological inactivation
Better targeting with NDDS for treatment of enzyme deficiency diseases
/ cancer therapy
↑ therapeutic efficacy (↓ dose) & safety of drugs compared to
conventional d.f by more precise spatial and/or temporal placement in
the body
Novel Drug Delivery System
“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.
It may involve scientific site-targeting within the
body, or it might involve facilitating systemic
pharmacokinetics; in any case, it is typically
concerned with both quantity and duration of drug
presence”.
Novel Drug Delivery System
Novel Drug delivery is often approached via a drug's
chemical formulation, but it may also involve medical
devices or drug-device combination products. Drug
delivery is a concept heavily integrated with dosage
form and route of administration.
NDDS is advanced drug delivery system which
◦ improves drug potency,
◦ control drug release to give a sustained therapeutic effect,
◦ provide greater safety,
◦ finally it is to target a drug specifically to a desired tissue.
Novel Drug Delivery System
NDDS is a system for delivery of drug other than
conventional drug delivery system.

NDDS is a combination of advance technique and

new dosage forms which are far better than
conventional dosage forms.
Terminology
Controlled Drug Delivery System
◦ Systems which can provide some control, either TEMPORAL or SPATIAL or
both, of drug release in body
◦ OR
◦ It refers to the precise control of the rate by which a particular drug dosage
is released from a DDS (ideally at a constant / near constant manner) for a
prolonged period of time without the need for frequent, repeated
administration either orally / parenterally
Terminology
Sustained Release System
◦ Systems designed to achieve a prolonged therapeutic effect by continuously
releasing medication over an extended period of time so that a relatively
constant, effective drug level in the body with concomitant minimization of
undesirable side effects associated with a saw tooth pattern of plasma drug
level.
Terminology
Delayed Release Systems
◦ Systems that are either those that use repetitive, intermittent dosing of a
drug from one or more immediate-release units incorporated into a single
dosage form, or an enteric delayed release system.
◦ E.g., repeat-action tablets and capsules, and enteric-coated tablets where
timed release is achieved by a barrier coating.
Terminology
Extended Release Systems
◦ Systems that include any dosage form that maintains therapeutic blood or
tissue levels of the drug for a prolonged period.
◦ If the system can provide some actual therapeutic control (temporal / spatial
/ both), of drug release in the body, it is considered a controlled delivery
system. This explains why extended-release is not equivalent to controlled-
release.
 Terminology
Targeted Delivery Systems
◦ Systems that target a drug directly to a certain biological location
◦ Site-specific release - the target is adjacent to or in the diseased organ or
tissue;
◦ Receptor release - the target is the particular drug receptor within an organ
or tissue.
TYPES

◦ Both of these systems satisfy the spatial aspect of drug delivery requirement
and are also
considered controlled drug delivery systems.
Rational for NDDS
To alter PK/PD of API by
◦ Using novel techniques in NDDS
◦ Modifying the chemical structure (prodrugs / soft drugs / co-drugs)
◦ Modifying physiological parameters inherent in the selected route of
administration

E.g, DOA of a drug becomes a design property of a CRDDS

rather than that of drug’s inherent kinetic property. Hence,
optimal design of a CRDDS necessitates a thorough
understanding of the drug’s PK/PD.
Rational for NDDS
The primary objective of CRDDS is to ensure safety and to improve
efficacy of a drug as well as to increase patient compliance. This is
achieved by better control of Cp and with less frequent dosing.
Advantages of NDDS
↑ patient compliance
↓ dose & frequency of dosing
↓ local / systemic side effects
Minimize drug accumulation (with chronic use)
↓ potentiation / loss of drug activity (with chronic use)
↑ in treatment efficacy
↑ in speed of control of medical condition
↓ in blood level fluctuations
↑ bioavailability
↑ in ability to provide special benefits
↓ in cost of therapy (Pharmacoeconomic advantage)
DISADVANTAGES OF NDDS
Chances of dose dumping
Less accurate dosage adjustment
↑ potential for First-pass metabolism
Dependence on residence time at site of action (e.g., in the GIT)
Delayed onset (for SRDDS)
↑ cost of unit dose
Unpredictable / poor IVIVC
Where drugs cannot be formulated as
CRDDS
CRITERIA EXAMPLES
• Drugs with long t½ (>12 hr) Diazepam, Phenytoin
• Drugs with narrow TI Theophylline digitoxin,
Phenobarbital
• Where GIT limits absorption (Oral route) Penicillin G, Peptides
• High dose formulations Sulfonamides
• Where cost of d.f. is exorbitant
• Extensive First-pass metabolism Verapamil
• Inadequate absorption in lower intestine Riboflavine, Ferrous salts
• Drugs with rapid absorption / excretion or have very Penicillin G, Furosemide
short t½ (< 1 hr)
• Where individualized therapy (precise dose titration Anticoagulants, Cardiac
is needed) glycosides
• Drugs with low aqs. Solubility / active absorption Vitamins, Some anticancers
• Where no clear advantage of CRDDS is indicated Griseofulvin