PH1.3 Enumerate and identify drug formulations and drug delivery systems

1. PH1.3 Enumerate and identify drug
formulations and drug delivery systems
Dr Pankaj Gupta, MD
Assistant Professor,
Department of Pharmacology
Al Falah School of Medical Science & RC
Faridabad (HARYANA)

2. Learning Objectives
• Difference between dosage form & formulation
• What is drug delivery & drug delivery systems
• Difference between conventional & newer drug
delivery systems
• Newer drug delivery systems, their advantages &
disadvantages
• Any question

3. Dosage form Versus Formulation
• Dosage form: is a product suited for
administration to the patient by various routes
for diagnosis or treatment. They provide
accurate dosage of drugs for the treatment of
disease. Eg: Tablet, Capsule.
• Formulations: it consist of name of drug,
strength and its dosage form. Eg: Ibuprofen
400 mg as tablet
Srivastava SK, Srivastava Rohan. Manual of practical pharmacology for MBBS, First Edition 2021. Avichal Publishing Company.

4. •Dosage form= Drug (API) + Excipients
•Formulation= Dosage form (Drug + Excipients) + Drug strength
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/

5. Drug delivery
• A method or a process of administering or
delivering a pharmaceutical compound in
systemic circulation to achieve its therapeutic
effect in humans or in animals.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3465154/

6. What are drug delivery systems?
• Drug delivery systems are engineered technologies for
the targeted delivery and/or controlled release of
therapeutic agents.
• Many drugs have unacceptable side effects due to the
drug interacting with healthy tissues that are not the
target of the drug. Side effects limit ability to design
optimal medications for many diseases such as cancer,
neurodegenerative diseases, and infectious diseases.
• Drug delivery systems control the rate at which a drug
is released and the location in the body where it is
released. Some systems can control both.
https://www.nibib.nih.gov/science-education/science-topics/drug-delivery-
systems-getting-drugs-their-targets-controlled-manner

7. What are drug delivery systems?
Any drug delivery system may be defined as a system comprising
of:
– Drug formulation
– Medical device or technology to carry the drug inside the
body
– Mechanism for the release
https://www.nibib.nih.gov/science-education/science-topics/drug-delivery-
systems-getting-drugs-their-targets-controlled-manner

8. Types of drug delivery system (DDS)
• Conventional/traditional drug delivery system
• Novel drug delivery system
https://www.pharmapproach.com/drug-delivery-systems-an-overview/

9. Conventional/traditional drug delivery system
• Conventional DDSs are classical methods for delivery of a drug
into the body.
• These systems are used more often when the goal is quickly
absorption of a drug; therefore, a quick release of the drug is
required.
• Example:- conventional drug delivery forms include simple
oral, topical, inhaled, or injection methods.
https://www.pharmapproach.com/drug-delivery-systems-an-overview/

10. Various routes & conventional/traditional drug
delivery system
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/

11. Limitations of Conventional drug delivery systems
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/

12. Ideal characteristics of drug delivery systems
• It should increase the bioavailability of the drug.
• It should transport the drug intact to the site of action
while avoiding the non-diseased host tissue.
• The product should be stable and delivery should be
maintained under various physiological variables.
• A high degree of drug dispersion.
• The same method should be applicable to a wide range
of drugs.
• It should be easy to administer to the patient.
• It should be safe and reliable.
• It should be cost-effective.
https://www.pharmapproach.com/drug-delivery-systems-an-overview/

13. Novel drug delivery systems (NDDS)
• A combination of advanced techniques and new
dosage forms to introduce better drug potency,
control drug release, provide greater safety, and
target a drug specifically to a desired tissue.
• NDDSs lead to efficient use of expensive drugs and
excipients, and reduce in production cost.
• NDDS brings better therapy by improved comfort
drug delivery devices which increase the standard of
living.
https://www.pharmapproach.com/drug-delivery-systems-an-overview/

14. Targeted drug delivery
Targeting is the ability to direct the drug-loaded system to the site
of interest. Two major mechanisms can be distinguished for
addressing the desired sites for drug release:
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

15. Therapeutic benefits of new systems
(Controlled drug release systems and targeted drug delivery systems)
• Increased efficacy of the drug
• Site specific delivery
• Decreased toxicity/side effects
• Increased convenience
• Viable treatments for previously incurable
diseases
• Potential for prophylactic applications
• Better patient compliance.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

16. Various Drug Delivery Systems
(For controlled and targeted delivery of drug)
Carrier based Drug Delivery System:
•Liposomes
•Nanoparticles
•Microspheres
•Monoclonal antibodies
•Niosomes
•Resealed erythrocytes as drug carriers
Trasdermal Drug Delivery Systems:
•Sonophoresis
•Mucoadhesive delivery systems
•Supramolecular delivery systems
•Variable release delivery systems
•Osmotic pump
•Microencapsulation
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

17. Drug Delivery Carriers
• To obtain systems with
– Optimized drug loading and release properties
– Long shelf-life
– Low toxicity
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

18. • Liposomes: Liposomes are a form of vesicles that consist either of many, few
or just one phospholipid bilayers. The polar character of the liposomal core
enables polar drug molecules to be encapsulated.
• Nanoparticles: Nanoparticles (including nanospheres and nanocapsules of
size 10-200nm) are in the solid state and are either amorphous or crystalline.
They are able to adsorb and/or encapsulate a drug, thus protecting it against
chemical and enzymatic degradation.
• Microspheres: Microspheres are characteristically free flowing powders
consisting of proteins or synthetic polymers which are biodegradable in nature
and ideally having a particle size less than 200 μm.
• Resealed Erythrocytes as Drug Carriers: Erythrocytes, the most abundant
cells in the human body, have potential carrier capabilities for the delivery
of drugs. Erythrocytes are biocompatible, biodegradable, possess very
long circulation half lives and can be loaded with a variety of chemically
and biologically active compounds using various chemical and physical
methods.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

19. Examples of nanocarriers in controlled drug delivery
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/

20. Properties of resealed erythrocyte of novel drug
delivery carriers
• The drug should be released at target site in a controlled manner.
• It should be appropriate size, shape and should permit the passage
through capillaries. And Minimum leakage of drug should take place.
• It should be biocompatible and should have minimum toxic effect.
• It should possess the ability to carry a broad spectrum of drug.
• It should possess specific physicochemical properties by which desired
target size could be recognized.
• The degradation product of the carriers system, after release of the drug
at the selected site should be biocompatible. It should be physico -
chemically compatible with drug.
• The carrier system should have an appreciable stability during storage.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

21. • Niosomes: the vesicles forming amphiphile is a non-ionic surfactant such as
Span – 60 which is usually stabilized by addition of cholesterol and small amount
of anionic surfactant such as dicetyl phosphate.
• Niosomes and liposomes are equiactive in drug delivery potential and both
increase drug efficacy as compared with that of free drug.
• Niosomes are preferred over liposomes because the former exhibit high chemical
stability and economy.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

22. Liposomal drug delivery system available in market

24. Transdermal Drug Delivery System
• Defined as self contained, discrete dosage forms which, when
applied to the intact skin, deliver the drug, through the skin at
controlled rate to the systemic circulation.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

25. Advantages
– Avoidance of first pass metabolism
– Avoidance of gastro intestinal incompatibility
– Predictable and extended duration of activity
– Improving physiological and pharmacological response
– Termination of therapy is easy at any point of time
– Greater patient compliance due to elimination of multiple
dosing profile
– Provide suitability for self administration
– Enhance therapeutic efficacy
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

26. Sonophoresis
• It is a process that exponentially increases the
absorption of topical compounds (transdermal
delivery) into the epidermis, dermis and skin
appendages by ultrasonic energy.
• Sonophoresis is a localized, non‐invasive, convenient
and rapid method of delivering low molecular weight
drugs as well as macromolecules into the skin.
• Ultrasound at various frequencies in the range of 20
kHz–16 MHz with intensities of up to 3W/cm2 are
being used for sonophoresis.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

27. Marketed Transdermal drug delivery product

28. Osmotically Controlled Drug Delivery Systems
• Osmotic pressure is used as driving force for these systems to
release the drug in controlled manner .
Classification of Osmotic Drug Delivery System:
They can be divided in oral and implantable systems
Implantable:
•The Rose and Nelson Pump
•Higuchi Leeper Pump
•Higuchi Theuwes pump
•Implantable Miniosmotic pump
Oral osmotic Pump
•Single chamber osmotic pump
•Elementary osmotic pump
•Multi chamber osmotic pump
•Push pull osmotic pump
•Osmotic pump with non expanding second
chamber
•Specific types:
•Controlled porosity osmotic pump
•Osmotic bursting osmotic pump
•Liquid OROS
•Delayed Delivery Osmotic device
•Telescopic capsule
•Oros ct (colon targeting)
•Sandwiched oral therapeutic system
•Osmotic pump for insoluble drugs
•Monolithic osmotic system and OSMAT
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

29. Osmotic Pressure Controlled
Gastrointestinal Delivery System
• These are systems fabricated by encapsulating an osmotic
drug core containing an osmotically active drug within a semi
permeable membrane made from biocompatible polymer eg-
cellulose acetate
Osmotic pressure controlled drug delivery system (Elementary Osmotic Pump)

30. Advantages of Osmotic Drug Delivery System
• They typically give a zero order release profile after an initial lag.
• Deliveries may be delayed or pulsed if desired.
• Drug release is independent of gastric pH and hydrodynamic condition.
• They are well characterized and understood.
• The release mechanisms are not dependent on drug.
• The rationale for this approach is that the presence of water in GIT is relatively
constant, at least in terms of the amount required for activation and controlling
osmotically base technologies.
• Higher release rates are possible with osmotic systems compared with
conventional diffusion-controlled drug delivery systems.
• The release from osmotic systems is minimally affected by the presence of food in
gastrointestinal tract.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

31. Disadvantages
• Expensive
• If the coating process is not well controlled there is a risk of film defects,
which results in dose dumping
• Size hole is critical
• Dose dumping
• Retrieval therapy is not possible in the case of unexpected adverse events.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

32. Marketed products of osmotic pump

33. ViadurTM implant is used for prostate cancer and after insertion it is effective for 12 months

34. Microencapsulation
• Process in which small droplets or particles of liquid or solid
material are surrounded or coated by a continuous film of
polymeric materials.
• Microencapsulation process helps for converting the liquids to
solids, changing the colloidal and surface properties, providing
environmental protection and controlling the release
characteristics of different coated materials.
http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-overview/?view=fulltext

35. Microencapsulation Technology

36. Example of marketed Microencapsulation product

37. References
• Srivastava SK, Srivastava Rohan. Manual of practical pharmacology for
MBBS, First Edition 2021. Avichal Publishing Company.
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8512302/
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3465154/
• https://www.nibib.nih.gov/science-education/science-topics/drug-
delivery-systems-getting-drugs-their-targets-controlled-manner
• https://www.pharmapproach.com/drug-delivery-systems-an-overview/
• http://ijpsr.com/bft-article/novel-drug-delivery-systems-an-
overview/?view=fulltext

39. Thanks