LH 11 (4)

Download as pdf or txt
Download as pdf or txt
You are on page 1of 18

Lecture 13 – Ocular drug delivery

.in
ist
ac
m
system

h ar
hP
c
en
tB
as
.L
w
w
w

1
© Ramaiah University of Applied Sciences
Intended Learning Objectives

At the end of this session, students will be able to

.in
• Discuss Contact lens as drug deliver device to the eye

ist
ac
m
• Enlist the QC tests for ophthalmic dosage forms

h ar
hP
• Briefly explain packaging of eye drops

c
en
tB
as
.L
w
w
w
Contact Lens

• Contact lenses are thin, and curved shape plastic disks which are designed
to cover the cornea

.in
ist
ac
m
• After application, contact lens adheres to the film of tears over the cornea

h ar
hP
due to the surface tension

c
en
tB
as
.L
w
w
w
Contact Lens
Early Conventional
Hydrogel
(CH) CLs did not
1930 1965 provide adequate
Polymethyl Use of soft oxygen transmission
methacrylate contact lens to the cornea, resulting
(PMMA) was used as (SCL) in hypoxia related

.in
ist
the first successful for ophthalmic complications

ac
contact lens (CL) drug delivery during overnight wear,

m
ar
material (Sedlacek) limiting their long term

h
hP
therapeutic

c
en
potential
tB
as
.L
w

1970,s 1960s
w
w

benefits of CL for Discovery of


1990,s
ocular drug delivery hydrogels
Highly oxygen
(Kaufman) (Witcherle and Lim)
permeable Silicone
Hydrogel
(SH) CLs were
introduced
Advantages of Contact lens

• Located in the immediate


vicinity of the cornea

.in
ist
• Limited mixing in the tear

ac
m
film between the lens and

h ar
the cornea leads to a

hP
c
en
residence time of more than
30 minutes (Compared to tB
as
.L

5min for eye drops)


w
w
w

• Increase in bioavailability
Materials For Contact Lens

• Hydrogels - good transmission of visible light, high chemical and


mechanical stability, reasonable cost and high oxygen

.in
transmissibility

ist
ac
m
• Poly HEMA - water content of about 38%

h ar
hP
• Methacrylic acid (MAA) with HEMA, soft contact lenses(SCLs) with

c
en
tB
different water contents, hardness, strength and oxygen
as
.L
permeabilities can be created
w
w
w
Strategies/Techniques For Contact Lens Based Drug
Delivery System

.in
ist
ac
m
h ar
hP
c
en
tB
as
.L
w
w
w
Soaking Method

• Involves soaking the preformed contact lenses in the drug solution,


followed by drug uptake and release in pre- and post-lens tear film

.in
ist
• Contact

ac
lenses have internal channels/cavity for

m
h ar
receiving/accommodating the drug molecules

hP
c
en
tB
• Drug loading depends on the water content, thickness of lenses, the
as
.L
w
w

molecular weight of the drug, soaking time period and


w

concentration of drug in soaking solution


Soaking Method

Limitations

• High molecular weight drugs or polymers like hyaluronic acid, do not

.in
ist
penetrate the aqueous channels of contact lenses and remain on

ac
m
ar
the surface only

h
hP
c
en
• Contact lenses have low affinity for most of the ophthalmic drugs
tB
as
.L

like timolol maleate, olopatadine HCl, brimonidine tartrate, etc.


w
w
w

• Effects of sterilization and packaging processes on the stability of


therapeutic contact lenses - may cause premature release of the
drug
Molecular Imprinting (MI)
• Monomers are polymerised in the presence of drug templated
followed by removal of the template

• Resulting in formation of tailored active sites or imprinted pockets


called macromolecular memory sites

.in
ist
ac
m
h ar
hP
c
en
tB
as
.L
w
w
w

10
Molecular Imprinting (MI)

Limitation

• Highly cross-linked structure of hydrogel affects the optical and

.in
ist
physical performance of contact lens

ac
m
h ar
• The drug-loading capacity is limited by the template molecules and

hP
c
en
functional monomers, and the deformation (change in dimension)
tB
as
of contact lenses after release of drug was also noted
.L
w
w
w

• The fall in water content (decrease in swelling) leads to an


insufficient ion and oxygen permeability which limit the use of
contact lenses for extended wear
Quality Control of Ophthalmic Products
• pH
• Universal tests • Isotonicity
– Description • Viscosity

.in
– Identification Therapeutic efficacy

ist
• Compatibility

ac
– Assay

m

ar
Clarity

h
– Impurities

hP
• Particulate matter

c
en
• IPQC • Insoluble particulate matter
tB
as
• FPQC • Particle size
.L
w

• Uniformity of volume
w
w

• Uniformity of content
• Uniformity of weight
• Bacterial endotoxin
• Sterility testing
Packaging of eye drops
• Ophthalmic liquids can be packaged in sterile glass bottles
with separate dropper or in plastic bottles with self-contained
dropper tips

.in
ist
ac
m
ar
h
chP
en
tB
as
.L
w
w
w

Plastic bottle with Glass bottles with


self container tip separate droppers

13
10
Glass bottle packaging
• Dropper bottle for eye drops are fitted with a cap , rubber teat
and dropper as the closure
• The bottles are used at a capacity of 10 ml or 20 ml

.in
• Glass containers are used in only a very few instances because of

ist
ac
stability limitations

m
h ar
• Type 1 glass vials with appropriate stoppers are used for

hP
c
en
ophthalmic products
tB
as
.L
w
w
w

14
10
© Ramaiah University of Applied Sciences
Plastic packaging
• Currently all most all commercially available ophthalmic
products are packaged in plastic containers
• Advantages of plastic containers are ease of use, little breakage,
less spillage. This led to universal acceptance of plastic

.in
ist
containers.

ac
m
• Plastic packaging components consists of bottle fitment and

h ar
closure

hP
c
• It has multi-component single-drop dispenser. Eye drops must be
en
tB
sterilezed after filling into the containers and sealing, by
as
.L

autoclaving at a temperature of 90-100oC for 30 mins, or


w
w
w

alternatively they may be pre sterilized and filled aseptically into


previously sterilised containers
• The containers are usually fitted with droppers attached to the
closures
Two types of dose preparations in plastic packaging
• Single dose preparations
• Multiple dose preparations
Single dose preparations
• The ideal type of packaging for eye drops is a disposable

.in
one shot container which eliminates the need for any

ist
ac
preservative and reduces the risk of infecting the eye during

m
applications almost to zero

h ar
hP
• Single dose packs are available in which the solutions can

c
en
be sterilised by autoclaving in air ballasted autoclaves these
tB
as
solutions can therefore be formulated without a
.L
w

preservative
w
w

Single dose blow fill seal packaging


• Single-use vials, when filled under sterile conditions, have
the additional advantage of enabling the product to be
formulated without preservatives

• Most products in multi-use containers need preservatives to


counteract microorganisms after each use
16
10
© Ramaiah University of Applied Sciences
Multiple dose preparations
• Multiple dose preparations must contain an antimicrobial
preservative to prevent proliferation of contaminants during use

.in
and to support the maintenance of sterility

ist
ac
• Examples of preservatives are phenyl mercuric nitrate or acetate,

m
h ar
hP
chlorhexidine acetate or benzalkonium chloride

c
en
tB
as
.L
w
w
w
w
w
w
.L
as
tB
en
chP
h ar
m
Summary

ac
ist
.in

You might also like

pFad - Phonifier reborn

Pfad - The Proxy pFad of © 2024 Garber Painting. All rights reserved.

Note: This service is not intended for secure transactions such as banking, social media, email, or purchasing. Use at your own risk. We assume no liability whatsoever for broken pages.


Alternative Proxies:

Alternative Proxy

pFad Proxy

pFad v3 Proxy

pFad v4 Proxy