REVIEW ON NOVEL ADVANCEMENT IN DRUG FORMULATIONS

1. Recent Advancement In Formulation
Development
PRESENTED BY
DR. HARSHIKA PATEL
PHARMACOLOGY DEPARTMENT
KENYA MENTHODIST UNIVERSITY

2. INTRODUCTION
• Pharmaceutical formulations is “a process where different chemicals
compounds admixture with active pharmaceutical ingredients and
form a final stable medical product”.
• “The aim of Novel, advance formulation is to provide a therapeutic
amount of drug to the appropriate site in the body to accomplish
promptly and then maintain the desired drug concentration with
minimum side effects.”
• It also provides the target delivery system with less systemic effects.

3. What is the Need to develop a novel
formulation?
The novel evolution might have following characteristics:
Dosing frequencies are lesser with improved bioavailability of the drug.
Reduce the side effects.
Improve the target delivery of the active ingredients.
Improve the stability of active compound and control the release of potent
drug.

4. To get that several factors to be considered
Physical, chemical, and mechanical properties of
drug substance
Polymorphism, solubility, pH, and particle size of
drug
Inactive ingredients or excipients in the
formulation
Drug stability studies for better shelf life of drug
Patient factors

5. Basic Types of Formulations
Types Examples Characteristics
Enteral Tablets, Capsules, syrups,
solutions, etc
Forms rapid effects and sustained
release effects through gastrointestinal
track
Parenteral Liquid and lyophilized
materials are involved
Use for Intravenous, intra-articular,
subcutaneous, intramuscular,
Liquids: preserved in ampules, vials
prefilled syringes
Lyophilized : available In dual chamber
syringes, cartridges, vial
Topical Creams, ointment, For skin / superficial

6. BENEFITS Medical
Optimum
dose , at the
right time and
at the right
target
Industrial
Efficient use of
expensive
ingredients,
reduction in
production cost
Social
Beneficial to
patients, better
therapy, improved
compliance and
standard of living

7. Excipients
• Have vital role to improve the pharmacological
parameters of pharmaceutical active ingredients.
• That’s improve the patients compliance indirectly.
• The history indicates it’s importance well, minor exchange
in this excipient causes great disasters.

8. Various formulations available and
constantly growing
1. Modified-release drug formulations-Sustained and Controlled
Polymers, Micelles, Liposomes, Ethosomes
Nanotechnology
2. Prodrugs
3. Transdermal Drug delivery systems
4. Ocusert
5. Insulin jet and Micro pump controlled delivery system
6. Patient controlled analgesia(PCA)
7. Drug eluting stents
8. Gene therapy
9. Personalised medicine

9. List of drug carriers in
NDDS
• Nanosomes
• Liposomes
• Niosomes
• Nanoparticle
• Nanosphere
• Microsphere
• Microparticle
• Microemulsion
• Nanosuspension
• Micelles
9
Novel polymers are Biodegradable and
biocompatible

10. Nanotechnology Based Formulations

13. Many novel formulations with old
generic drugs
(with increased the drug effectiveness)

14. Modified-release drug formulations-
Sustained and Controlled manner
Oral formulations: High risk of compliance
Types
Enteric and reverse enteric
coating  delayed release via
pH
Sustained release
Matrices, osmotic, inserts
Pulsatile release
Beads , mini tablets
(ODMT)

15. Matrix Diffusion
Types
Rigid Matrix Diffusion
Swellable Matrix Diffusion
Reservoir System
Dissolution
Matrix
Type
Dissolution
& Diffusion
Controlled
Release
System
Water
penetration/
Osmotic
Pressure
Controlled
Chemically
controlled
NDDS
Hydrogels
Ion Exchange
Resins
Controlled
Release
Systems
Types
Modified
release
formulation

16. Sustained release formulation- Ocular system
• Glaucoma Sustained-release modalities is Allergan’s Bimatoprost SR
implant, favorable safety and efficacy through 6 months. (under phase 3
CT)
• Dexycu (dexamethasone intraocular suspension 9%)  post-cataract
inflammation
• Yutiq (fluocinolone acetonide intravitreal implant 0.18mg) non-
infectious posterior uveitis
• Dextenza (dexamethasone ophthalmic insert 0.4 mg)  ocular pain
following surgery
•
https://crstodayeurope.com/articles/2019-june/ophthalmic-drug-delivery-history-status and-trends-for-the-future/#

17. Ocular insert - Occusert
To increase the contact time between the preparation and the
conjunctival tissue to ensure a sustained release suited to topical or
systemic treatment.

18. Oral formulations
• Immediate release (IR) Tablets & Capsules
• Modified release (MR) Tablet and Capsules
• Orally disintegrated tablet
• ODMT – oral disintegrated mini tablet for pediatric (for even 6month
old) and geriatric use
• Two properties where combined ODT and small size tab (2-4 mm)
(T Comoglu, E Dilek Ozyilmaz 2019)
• Buccal/sublingual tablet
• Oral thin films
• Oral liquids
• Others: Sprays, Lozenges, Gums, Granules, Effervescent Tablet

19. Prodrugs

20. Parenteral formulation
Key considerations
• Sterilization for microbes, endotoxins, particulate matter
• Stability of formulation on chemical, physical, extractable and leachable
• Isotonicity, pH, volume of administer of the product which can damage
the cell and cause pain
• Viscosity of the formulations  think about the capacity of syring

21. Route of drug administration
• Intravenous:
Injections/ Infusion
Lyophilized powder for reconstitution
Solution for injection
• Intramuscular:
Rapid or sustained release, depot ppn are available
• Subcutaneous Injection (for antibody and diabetes therapy)
Self medication possible
Prefilled syringes are available (for life threatening condition)
Insulin pumps, autoinjector, pen injector

22. Emerade, EpiPen and Jext.
Bolus injector
Micro pump insulin

23. Patient controlled analgesia pump
• Patient can control the release of analgesic
drug depending on the pain.
• Patient’s IV line is used.
• Applications
• Post-operative pain management
• End-stage cancer patients
• The infusion is programmable by the
prescriber.
• Must always observe the first administration to
allergic reactions.
A patient-controlled analgesia infusion
pump, configured for epidural
administration of fentanyl and bupivacaine
for postoperative analgesia

24. Nasal Drug formulations
• Can be systemic or local
• Required potent drug  effect is very rapid
• Local irritations
• Formulation:
• Solution, suspension  nasal spray
• Dry powders
• Peptide delivery (nano particles)
• Inhalers

25. Transdermal DDS
Active ingredient is delivered across the skin for systemic distribution.
Example: transderm scopolamine, nitroglycerine , nicotine, Fentanyl
Transdermal-SCOP
(scopolamine) for motion
sickness
Hydrogel transdermal patch –
for burns

26. Merits of transdermal DDS
Avoid the risk and inconveniences associated with parenteral/ oral
routes.
Increase the bioavailability – bypassing hepatic first pass metabolism
Bypass the variation in absorption and metabolism.
continuous drug administration
Reduce the chance of over or under dosing

27. Drug Eluting Stents
• First generation DES: stainless steel scaffolding  RAVEL, SIRIUS, and TAXUS 
Paclitaxel-Eluting Coronary Stent System, which releases paclitaxel/ sirolimus
• Second generation: cobalt-chromium scaffolding with different polymer
• Third generation of DES with a biodegradable polymer or entirely bioabsorbable
scaffolds
• It placed within the peripheral or coronary artery by an interventional cardiologist or
interventional radiologist during an angioplasty procedure.
https://www.ncbi.nlm.nih.gov/books/NBK537349/#:~:text=Drug%2Deluting%20stents%20(DES),stent%20(BMS)%20in%201986.

28. Gene Therapy -Genetic Transfer System
Under evaluation & III Phase clinical trials are going on for
Adenovirus & HIV

29. Personalized medication : Ultimate goal
of new drug delivery formulations
Means prescription of specific treatment and therapeutics best suited for an
individual.
It is also referred to as individualized or individual based therapy based on
the patient genotype, circadian rhythm, biochemical and hematological
parameters.
Example: Isoniazid , Sch , G-6PD, pglycoprotein, Malignant hyperthermia by
halothane

30. Risk factors or disadvantages
• Physical. Chemical, and microbiological stability
• Sometime oral liquid has dosing error
• Cost effectiveness:; eg. Liposomal ppn
• Easy Availability
These Risk factors or disadvantages are
become target for novel formulations

31. THANK YOU

32. References
• http://shodhganga.inflibnet.ac.in/bitstream/10603/161405/10/
10_chapter%201.pdf
• https://en.wikipedia.org/wiki/Patient-controlled_analgesia
• https://www.pharmatutor.org/articles/novel-drug-delivery-
system: carriers of NDD formulations
• https://www.ncbi.nlm.nih.gov/books/NBK537349/#:~:text=Drug
%2Deluting%20stents%20(DES),stent%20(BMS)%20in%201986
• Remington 2001 (Text book)