The document discusses the evaluation of novel ocular drug delivery systems. It outlines various challenges with conventional ocular drug delivery and introduces novel approaches like controlled release systems, particulate systems, and vesicular systems. The key evaluation parameters discussed for different novel delivery systems include in vitro drug release studies, drug loading efficiency, stability studies, permeability studies, and in vivo efficacy studies in animal models. The document provides examples of evaluating implants, hydrogels, contact lenses, liposomes, niosomes, and micro/nanoparticles as potential novel ocular drug delivery systems.

1. Evaluation of Novel Ocular
Drug Delivery System
Presented by
Tanmoy Chatterjee
M.Pharm 1st Year (Pharmaceutics)
1st semester
Roll No: PG/06/MAPHARMP/2022/006
Registration No: AU/2022/0006937

2. Contents
 Introduction.
 Diseases of Eye.
 Anatomy of Eye.
 Challenges with Conventional Ocular Drug Delivery.
 Various Ocular Drug Delivery System.
 Reference.
 Acknowledgement.

3. Introduction:
 Ocular administration of drug is primarily
associated with the need to treat ophthalmic
diseases.
 Eye is the most easily accessible site for topical
administration of a medication.
 Ideal ophthalmic drug delivery must be able to
sustain the drug release and to remain in the vicinity
of front of the eye for prolong period of time.

5. Anatomy of Eye:

6. Challenges with conventional ocular drug delivery

7. Ocular
Drug
Delivery
System
Conventional :
i. Solutions,
ii. Suspension,
iii. Emulsion,
iv. ointments
Vesicular:
i. Liposomes,
ii. Niosomes,
iii. Desmosomes
Particulate:
i. Microparticle
ii. nanoparticle
Control release:
i. Inserts
ii. Implants
iii. Hydrogels
iv. Contact lenses
v. Collagen shield
vi. Microneedle
vii. Iontophoresis
To overcome the challenges with
conventional approach we need novel
ocular delivery system
Novel delivery systems are i.
control release, ii. Particulate,
iii, vesicular

8. Evaluation of Novel Ocular Drug delivery System
1. Implants or ocusarts:
 in vitro Degradation Studies:
Results were plotted to evaluate the pH change rate because of the degradation.
 in vitro Release Studies:

9. Cont.…
 Experiments were performed under sink conditions, where maximum CsA
concentration was kept below 100 :g/mL as CsA solubility was reported as 1
mg/mL. The difference factors (f1) and the similarity factors (f2) were
calculated to compare release profiles.
 in vivo Efficacy Studies:
 Then hydrogel is applied for healing.

10. 2. Hydrogels:
Evaluation of contact lens can be
categorized into two parts
Physicochemical characteristics of
the hydrogel
pH titrations
Optical transmission
Rheological studies
Dynamic strain sweep test.
Dynamic frequency sweep test
In vitro release studies
Drug loading efficiency
In vitro release
In vivo studies
Eye irritation test
In vivo efficacy

11. A. Physicochemical characteristics of the hydrogel:
 pH titrations:
 Optical transmission:
All OT studies were done in triplicate and the mean± standard error (SEM) has to be reported.
The statistical significance between groups has to be measured using Student's t-test.

12. Cont.…
 Rheological studies:
All rheological studies are performed in triplicate and the mean ± SEM is reported.
 Dynamic strain sweep test:

13. Cont.…
 Dynamic frequency sweep test:
 Degree of swelling:

14. Cont.…
B. in vitro Release Studies:
 Drug loading efficiency:
 in vitro Release:

15. Cont.…
C. in vivo Studies
 Eye irritation test: It is totally depends on drug or API
in hydrogel.
 in vivo Efficacy: Depends on API and standard protocol
developed by researcher. Preferences is given on animal
studies with albino mice.

16. 3. Contact lenses:
 Surface characterization: It is done field emissions canning electron microscopy (FE-
SEM) (HITACHI S 4160) and transmission electron microscopy (TEM) technique to
determine surface morphology.
 Equilibrium water content (EWC) of contact lens and nanoparticles loaded contact
lens: The swelling kinetics of the contact lens was measured gravimetrically. Done by this
equation
%EWC =
Wwet−Wdry
Wwet
× 100
 Transmittance. Optical property of nanoparticles loaded contact lens with 200 µm
thickness was measured using UV–Vis spectrophotometer in the range from 200 to 900 nm.
Before the examination, the contact lens were soaked in PBS overnight for complete
hydration. Each sample was mounted in a quartz cuvette.
 Mechanical properties. A dynamic mechanical analyzer (eg; DMA Q800, TA instruments)
was used to measure the storage and loss modulus of different api loaded systems.

17. Ion permeability: Determine by conductometry
procedure using NaCl as a fluid.
Oxygen permeability: Determine by OX-TRAN
instrument.

18. 4. Liposomes & Niosomes:
Morphology: Detected by TEM.
Particle size and zeta potential: The particle sizes, size
distribution and zeta potentials of liposomes were measured
by dynamic light scattering detector at 25 °C. 50 L of
original 234 sample was diluted in 950 L of deionized
water for measurement.
Encapsulation efficiency: Determine by HPLC with
appropriate mobile phase as per drug. Equation for
determination is
𝐸𝐸 = 1 − 𝐶𝐹𝑟𝑒𝑒 𝐷𝑟𝑢𝑔 𝐶𝑇𝑜𝑡𝑎𝑙 𝐷𝑟𝑢𝑔 × 100%

19.  in vitro Drug release : Determine by using Franz diffusion cells.
 in vitro Corneal permeation: In vitro corneal permeation studies were
carried out using modified Franz-type diffusion cells with a diffusion area of
0.5 cm2.
The amount of drug permeating through the corneal epithelium was plotted
versus time, and the apparent corneal permeability coefficient (cm/s) was
determined according to the equation:
P app = Q (t X C0 X A X 60)
where Q/t is the slope of the linear portion (lg per minute), C0 is the initial
drug concentration (g/cm3), A is the corneal surface area (cm2), and 60 is the
conversion constant from minute to seconds.

20. 5. Desmosomes:
 All evaluation parameters are same as above mentioned liposomes and
niosomes but only one evaluation parameter is added and that is
“Transepithelial Electrical Resistance”
 It is determined by Endohm instrument. It is determined in different phases of
cell growth.
6. Micro & Nanoparticles:
 Morphology: Determine by TEM
 Stability studies: It is done as per ICH stability study guideline.
 Content uniformity: It is done by HPLC with appropriate mobile phase as
per API

21. Reference
 BozdağPehlivan1PersonEnvelopeBurçinYavuz1SemihÇalamak2KezbanUlubayram2AbbasKaffashi3ImranVural1Hasan BasriÇakmak4Meltem
EzgiDurgun1Emir BakiDenkbaş5NurşenÜnlü1 et al. (2015) Preparation and in vitro/in vivo evaluation of cyclosporin A-loaded nanodecorated ocular
implants for subconjunctival application, Journal of Pharmaceutical Sciences. Elsevier.
 SivaNaga S. Anumolu et al. (2009) Design and evaluation of novel fast forming pilocarpine-loaded ocular hydrogels for sustained pharmacological response
 Farzaneh Hashemi Nasra et al. Preparation and Evaluation of Contact Lenses Embedded with Polycaprolactone-based Nanoparticles, for Ocular Drug
Delivery.
 Hamad Alyami et al. Nonionic surfactant vesicles (niosomes) for ocular drug delivery: Development, evaluation and toxicological profiling.
 Elisa Toropainen et al. Culture Model of Human Corneal Epithelium for Prediction of Ocular Drug Absorption.
 T. K. DE et al. Polycarboxylic acid nanoparticles for ophthalmic drug delivery: an ex vivo evaluation with human cornea.
 https://www.shutterstock.com/search/eye-disease
 https://www.pharmafocusasia.com/research-development/ocular-drug-delivery-perspective
 Yixuan Dong et al. Fabrication and characterization of silk fibroin-coated liposomes for ocular drug delivery.

22. Acknowledgement
 I would like to express my gratitude to the Pharmaceutics
faculty of Adamas University, especially, Dr. Anwesha Barik
for guiding me to complete this presentation. I’m thankful to
our Dean sir, Dr. Sajal Jha and HOD sir, Dr. Sanjay Dey, for
giving me the opportunity to present this topic.
 Secondly I like to thanks my parents to help me always in
my studies.