Modified release drug products, Targeted Drug Delivery Systems and Biotechnological Products(application of biopharmaceutics)

1. Presented By,
Mr. Chavan saurav Rajendra
Roll no. 102
First Year M. pharm (Pharmaceutics)
Semester –II
STES’s Smt . Kashibai Navle College of Pharmacy Kondhwa
(BK) Pune -411048
Guided by,
Mrs. Pallavi Chede
(M.Pharm )
Assistant professor
Department of Pharmaceutics
TOPIC
Modified–release drug products, targeted drug delivery systems and
biotechnological products.
1

2. Contents:-
●Introduction
●Variables to consider for modified release dosage Form
●Advantages
●Disadvantages
●Types of modified release oral drug products
●marketed examples
●Targeted drug delivery system
●Need of Targeted drug delivery system
●Ideal characteristics of Targeted drug delivery system
●Advantages Of Targeted drug delivery system
●Disadvantages of Targeted drug delivery system
●various approaches for Targeted drug delivery system
●Biotechnological products
●Case study of Alpress®L.P.
●References
2

3. Introduction:-
●Most conventional (immediate release) oral drug products, such as tablets and capsules,
are formulated to release the active drug immediately after oral administration.
●In the formulation of conventional drug products, no deliberate effort is made to modify
the drug release rate.
● Immediate-release products generally result in relatively rapid drug absorption and
onset of pharmacodynamic effects.
●A modified release drug product refers to a medication that is formulated to release its
active ingredient(s) in a controlled manner over an extended period of time, as opposed to
immediate release formulations that rapidly release the drug upon administration.
●Modified release formulations are designed to optimize drug absorption, maintain
therapeutic drug levels in the body, and reduce the frequency of dosing.
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4. Variables to consider for modified release dosage form:
1. Low dose
2. Short half life
3. Wide Therapeutic Window
4. Absorbed through the entire GI
5. Modest to rapid absorption
6. Highly stable in the GI
7. Chronic treatment
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5. Advantages:
1. Increased time within the Therapeutic Window due to lower peak plasma
concentration and shallower slope
2. Reduce dosing frequency
3. Improve patient compliance
4. Reduce gastric irritation and side effects
5. Possible to enhance the bioavailability
6. Alleviate the risk of dose dumping
7. Reduce fluctuation in circulation drug level
8. Avoidance of night time dosing
9. More uniform effect 5

6. Disadvantages:
1. If a toxic dose is given, it will stay toxic for a long time
2. Takes a long time to titrate patient
3. Strong first pass effect by staying below the metabolizing enzymes saturation point
4. Risk of Dose Dumping (failed delivery device) a large immediate dose
5. Inflexible dosing schedule
6. Can't usually split tablets
6

7. Types of modified-release oral drug products :-
1) Extended-release drug products
2) Delayed-release drug products
3) Targeted-release drug products.
4) Orally disintegrating tablets (ODT)
5)Osmotic drug delivery system
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8. Extended-release drug products:-
This are designed to release the medication into the body over an extended period of
time, providing a sustained and controlled release of the active ingredient. This
allows for less frequent dosing compared to immediate-release formulations. The
extended-release mechanism can be achieved through various technologies, such as
matrix systems, osmotic pumps, or coated beads, which control the drug release
rate.
Delayed-release drug products:-
Delayed-release drug products are designed to release the medication at a specific
time or location in the digestive system, usually to protect the drug from degradation
by stomach acid or to target a specific site in the gastrointestinal tract. These
formulations use enteric coatings or other technologies that resist dissolution in the
acidic environment of the stomach but dissolve or release the drug in the more
alkaline environment of the small intestine.
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9. Targeted-release drug products:
Targeted-release drug products aim to deliver the medication to a
specific site or tissue within the body. These formulations often utilize
specialized drug delivery systems or carriers that can specifically target
the desired location while minimizing the drug's exposure to other
tissues or organs. Targeted-release systems can be designed for various
routes of administration, such as oral, injectable, or topical.
Orally disintegrating tablets (ODT):
Orally disintegrating tablets, also known as quick-dissolving or fast-
dissolving tablets, are solid dosage forms that rapidly disintegrate or
dissolve in the mouth without the need for water. These tablets are
particularly useful for patients who have difficulty swallowing
conventional tablets or for situations where immediate drug action is
desired. ODTs can be prepared using technologies like lyophilization.
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10. Osmotic drug delivery system:-
Osmotic drug delivery systems are specialized formulations designed to deliver
drugs in a controlled and predictable manner over an extended period of time. These
systems utilize osmotic pressure as the driving force for drug release. When the
osmotic drug delivery system comes into contact with aqueous fluids, water
permeates through the semi-permeable membrane into the osmotic core due to the
osmotic gradient created by the osmotic agents. As water enters the osmotic core, it
creates pressure that causes the core to expand. This expansion leads to the drug
being pushed out through the delivery orifice at a controlled rate.
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11. Marketed examples :-
Sr no. Types of modified release
oral drug products
Marketed examples
1) Extended release
1) Sustained release
2) Controlled release
JENBRO-200SR
Flamace CR 200
2) Delayed release Meslataj DR 400mg
3) Target release Proscar®
4) Orally disintegrating
tablet’s
NRZOF-MD
5) Osmotic drug delivery Alpress LP
11

12. Targeted drug delivery system :-
●The conventional drug delivery system involves the absorption of the drug across a
biological membrane, where as the targeted release system releases the drug in a dosage form
at targeted site.
●Targeted drug delivery is a special from of drug delivery system where the medicament is
selectively targeted or delivered only to the site of action and not to the non-targeted organs
or tissues or cells.
●The system is stand on a method that delivers a certain amount of a therapeutic agent for a
prolonged period of time to a targeted diseased area within the body and improves the
efficacy and reduces the side effect.
●This helps maintain the required plasma and tissue drug levels in the body, thereby
preventing any damage to the healthy tissue via the drug.
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13. ●Carriers used should be biodegradable or readily eliminated from the body without any
problem.
●The preparation of the targeted drug delivery system should be simple, reproductive and
cost effective.
●Targeted drug delivery has high solubility and more drug stability as compare to
conventional drug delivery.
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14. Need of targeted drug delivery system:-
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15. Ideal characteristics of Targeted drug delivery system:-
●It should be non-toxic and Non-immunogenic.
●It should be physically and chemically stable in vivo and in vitro.
●They control the drug distribution to target cells or tissues or organs.
●Must have uniform capillary distribution.
●Convenient and predicate rate of drug release.
●Drug release does not influence the drug action.
●Carriers used must be bio-degradable or readily eliminated from the body without
any problem and no carrier induced modulation of diseased state.
●The preparation of the delivery system should be easy or reasonably simple,
reproductive and cost effective. 15

16. Advantages of Targeted drug delivery system:-
●Drugs deliver / releases over extended period of time.
●Intermittent dosing can be avoided.
● Improve patient compliance.
●Reduce inter and intra-patient variability.
●Drug can be administered in a smaller dose to produce the desired effect.
● Toxicity is reduced by delivering drug at the targeted site.
● Self administration is possible.
●Enhance absorption of drug.
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17. Disadvantages of targeted drug delivery system:-
●Requires a skill in manufacturing storage, administration.
●Diffusion and redistribution of drug release
●Rapid clearance of targeted systems.
●Maintaining stability of dosage form is difficult.
●Highly sophisticated technology requires for formulation.
●Expensive.
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18. Various Approaches for targeted drug delivery system:-
1) Nanoparticals
2) lyposomes
3) Antibody drug conjugets (ADC)
4) microneedles
5) microspheres and microcapsules
18

19. Nanoparticles:-
●Nanoparticles can be engineered to
encapsulate drugs and deliver them to specific
sites in the body.
●They can be made from various materials such
as lipids, polymers, or metals.
●Nanoparticles can be designed to release the
drug payload gradually or in response to
specific stimuli such as changes in pH,
temperature, or enzyme activity.
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20. Liposome:-
●liposome based targeted drug delivery systems are
a type of drug delivery technology that utilize
liposomes as carriers to transport drugs to specific
target sites in the body.
● Liposomes are artificial vesicles composed of
lipid bilayers, similar to the structure of cell
membranes.
●The main advantage of liposomes as drug carriers
is their ability to encapsulate both hydrophilic
(water-soluble) and hydrophobic (fat-soluble) drugs
within their aqueous core or lipid bilayers,
respectively.
●This flexibility allows liposomes to deliver a wide
range of therapeutic agents, including small
molecules, proteins, nucleic acids, and peptides. 20

21. Antibody-drug conjugates (ADCs) :-
●it is a type of targeted drug delivery system designed
to combine the specificity of antibodies with the
potency of cytotoxic drugs.
●They are engineered molecules that consist of three
main components: an antibody, a linker, and a cytotoxic
drug.
●The antibody component of an ADC is a monoclonal
antibody that specifically recognizes and binds to a
target antigen found on the surface of cancer cells or
other diseased cells.
●The linker is a chemical bridge that connects the
antibody and the cytotoxic drug. It is designed to be
stable in circulation but can be cleaved or degraded
under specific conditions once the ADC reaches its
target site. 21

22. Microneedles:
●Microneedles are tiny needles typically
ranging from hundreds of micrometres to a
few millimetres in length.
●They can be used to painlessly penetrate the
skin and deliver drugs to a specific depth,
allowing targeted delivery to specific tissues
or cells.
●They consist of an array of tiny needles,
which can penetrate the outermost layer of
the skin.
●microneedles have demonstrated great
potential as a promising technology for
targeted drug delivery systems.
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23. Microspheres and microcapsules:-
●This are important components of targeted drug delivery
systems. They are designed to encapsulate therapeutic
agents, such as drugs or biological molecules, and deliver
them to specific target sites in the body.
●These systems offer several advantages over
conventional drug delivery methods, including controlled
release, improved drug stability, reduced side effects, and
enhanced efficacy.
● Microspheres and microcapsules are spherical particles
with diameters typically ranging from a few micrometres
to several hundred micrometres.
●They can be made from various materials, such as
natural or synthetic polymers, lipids, or proteins.
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24. Biotechnological products:-
●Biotechnology products means those products that are applicable to the prevention,
treatment, or cure of a disease or condition of human beings and that are produced
using living organisms, materials derived from living organisms, or cellular,
subcellular, or molecular components of living organisms.
●These are those products which are manufactured by recombinant DNA technology
(basically produced by Biotechnology).
●Biotechnology utilizes living organisms or their components to develop products or
processes for various industries, including medicine, agriculture, food production.
●Examples: Antibiotics, vaccines, Genetically Modified Organisms (GMO's),
transgenic plants, beverages etc.
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25. Genetically Engineered Antibiotics:-
●Biotechnological products have revolutionized the field of
antibiotics by enabling the development of new and more
effective drugs.
●Biotechnology allows scientists to manipulate the genetic
makeup of microorganisms to produce novel antibiotics.
● For example, genetically modified bacteria or fungi can be
designed to produce specific antibiotics in large quantities.
●This approach has led to the development of antibiotics like
vancomycin, which is produced by a genetically engineered
strain of bacteria(Amycolatopsis orientalis).
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26. Vaccines:-
●Biotechnological products have played a crucial
role in the development and production of
vaccines.
●Vaccines are created to stimulate an immune
response in the body, helping to protect against
specific diseases.
● Biotechnology has provided innovative
techniques and tools that have greatly advanced
the vaccine development process.
●Recombinant DNA technology involves
combining genetic material from different sources
to create novel genetic sequences. This technology
has been used to produce recombinant subunit
vaccines.
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27. GENETICALLY MODIFIED ORGANISMS (GMO’S):
●A GMO, or genetically modified organism is a plant, animal,microorganism or
other organism whose genetic makeup has been modified in a laboratory using
genetic engineering or transgenic technology.
●This creates combinations of plant, animal, bacterial and virus genes that do not
occur in nature or through traditional crossbreeding methods.
●GMOs have been created for various purposes, including improving crop yield,
enhancing nutritional content, increasing resistance to pests, diseases, or
environmental conditions, and producing pharmaceuticals.
●Types:-
1) Genetically Modified Animals
2) Genetically Modified Bacteria
3)Genetically Modified Plants
4)Genetically Modified Flowers
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28. Dolly Sheep
Ice-minus Bacteria
Carnation
Flower
Genetically
Modified Crop
Figure : Genetically modified plant, animal, flower and bacteria
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29. Case study of Alpress® L.P.
●product name :- Alpress L.P. 5mg
●Active ingredient :- prazosine
●Manufacturer /marketer:- Pfizer
●The Alpress is a modified release dosage form and comes
under osmotic drug delivery system (ODDS).
●The advantage of the Alpress L.P. system is its ability to
deliver drugs in a controlled manner, ensuring a constant
therapeutic effect and reducing the need for frequent dosing.
●It can be particularly beneficial for drugs that require steady
blood levels or for patients who have difficulty adhering to a
frequent dosing schedule.
●Dosage:-5mg/day
●Special warnings and precautions for use:-
●In order to have its full antihypertensive effect, the prolonged
release prazosin tablet requires the gastrointestinal transit time
to be normal. If the transit time is shortened, the
pharmacokinetic and pharmacodynamic profile may be
changed, reducing the hypertensive efficacy. 29

30. ●Mechanism of action:-
●The Alpress ODDS consists of a drug reservoir, a
semipermeable membrane, and an osmotic engine.
●The drug reservoir contains the medication to be
delivered, while the semipermeable membrane allows for
the passage of water but not the drug molecules.
●The osmotic engine creates a pressure gradient within
the device, driving water into the reservoir through
osmosis.
●As water enters the reservoir, it creates hydrostatic
pressure, which pushes the drug solution out of the system
through a small orifice or delivery port.
●Usage:-Raynaud Disease, Hypertension, Secondary
Hypertension, Benign Prostatic Hyperplasia, Congestive
Heart Failure, Heart Failure.
● adverse effects:- Orthostatic hypotension
●conclusion:-The adverse effects of hypotension may
occur occasionally with ALPRESS LP but there’s is not
require step-wise dose increases or attentive medical
supervision of patients when the treatment is started. 30

31. Reference:-
1)Nalla chandaha, Harish Gopinath, Debjit Bhowmik, wiliamkeri, Thirupathi Reddy
A. Modified release dosage forms.Journal of chemical and pharmaceutical Sciences
Jan- march 2016, Vol 6, page no-13-21.
2) Magoba shivappan, Warkari Rajah.D.,chandrawanshi mayuri I. Bhalekar Rohini
V. viayjendra swamy S.M. A Review on targeted. drug delivery. American Journal
of pharmaceutical research, June 2018, vol4, page no:- 1-11.
3) A. V. Yadav, S. P. Yadav, and R. K. Singh. "Modified-release drug delivery
technology," International Journal of Pharmaceutical Sciences and Research,may
2012. Page no:- 23-34
4) S. S. Patel, D. R. Patel, and M. K. Patel. Recent advances in modified release
drug delivery systems, Journal of Controlled Release, June 2011,Vol 5,page no 81-
99.
5) K. Rani and S. Paliwal, “A review on targeted drug delivery: Its entire focus on
advanced therapeutics and diagnostics,” Scholars Journals of Applied Medical
Sciences, 2014 31

32. 6)Sriharitha, Preethi J, Hemanth Swaroop A Review on Nanoparticles in targeted
drug delivery system Research and Review : Journal of Material Science 2014
7)Priyanka R Kulkarni, Jaydeep D Yadav, Kumar A Vaidya Liposomes: A Novel
Drug Delivery System International Journal of Current Pharmaceutical Research
2011.
8) Brahmankar HA, Jaiswal SB, Biopharmaceutics and Pharmacokinetics A
Treatise, Vallabh Prakashan, 2000, 337, 348-357
9) N. K. Jain Introduction to novel drug delivery systems Vallabh prakashan First
edition 2010 page no 118- 134.
10) https://labeling.pfizer.com/ShowLabeling.aspx?id=15060
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