Ocular drug delivery aims to administer drugs to the eye, which can target either the anterior (front) or posterior (back) segments. Traditional eye drops lack bioavailability and patient compliance. Recent advances in ocular drug delivery include polymers, nanoparticles, liposomes, and ocular inserts. Glaucoma is a leading cause of blindness where intraocular pressure increases, damaging the optic nerve. Current glaucoma treatments include prostaglandins, beta-blockers, and carbonic anhydrase inhibitors. New areas of research are investigating sustained release inserts, dendrimers, travoprost extended release, gene therapy, and continuous monitoring devices to better treat glaucoma.
2. INTRODUCTION
• Ocular drug delivery is a system which involve the
administration of drug in the eye.
• Drug delivery to the eye can be broadly classified into
1) Anterior Segments.
2) Posterior segments.
• The unique structure of the eye restricts the entry of
drug molecules at the required site of action.
2
3. Traditionally used eye drops formulations lacked good
bioavailability and had low patient compliance, hence
most investigations in this field emphasize on the
duration of action and enhancement of corneal
absorption.
Recent developments in ophthalmic drug delivery
systems include use of gelling polymers, prodrugs,
microspheres, nanoparticles, liposomes and hydrophilic
ocular inserts, non-aqueous vehicles are new areas of
interest in ophthalmic drug delivery.
3
9. CurrentGlaucomaMonitoringSystems:
Measures static intraocular pressure
Single Snapshots in Time
taken during the day when pressure is lowest
Monitoring in Overnight Sleep Labs
cumbersome
expensive
Frequent Punctual Measurements
affects intraocular pressure
checks pressure peaks
9
11. NewAPPROVEDPREPRATION Glaucoma
Simbrinza :
Simbrinza is the first combination eye drop containing a carbonic
anhydrase inhibitor and an alpha2 agonist for the treatment of
glaucoma.
Taptiqom :
Taptiqom is a fixed-dose combination of the prostaglandin analogue
tafluprost and the beta-blocker timolol, for the treatment of
glaucoma.
11
13. ONGOINGResearchworkonGlaucoma
Rho kinase inhibitors :
Rho kinase inhibitors, such as Ripasudil work by inhibition of the actin
cytoskeleton, resulting in the morphological changes in the trabecular
meshwork and increased aqueous outflow. More compounds in this class are
being investigated in phase 2 and phase 3 trials
Dendrimers as tunable vectors of drug delivery systems and biomedical
and ocular applications:
• Dendrimers were examined for the putative use as ophthalmic vehicles for
ocular delivery of pilocarpine nitrate (cholinomimetic). It was observed that
the use of dendrimers with carboxylic or hydroxyl surface groups as drug
carriers increased the bioavailability of pilocarpine nitrate in eyes of albino
rabbits and the time of drug residence .
13
14. DESIGN OF OCULAR CONTROLLED RELEASE OCUSERTS OF
BRINZOLAMIDE:
Ocuserts were formulated using various polymers and plasticizers by film
casting technique.
ENV515 Travoprost Extended Release (XR) in Patients With Open
Angle Glaucoma:
• Envisia Therapeutics Releases ENV515 (travoprost XR) Phase 2 Data
Showing Nine-Month Duration Of Action After A Single Dose in Patients
with Glaucoma showing clinically meaningful reduction in intraocular
pressure.
14
15. Ocular Inserts for Sustained Release of the Angiotensin-Converting
Enzyme 2 Activator, Diminazene Aceturate, to Treat Glaucoma.
• In view of the fact that activation of endogenous ACE2 is a potential strategy
to develop new anti glaucomatous agents, a non-implantable drug delivery
device made of chitosan .
15
16. Gene Therapy For Glaucoma
• A gene therapy approach in which a mutated gene is replaced or
inactivated, or in which a new gene is introduced, could provide a novel
and more effective way of targeting the disease
• Both viral and non viral vector gene delivery systems have been used to
target specific tissues involved in the pathogenesis of glaucoma. These
tissues include the trabecular meshwork, ciliary body, ciliary epithelium.
• Given recent laboratory studies utilizing gene therapy techniques to
lower intraocular pressure and to provide neuroprotection, and the
continued development of tissue-specific vectors, it seems that we are
well poised for a new generation of treatments for glaucoma.
16
18. ADVANCED SYSTEMS :
1. Punctal plugs are placed in the tear duct (punctum) to
release a variety of drugs.
2. Currently targeting the treatment of glaucoma and ocular
hypertension .
18
20. DesignofReplenishMiniPump
1. Micro-electromechanical system that delivers continuous or
bolus-targeted drugs to both the anterior and posterior
segments.
2. Refillable drug reservoir (via 31 gauge needle) that is capable
of storing and delivering up to 12 months.
20
22. TriggerfishSystem
Created by SENSIMED.
First of its Kind on the market constant reading device.
Safety Approval in Europe last year.
22
23. BenefitsofTriggerfishSystem
• Improved Understanding of Pressure Change
• pressure during day versus night
• More Efficient
• Personalized Drug Delivery and Treatment
• Adapt Treatment
• dependent on changing conditions
• Sensor is Placed Outside of Vision Field
• Early Diagnosis and Treatment
23
24. Conclusion
A considerable amount of research has been carried
out on the development of ocular drug delivery
systems.
It is appreciated that the topical route is preferred
for delivery of drugs to the eye.
The primary objective of all the ocular drug
delivery systems developed till date is to increase
ocular drug residence time which leads to
improvement in ocular drug bioavailability, diminish
side effects for a therapeutic response in the eye
24
25. References
• K. P. Sampath Kumar, Debjit Bhowmik, G.Harish, S.Duraivel, B. Pragathi
kumar,Ocular Inserts: A Novel Controlled Drug Delivery System.
• Chrai SS, Makoid MC, Erikson SP, Robinson JR.Drop size and initial
dosing frequency problems of topically applied ophthalmic drugs. J Pharm
Sci. 1974;64:333–8.
• Shweta Kaul, G. Kumar and P. Kothiyal AN INSIGHT INTO OCULAR
INSERT, IJPSR, 2012; Vol. 3(7): 1905-1912 .
• Sikandar et al.: Ocular Drug Delivery System: An Overview. Int. J. Phar.
Sci. Res 2011, 2(5): 1168-1175.
• Robinson J C: Ocular Anatomy and Physiology Relevant to Ocular Drug
Delivery Chapter – 2, In: Ophthalmic Drug Delivery Systems. Marcel
Dekker, New York, Vol – 58 , 1993: 29.
• Marina Kalomiraki, Kyriaki Thermos, NikosChaniotakis, Dendrimers as
tunable vectors of drug delivery systems and biomedical and ocular
applications, International Journal of Nanomedicine
25
26. • Kesharwani P, Jain K, Jain NK. Dendrimer as nanocarriers for drug
delivery. Prog Polym Sci. 2014;39:268–307.
• Azmat Shaikh , Talat Farheen, Dr. Sadhana Shahi, OPHTHALMIC
DRUG DELIVERY SYSTEM WITH RECENT ADVANCES, IJPRD,
2015; Vol 7(05):July-2015 (011 - 022).
• Foureaux G, Franca JR, Nogueira JC,Fulgêncio GdO, Ribeiro TG,
Castilho RO, et al. Ocular Inserts for Sustained Release of the
Angiotensin-Converting Enzyme 2 Activator, Diminazene Aceturate, to
Treat Glaucoma doi:10.13.71/journa l(133 -149).
• Weinreb RN,Tee Khaw P. Primary open-angle glaucoma. Lancet. 2004;
363: 1711–1720. PMID:15158634.
• S K Motwani ; S Chopra ; S Talegaonkar ; K Kohli; F J Ahmad ;R.K.Khar
Eur.J.Pharm.Biopharm. 2008; 68:513–525.
• Rekas M, Danielewska ME, Byszewska A, et al. Assessing efficacy of
canaloplasty using continuous 24-hour monitoring of ocular
dimensionalchanges. Invest Ophthalmol Vis Sci.2016;57:2533–2542.
DOI:10.1167/iovs.16-19185.
• Akanksha Tiwari1, Raj Kumar Shukla, Novel ocular drug delivery
systems: An overview, J. Chem. Pharm. Res., 2010, 2(3):348-355.
26
27. • Tarek Shaarawy , Shibal Bhartiya, Recent Advances in the Treatment of
Glaucoma, European Ophthalmic Review, 2011;5(1):33–7.
• R M Handjani-Vila ; A Rlbier ;B Rondot ; G Vanlerberghe . Int. J.
Cosmetic Sci. 1979; 1, 303-314.
• Quigley HA, Broman AT. The number of people with glaucoma worldwide
in 2010 and 2020. Br J Ophthalmol. 2006;90:262–267.
• V’Ooteghem MM., 1993.,Edman Biopharmaceutics of Ocular Drug
Delivery. Boca Raton, CRC Press., 27–41.
• Barbu E, Sarvaiya I, Green KL, Nevell TG and Tsibouklis J., A. 2005.
Vinylpyrrolidone-co-(meth) acrylic acid inserts for ocular drug delivery:
synthesis and evaluation. J Biomed Mater Res.,74(4):598-606.
27
28. 28
“Sight is the sense which is more valuable
than all the rest.” So Take care of Eyes!!!