Int. J. Pharm. Investigation, 2022; 12(3) : 386-390
386 International Journal of Pharmaceutical Investigation, Vol 12, Issue 3, Jul-Sep, 2022
Original Article
INTRODUCTION
Te primary goal of ocular medicine administration is to get better the
already accessible conventional dosage shape as well as to make use of
innovative drug delivery systems to improve therapeutic efcacy. Te
use of eye drops as a topical treatment for people with eye problems
is extremely prevalent, because of continual lachrymal secretion, tear
turnover, blinking, refex, moreover quick nasolachrymal drainage,
traditional eye drops have a low ocular bioavailability. Usual drainage
of an administered dosage begins almost instantly afer administration
furthermore is fnished in less than 5 min.
1
As a decision, a regular
infux of concerted mixture ensures required to obtain these expected
healing efects. To address these issues, researchers have looked into a
variety of ocular formulations, including viscous solutions, ointments,
gels, nanoparticles, and polymeric inserts.
2
Tese vehicles occupy
enhanced corneal contact time to varying degrees, but they have not
been universally adopted due to obscured vision or a lack of patient
compliance. As a decision, achieving adequate ocular bioavailability
afer topical distribution of a medicine to the eye is a difculty that
has yet to be overcome.
3
Timolol maleate (TM) was used as the model
medication in this investigation. Te most ofen used medicine in the
treatment of glaucoma is TM, which is a non-selective beta-blocker.
Glaucoma is the world’s next to the mass routine source of darkness.
It afects around 70 million people all over the world.
4
TM was chosen
above other medications in the same class because it had a faster onset,
better tolerance, and fewer adverse efects. Tis medication reduces
intraocular pressure by inhibiting the generation of aqueous humor in
the ciliary epithelium by blocking sympathetic nerve terminals. Te goal
of this work was to fnd a way for dispersing proniosomal gel including
TM within the in-situ gel to improve the mucoadhesive and long-term
release behaviour of the gel.
MATERIALS AND METHODS
Materials
Yarrow chem products, Mumbai, India, provided Timolol maleate,
Lecithin, and Poloxamer. Loba Chemie Pvt. Ltd, Mumbai, India,
provided the cholesterol. Rolex Chemical Industries in Mumbai, India,
provided Span 60. Spectrum Chemicals in Mumbai, India, provided Brij
72. S D Fine Chemicals in Mumbai, India, provided Tween 80. Each
chemical utilised were of the highest quality.
Methods
pre-formulation studies
determination of solubility of timolol maleate
By using the shake fask method, the solubility of Timolol maleate in
aqua, ethyl alcohol, PBS pH 6.8, PBS pH 7.4, and ether was measured.
In a fask containing 10 ml of each solvent, an excess amount of the
medication was introduced. Te mixtures were then agitated at 100 rpm
for 24 hours inside a thermostatically managed water bath at 370.5°C,
fltered, diluted, and spectrophotometrically assessed at 294.4 nm using
a UV spectrophotometer against a blank that had been treated similarly.
5
Standard curve for timolol maleate
Te medication (10 mg) was precisely weighed and put within a 100 mL
measuring fask. To make this stock solution-I, the drug was dissolved
in 7.4 pH bufer solution and diluted until 10 mL with the similar
Formulation and Evaluation of Timolol Maleate Proniosomal Gel
for Ocular Drug Delivery
Jayatheertha S Lokapur*, Prakash S Goudanavar, Arpitha J Lokapur, Ankit Acharya, Sandip A Murtale
Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, B. G. Nagara, Nagamangala, Mandya, Karnataka, INDIA.
ABSTRACT
Introduction: The objective of this task is to succeed with the trial of an
ocularly ef fcient Timolol maleate formulation produced from prolonged
proniosomal gel niosomes to get signifcant therapy for glaucoma.
Methods: Cholesterol, Lecithin, Span 60, Brij 72, and Tween 80 in various
concentrations were used to create Timolol maleate loaded proniosomal
gel derived niosomes utilizing the phase coacervation method. Found on
these outcomes of entrapment ef fciency and in-vitro release, an optimised
batch of proniosomal gel-produced niosomes was chosen. By spreading
proniosomes in an in-situ gelling method, timolol maleate proniosomal
gel-derived niosomes were created. Fourier transforms infrared
spectroscopy (FTIR) experiments confrmed each interaction study.
Wetting agent with additive effects on entrapment ef fciency along
with in-vitro drug release manner based on proniosomal gel-produced
niosomes was investigated. Cholesterol, Lecithin, Span 60, Brij 72, and
Tween 80 in various quantities were used in a coacervation technique,
by dispersing proniosomes in an in-situ gelling method, a timolol maleate
proniosomal gel was created. Results: The FTIR analyses revealed no
signs of interaction between the medicine and the excipients, indicating
that they are compatible. At the end of 12 hr, formulations T2 and T10 had
99.98 percent and 99.90 percent drug release, respectively. Conclusion:
Starting with these fndings secured, it can be closed this one proniosomal
gel derived niosomes might be a satisfactory alternative to conventional
eye drops as they exhibited elevated penetrability with sustained-release
actions.
Keywords: Timolol maleate, Proniosomal gel, Phase co-acervation
technique, Ocular delivery, Niosomes.
Correspondence
Mr. Jayatheertha S Lokapur
Ph.D. Research Scholar, Department of Pharmaceutics, Sri Adichunchanagiri
College of Pharmacy, Adichunchanagiri University, B. G. Nagara-571448,
Nagamangala, Mandya, Karnataka, INDIA.
Email id: jayatheertha.lokapur@gmail.com
DOI: 10.5530/ijpi.2022.3.65
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