Volume 1 • Issue 1 • 1000103 13 Madridge J Pharm Res.
ISSN: 2638-1591
Madridge
Journal of Pharmaceutical Research
Research Article Open Access
Dorzolamide in situ Gel Forming System:
Characterization and Evaluation for Glaucoma
Treatment
Puneet Kataria
1
, Rajesh Katara
1
, Pravat K Sahoo
1
and Sameer Sachdeva
1,2
*
1
Department of Pharmaceutics, Delhi Institute of Pharmaceutical Sciences and Research, (Formerly College of Pharmacy), University of
Delhi, Pushp Vihar, Sector III, New Delhi-110017 , India
2
Amneal Pharmaceuticals, Piscataway, NJ 08854, USA
Article Info
*Corresponding author:
Sameer Sachdeva
Research Scientist
Amneal Pharmaceuticals
Piscataway NJ 08854
USA
Tel: 3123153194
E-mail: samsach14@gmail.com
Received: May 2, 2017
Accepted: June 23, 2017
Published: June 30, 2017
Citation: Kataria P, Katara R, Sahoo PK,
Sachdeva S. Dorzolamide in situ Gel Forming
System: Characterization and Evaluation for
Glaucoma Treatment. Madridge J Pharm Res.
2017; 1(1): 13-21.
doi: 10.18689/mjpr-1000103
Copyright: © 2017 The Author(s). This work
is licensed under a Creative Commons
Attribution 4.0 International License, which
permits unrestricted use, distribution, and
reproduction in any medium, provided the
original work is properly cited.
Published by Madridge Publishers
Abstract
The objective of the present study was to develop an efficient in situ gel forming
system of Dorzolamide for the treatment of glaucoma. The in situ gel was formulated
using alginate and hydroxyl propyl methyl cellulose (HPMC) polymer combination. The
developed formulation was characterized for various in vitro parameters e.g. drug
content, pH, isotonicity, surface tension, rheological behavior, drug release profile and
transcorneal permeation. The rheological behavior of all formulations was not affected
by the incorporation of the drug. The bioadhesive strength of the developed formulation
was found to be 0.311 Nmm. The optimized formulation was stable and non-irritant to
rabbit eyes. In vitro drug release was found to be 91.27 ± 0.61 % over a period of
10 hours. The best-fit kinetic model (Korsmeyer model) for the optimized formulation
DIG 8 suggests that the drug release via Fickian-diffusion mechanism. A maximum mean
difference of 27.4% in lowering intra ocular pressure was observed between control and
treated eyes with optimized formulation after water loading (p<0.01). The in situ
alginate/HPMC gel forming system could be a potential approach for Dorzolamide
formulation to enhance ocular bioavailability for the treatment of glaucoma, ultimately
improving the patient compliance.
Keywords: In Situ Gel; Dorzolamide; Alginate; Intraocular pressure; Ocular delivery.
Introduction
Medications for ocular diseases are often administered topically to attain a higher
concentration at the local site and to avoid any systemic side effects. Ocular diseases
like conjunctivitis, uveitis and glaucoma are generally treated with solutions, suspension
and semisolids like ointments and gels [1-3]. Conventional liquid ophthalmic formulations
results in poor bioavailability and decreased therapeutic response due to high tear turn
over and constant lachrymal drainage in the eye [4].
The constant tear drainage sweeps away a large portion of the applied drug solution
via nasolachrymal duct to the gastro-intestinal tract from where it may be absorbed
systemically, causing untoward side effects [2]. Moreover, conventional dosing shows an
initial peak level of the drug, which may be usually several folds higher than the required
therapeutic level, imparting the reason for toxicity again.
Other preparations like ointments, suspensions, inserts and aqueous gels are
capable to extend the pre-corneal residence time and slow down the drug elimination
ISSN: 2638-1591