Conventional ocular drug delivery system i.e., eye drops, ointments, gels etc., had become less popular pertaining to their disadvantages like evaporation by tears, pre-corneal loss, drug metabolism, drug-protein interaction, drainage, sticking of eye lids, induced lacrimation, poor patient compliance, systemic side effect and blurred vision etc. That’s why fundamentals of controlled release by means of ocular inserts were utilized to increase problem pre-corneal drug residence time. This project title “Formulation and Evaluation of Ocuserts of Ciprofloxacin HCl” revealed following results:  Compatibility study using FTIR was performed to check the compatibility of drug with various excipient. Characteristics peaks obtained with pure drug were compared with that produced with different excipients that confirmed the compatibility of drug with excipients.  Ocusert of Ciprofloxacin HCl was prepared using different material i.e., PVP K-30, PVA, PEG 400 and glycerin.  Prepared ocuserts were evaluated for various parameters viz., percentage moisture loss, percentage moisture absorbs, thickness, weight variation, drug content and In-vitro diffusion.  The percentage (%) moisture absorption and loss of ocular insert were found to be 26% and 27% respectively.  The thickness of ocular insert was found to be uniformed and its mean while measuring at different points was found to be 0.124mm.  The weight of ocular inserts was found to be in the range of 12.2 - 12.6mg which indicated decent distribution of the drug, polymer and plasticizer.  The drug content of ocular insert was found to be 99.89%.  Percentage drug release from Ciprofloxacin HCl Ocusert was found to be 41.969% in 8 hr. It was concluded that prepared Ocusert of Ciprofloxacin HCl could be a better alternative to conventional ocular formulations that retained on ocular surface for longer duration and released drug in controlled manner.

1. A
PRESENTATION
ON
FORMULATION AND EVALUATION OF OCUSERTS OF CIPROFLOXACIN HCl
Submitted for the partial fulfilment of the award of the degree of
Bachelor of Pharmacy
By
MOHAMMAD ADIL
Enrollment No. TPH1102033Approved by Supervised by
PROF. (DR.) K. K. JHA MRS. SHAWETA SHARMA
(Director) (Asst. Prof.)
TEERTHAKER MAHAVEER COLLEGE OF PHARMACY
TEERTHANKER MAHAVEER UNIVERSITY MORADABAD
2015- 2016
1

2. INTRODUCTION
Eye is an essential organ with unique qualities and enable us to see the world.
Eye sicknesses can influence the body and consequently led to loss of vision also.
Therefore, many traditional and new ocular drug delivery systems are available.
Most commonly available ophthalmic preparations i.e. eye drops and ointments covers about 70% of
the total formulations in market.
From conventional dosage forms, just a little amount is available for its therapeutic effect resulting in
frequent dosing.
That’s why to overthrown these issues, newer pharmaceutical formulation such as In-situ gel,
nanoparticles, liposomes, nanosuspension, microemulsion, iontophoresis and ocular inserts have been
developed to increase the bioavailability of the drug in sustained and controlled manner.
2

3. CLASSIFICATION OF OCULAR DRUG DELIVERY
SYSTEMS: -
Ocular drug delivery system are classified as:
• LIQUIDS: - Sprays, sol-gel systems, suspensions & solutions.
• SOLIDS: - Ocular inserts, artificial tear inserts, contact lenses, filter paper strips & corneal shield.
• SEMI-SOLIDS: Gels & ointments.
• MISCELLANEOUS: Ocular iontophoresis, Muco-adhesive dosage forms & vesicular systems.
3

4. OCUSERTS:
 Ocular inserts have been developed through which the drug is
delivered at a near constant known rate based on diffusional
mechanisms.
 Minimizes side effects by avoiding excessive absorption peaks.
 The delivery of pilocarpine by such an insert was
commercialized in 1975 (ocuserts Pilo) by Alza corporation.
 The ocuserts was designed to be placed in the lower cul-de-sac
to provide a weekly dose of pilocarpine and removed &
replaced by a new one after completion of time.
 The near zero-order rate delivery is based on the selection of an
non-eroding copolymer membrane enclosing the drug reservoir.
Placement of ocusert into eye
4

5. ADVANTAGES OF OCUSERTS:
 Increased contact time that led to enhanced bioavailability.
 Possibility of providing a prolonged drug release and in consequence a better efficacy.
 Administration of a precise dose in the eye and thus an improved therapy.
 Decrease of systemic side effects and adverse effects.
 Reduction of the number of administrations and thus improved patient compliance & ease.
 Lack of explosion.
 Ease of handling and insertion.
 Reproducibility of release kinetics.
 Sterility.
 Better stability.
 Exclusion of additives.
 Improved shelf life with comparison to aqueous solutions due to lack of water. 5

6. MECHANISM OF DRUG RELEASE
Drug release from Ocusert involves one of following mechanisms:
• Diffusion
• Osmosis
• Bio-erosion
6

7. METHODS OF PREPARATION OF OCUSERTS
 Solvent casting method
 Glass substrate technique
 Melt extrusion technique
7

8. S.N
o.
AUTHOR NAME TITLE & JOURNAL FINDINGS
1. Sneha prabha Lad et al.
(2016)
“Design of ocular controlled release ocuserts
of brinzolamide”, Int J Pharm 2016; 6(2):
191-202
In-vitro diffusion and In-vivo studies
revleaed 82.0% ± 0.594 & 80.00 ± 1.003%
respectively. Drug polymer compatibility
was confirmed by IR & DSC studies.
2. Sayani Bhattacharyya et
al. (2015)
“Preparation and Evaluation of Ophthalmic
Inserts of brimonidine tartrate”, IJPCBS
2015, 5(1), 177-183
It was found that Inserts containing HEMA
plasticized with DBP indicated better shape
holding properties and a controlled drug
release.
3. Narendra V et al. (2014) “Azithromycin β –cyclodextrin ocular films:
Preparation and Evaluation”, IJCPS, 2014,
Vol.2(11): 1265-1269
The prepared ocular films gave satisfactory
physicochemical characteristics and in-vitro
release characteristics
4. Vivek Dave et al. (2013) “Formulation and evaluation of controlled
delivery of Aceclofenac through ocular
insert”, Turk J Pharm Sci., 2013, 10 (2), 205-
220
It was observed that 98.24% drug was
released from the formulation consisted of
3% HPMC while it was 70.25% with 3%
Ethyl Cellulose for a period of 24 hr and
followed zero order kinetics.
8
REVIEW OF LITRATURE

9. 5. Kaul Shweta et al.
(2012)
Development and In-vitro characterization of
ocular insert containing erythromycin, IRJP
2012, 3 (8) Pg. no. 246-250
It was concluded that the Erythromycin
ocuserts would be able to offer benefits such
as increased residence time, prolonged drug
release, reduced frequency of administration,
and thereby might help to improve patient
compliance.
6. T.K. Ghelani et al.
(2011)
Formulation and Evaluation of Timolol
Maleate Ocular Insert, Asian Journal of
Biochemical and Pharmaceutical Research
2011, (1), 167-174
In-vitro release study was carried out for all
formulations and overall results revealed that
as concentration of polymer increased, the
drug release was decreased.
7. A. Rajasekaran et al.
(2010)
Design and evaluation of polymeric
controlled release Natamycin ocular inserts,
Kathmandu university journal of science,
engineering and technology 2010, 6 (I),108-
115
FTIR studies indicated no possibility of
interaction between drug and polymer and all
formulations showed no change in physical
appearance. The formulation consisted of 3%
Eudragit RL 100 and 1% Eudragit L 100
showed expected zero order release for one
day.
9

10. 8. Hitesh B. Gevariya et al.
(2009)
Sustained ophthalmic delivery of
levofloxacin from once a day ocuserts,
International Journal of Pharmacy and
Pharmaceutical Sciences, 1 (1), Nov.-Dec.
2009 pg. no. 24-32
In-vitro drug release studies revealed that,
the formulation with PEO/EC (3:7) was
found to be better than the other
formulations . The formulation L6 followed
perfect zero order kinetics release (n=1.03)
while rest of formulations released super
case II kinetics (n>1).
9. Shreenivas et al. (2006) Ofloxacin ocular inserts: Design,
Formulation and Evaluation, IJPT 5:159-
162, 2006
Best formulation showed maximum
cumulative percentage drug release of 91.27
% at the end of 24 hr. Prepared ocuserts
were also passed the test for sterility &
showed zero-order drug release in the in-
vitro and in-vivo release studies.
10. Venkateshwar RAO et al. Preparation and Evaluation of Ocular
Inserts Containing Norfloxacin, Turk J
Med Sci 34 (2004) 239-246
All the prepared films were found to be
uniform in thickness and the partition
coefficient of norfloxacin and its beta
cyclodextrin complex was 0.048 and 0.853
respectively. I.R. spectra revealed
complexation of norfloxacin with b-
cyclodextrin.
10

11. ADOPTED METHODOLOGY
• PREPARATION OF STANDARD CALIBRATION CURVE
• DRUG EXCIPIENT COMPATIBILITY STUDIES BY USING FTIR
11

12. • PREPARATION OF OCUSERTS
S.No. Ingredient Amount
1. Ciprofloxacin HCL 100 mg
2. Poly Vinyl Pyrrolidone (K-30) 500 mg
3. Poly Vinyl Alcohol 500 mg
4. Poly Ethylene Glycol 400 0.5 ml
5. Glycerine 25 mg
Ocusert of ciprofloxacin was prepared
with three different polymers by solvent
casting method.
12

13. • EVALUATION OF OCUSERTS OF CIPROFOLAXCIN:
Percentage (%) moisture absorption
Percentage (%) moisture loss
Uniformity of thickness
Uniformity of weight
Drug content
In vitro drug release studies
13

14. EXPERIMENTAL STUDIES:
• Spectrophotometric scan of Ciprofloxacin HCl:
The λmax of ciprofloxacin hcl was found to be 278nm.
U.V scan of Ciprofloxacin HCl in 0.1N HCl
14
RESULT AND DISCUSSION

15. • Validation of λmax
Overlain spectra of ciprofloxacin HCl
15

16.  Preparation of standard curve of ciprofloxacin HCl:
S.
No.
Concentration
(µg/ml)
Absorbance
1. 2 0.195
2. 4 0.389
3. 6 0.598
4. 8 0.795
5. 10 0.989
0
0.195
0.389
0.598
0.795
0.989
y = 0.0993x - 0.0024
R² = 0.9999
-0.2
0
0.2
0.4
0.6
0.8
1
1.2
0 2 4 6 8 10 12
Absorbance
Concentration (µg/ml)
Caliberation curve of Ciprofloxacin HCl
Concentration v/s absorbance data of
Ciprofloxacin HCl in 0.1N HCl
Calibration curve of Ciprofloxacin HCl in
0.1N HCl
16

17. DRUG - EXCIPIENT COMPATIBILITY STUDY BY FTIR
FTIR scan of Ciprofloxacin HCl (pure drug) FTIR scan of formulation blend
17

18. EVALUATION OF OCUSERTS:
• Percentage (%) moisture absorption:
The percentage (%) moisture absorption of ocusert was observed to be 26%.
• Percentage (%) moisture loss:
The percentage (%) moisture loss of ocusert was observed to be 27%
• Uniformity of thickness:
The mean thickness of ocusert measured at different points was found to be 0.124mm.
• Uniformity of weight:
The weight of ocusert was observed to be in the range of 12.2 - 12.6mg. It showed great
distribution of the drug, polymer and plasticizer.
• Drug content:
The drug content of ocular insert was found to be 99.89%.
18

19. • In vitro drug release study of Ocusert of Ciprofloxacin HCl:
Sr.
No.
Time
(hrs.)
Absorbance Concentrati
on (µg/ml)
Amt. in
30ml
% Drug
Release
1. 1 0.191 1.923 0.577 8.127
1. 2 0.212 2.135 0.640 9.021
1. 3 0.363 3.655 1.097 15.447
1. 4 0.620 6.244 1.873 26.382
1. 5 0.732 7.372 2.212 31.148
1. 6 0.803 8.087 2.425 34.169
1. 7 0.898 9.043 2.713 38.211
1. 8 0.988 9.949 2.984 41.969Percentage drug release from Ciprofloxacin HCl Ocusert
0
5
10
15
20
25
30
35
40
45
0 1 2 3 4 5 6 7 8 9
%DrugRelease
Time (hr.)
In-vitro Drug Release form Ciprofloxacin Ocusert
19

20. CONCLUSION
This project title “Formulation and Evaluation of ocuserts of ciprofloxacin HCl” revealed following results:
• Compatibility study using FTIR was performed to check the compatibility of drug with various excipient.
Characteristics peaks obtained with pure drug were compared with that produced with different excipients that
confirmed the compatibility of drug with excipients.
• Ocusert of ciprofloxacin HCl was prepared using different material i.e., PVP K-30, PVA, PEG 400 and glycerin.
• Prepared ocuserts were evaluated for various parameters viz., Percentage moisture loss, percentage moisture
absorbs, thickness, weight variation, drug content and in-vitro diffusion.
• The percentage (%) moisture absorption and loss of ocular insert were found to be 26% and 27% respectively.
• The thickness of ocular insert was found to be uniformed and its mean while measuring at different points was found
to be 0.124mm.
• The weight of ocular inserts was found to be in the range of 12.2 - 12.6mg which indicated decent distribution of the
drug, polymer and plasticizer.
• The drug content of ocular insert was found to be 99.89%.
• Percentage drug release from ciprofloxacin HCl ocusert was found to be 41.969% in 8 hr.
It was concluded that prepared ocusert of ciprofloxacin HCl could be a better alternative to conventional ocular
formulations that retained on ocular surface for longer duration and released drug in controlled manner.
20

21. REFERENCES
• Jitendra, sharma P.K, banik A., Dixit S. A new trend: ocular drug delivery system. International journal of pharmaceutical sciences 2011;
2(3):1-2.
• Http://anatomy.Iupvi.Edu
• www.Aioeyesurgeons.Com
• www.Myeyeworld.Com
• Patel hitesh A, patel jayavadan K., Patel kalpesh N, patel ravi R. Ophthalmic drug delivery system-a review. Scholars research library
2010; 2(4): 103.
• Williams Lippincott and Wilkens, Remington - the science and practice of pharmacy, 21st edition, 2005, published by wolters kluwer
company, page no. 850, 851 & 857
• Yie.W. Chien, novel drug delivery systems 2nd edition,1982,100-120.
• Kaul shweta, kumar g., Kothiyal P. An insight into ocular insert. International journal of pharmaceutical sciences and research 2012;
3(7):1907-1908.
• Tangri p, khurana s. Basics of ocular drug delivery systems. International journal of research in pharmaceutical and biomedical sciences
2011; 2(4): 1547.
• Heller j. Controlled release of biologically active compounds from bio erodible polymers. Biomaterials 1980; 1:51-7. 21

22. THANK YOU
22