Some Polymers Used as Nasal Delivery System

By

Aya Wael Abdu

Fatima Muhaymen Sabah

Supervised By

Dr. Aseel Qasim Muhammad

 Introduction

Recent advancements have sparked increased interest in transdermal and

transmucosal drug delivery methods due to their noninvasive nature, ease of
self-administration, and ability to overcome challenges associated with oral
administration. These routes offer solutions to issues like first-pass
metabolism, gastrointestinal degradation, poor absorption, and slow onset of
action commonly faced with oral drugs.
 Aim of study

The study aims to explore various polymers employed in nasal drug delivery
systems, examining their properties, applications, and contributions to
optimize drug administration through the nasal route. By delving into both
natural and synthetic polymers.
 Nasal Anatomy and Physiology
 The human nasal cavity consists of five regions: vestibule, atrium, respiratory region, olfactory
region, and nasopharynx. Among these, the respiratory region, lined with respiratory epithelium, is
the most permeable, while the vestibule is the least. Mucociliary clearance (MCC), driven by ciliated
cells, is a key protective mechanism facilitated by mucus secretion, which includes water, mucin,
salts, proteins, and lipids.
 Nasal drug delivery encounters challenges like anterior leakage and postnasal drip due to MCC. To
address these issues, in situ nasal gelling systems using smart polymers have emerged. These
polymers undergo reversible gelation in response to nasal conditions, providing controlled drug
release influenced by factors like temperature, pH, and ion composition. This approach offers a
promising path for improving drug delivery in the nasal cavity.
 Nasal Anatomy and Physiology

Schematic diagram of the sagittal section of human nasal cavity Cell types of the nasal epithelium.
 Advantages of smart polymers in nasal drug
delivery
 Smart polymers used in nasal drug delivery systems respond to specific stimuli like changes in temperature, pH,
or ion concentration within the nasal cavity.
 These polymers enable the creation of in situ nasal gels that transition from a liquid to a gel state upon exposure
to nasal conditions, enhancing prolonged retention and controlled drug release.
 Certain smart polymers, such as chitosan derivatives like trimethyl chitosan, can enhance drug absorption by
opening tight junctions and facilitating paracellular transport of large drug molecules across the mucosal
surface.
 Smart polymers adapt well to the physiological environment of the nasal cavity, improving drug absorption and
protecting the drug from enzymatic degradation.
 The use of stimulus-responsive polymers in nasal drug delivery systems not only improves drug absorption but
also offers prolonged nasal retention, sustained drug delivery, and user-friendly administration.
 Polyvinyl alcohol (PVA):

 Polyvinyl alcohol (PVA) is a synthetic polymer known for its biocompatibility, low
protein adhesion, and low toxicity, making it suitable for various medical
applications such as cartilage replacements, contact lenses, and eye drops. In
industrial applications, PVA is used in suspension polymerizations and as a
protective colloid to make dispersions like PVAc in China. In Japan and North
Korea, PVA is used to produce Vinylon fiber, a self-sufficient alternative fiber that
doesn't require oil for production. PVA is also used in photographic film.
 It has the idealized formula [CH2CH(OH)]n
Polyvinyl alcohol (PVA)
 Poly (lactic-co-glycolic acid) (PLGA):

PLGA is a biodegradable copolymer of lactic acid and glycolic acid. It is

widely used in pharmaceuticals due to its biocompatibility and ability to
degrade into non-toxic byproducts.
Use in Nasal Delivery: PLGA is utilized for sustained drug release in nasal
formulations. Its biodegradability allows for gradual drug release over
time, providing extended therapeutic effects.
Poly (lactic-co-glycolic acid) (PLGA):
 Hydroxypropyl methylcellulose (HPMC):

(Hypromellose) HPMC is a semi-synthetic polymer derived from

cellulose. It is water-soluble and forms transparent, flexible films.
Use in Nasal Delivery: HPMC is employed in nasal drug delivery systems
for its mucoadhesive properties. It enhances drug residence time in the
nasal cavity and contributes to controlled drug release.
Hydroxypropyl methylcellulose (HPMC):
 Poloxamers (Pluronics):

Poloxamers are triblock copolymers with hydrophilic and hydrophobic

segments. They exhibit temperature-sensitive gelation behavior.
Use in Nasal Delivery: Poloxamers are used to create in situ nasal gelling
systems. These polymers are liquid at room temperature but form a gel in
response to physiological conditions in the nasal cavity, ensuring
prolonged drug retention and controlled release.
Poloxamers (Pluronics):
 Discussion
 Nasal drug delivery is entering a transformative phase, with an expected influx of nasal products
in the market. This delivery method holds great promise for peptides, protein drugs, CNS
medications, and drugs crucial for crisis and long-term treatments. Overcoming challenges like
drug retention and permeability requires innovative solutions, with stimuli-responsive polymeric
systems emerging as key strategies.
 Currently, in situ gel-forming nasal delivery is limited to a few stimuli-responsive polymers, but
there is substantial potential for expansion. Polymers like poly(N,N-diethyl acrylamide) and
poly(N-vinyl caprolactam), with tailored lower critical solution temperature (LCST) properties,
offer promising directions. Grafted copolymers also present new avenues for in situ gelling nasal
drug delivery.
 Discussion
 The future may bring stimuli-responsive vesicular and nanoparticulate
systems that significantly enhance the efficiency of nasal drug delivery,
addressing critical drug delivery challenges and fostering innovation in
therapeutic solutions. As research advances, nasal drug delivery is
expected to evolve, offering impactful solutions for diverse
pharmaceutical applications.
 Conclusion

 The use of polymers in nasal drug delivery systems holds great promise for advancing
pharmaceutical applications. This approach has gained attention due to the noninvasive
administration method, ease of use, and potential to enhance drug bioavailability. Stimuli-
responsive polymers, such as those capable of forming in situ gels, address critical challenges like
drug retention, permeability, and physicochemical properties, improving overall delivery
efficiency.
 Specific polymers like poly(N,N-diethyl acrylamide) and poly(N-vinyl caprolactam) have shown
effectiveness in creating systems that respond to nasal temperature, optimizing drug delivery.
Additionally, mucoadhesive agents such as chitosan derivatives contribute to prolonged drug
retention, overcoming issues like leakage and ensuring better therapeutic outcomes.
 Conclusion

 Smart polymers not only aid in administration and retention but also enhance drug
absorption and protect against enzymatic degradation. Copolymers containing
hydrophobic and polyelectrolyte segments, like Pluronic-poly(acrylic acid), demonstrate
improved mucoadhesion and residence time in the nasal cavity.
 As the field advances, future prospects include stimuli-responsive vesicular and
nanoparticulate systems, which could revolutionize nasal drug delivery and address
existing challenges. Continued research and innovation are essential to fully harness the
potential of polymers, improving efficiency, precision, and therapeutic outcomes while
enhancing patient experiences in pharmaceuticals.
Thanks for listening