Online citations, reference lists, and bibliographies.
Please confirm you are human
(Sign Up for free to never see this)
← Back to Search

Improved Pharmacodynamics Of Timolol Maleate From A Mucoadhesive Niosomal Ophthalmic Drug Delivery System.

Deepika Aggarwal, I. P. Kaur
Published 2005 · Medicine

Save to my Library
Download PDF
Analyze on Scholarcy
Share
In the present study chitosan (REVTMbio1) or Carbopol (REVTMbio2 and 3) coated niosomal timolol maleate (0.25%) formulations were prepared by reverse phase evaporation (REV) and compared to timolol solution (TMS; 0.25%) in terms of in vitro release and IOP lowering pharmacodynamic effect. The in vitro release phase of timolol (91% release in 2 h) was extended significantly by its incorporation into niosomes and further by the polymer coating (40-43% release upto 10 h). The developed formulations were evaluated for their pharmacodynamics in albino rabbits, by measuring intraocular pressure (IOP) using a non-contact pneumatonometer, and were compared to a marketed in situ gel forming solution of timolol (Timolet GFS, 0.5%; Sun Pharma). REVTMbio1 formulation showed a more sustained effect of upto 8h (vis a vis 6 h for carbopol-coated niosomes). TMS in comparison showed effect for only 2 h though the peak effect was slightly more (14%). Lowering of IOP in the contralateral eye (20-40% as compared to 100% in case of TMS), considerably reduces with REV and REVbio formulations indicating lesser systemic side effects. Moreover, the results of REVTMbio1formulation containing 0.25% of timolol maleate compared well with the 0.5% marketed gel formulation, indicating our formulation to be significantly better considering that similar effect is obtained at half the concentration. The later becomes especially important in context to the cardiovascular side effects associated with ocular timolol maleate therapy.
This paper references
The corneal penetration of trifluorothymidine, adenine arabinoside, and idoxuridine: a comparative study.
W. O'Brien (1977)
Non-ionic surfactant vesicles as ophthalmic carriers for cyclopentolate. A preliminary evaluation
M. F. Saettone (1996)
10.1111/j.2042-7158.1985.tb04990.x
The preparation and properties of niosomes—non‐ionic surfactant vesicles
A. Baillie (1985)
10.1002/MACP.1997.021980220
Rheological characteristics of semi‐dilute chitosan solutions
M. Mucha (1997)
10.1211/0022357022476
The potential of chitosan in ocular drug delivery
M. Alonso (2003)
10.1023/A:1016467219657
Mechanisms of Mucoadhesion of Poly(acrylic Acid) Hydrogels
H. Park (2004)
10.1016/0168-3659(95)00117-4
Polyacrylic acid mediated ocular delivery of ribozymes
D. Ayers (1996)
10.1016/S0378-5173(99)00030-7
Effect of chitosan on epithelial permeability and structure.
V. Dodane (1999)
10.1111/J.1600-0420.1996.TB00062.X
The intraocular pressure lowering effect of timolol in gel-forming solution.
E. Rosenlund (1996)
10.1016/0169-409X(95)00017-2
Microspheres and nanoparticles used in ocular delivery systems
A. Zimmer (1995)
10.1016/0168-3659(85)90032-X
Physico-chemical properties of water insoluble polymers important to mucin/epithelial adhesion☆
H. Park (1985)
10.1023/A:1012160102740
Chitosans as Absorption Enhancers for Poorly Absorbable Drugs 2: Mechanism of Absorption Enhancement
N. G. Schipper (2004)
10.1201/b14099-4
A RHEOLOGICAL APPROACH TO EXPLAIN THE MUCOADHESIVE BEHAVIOR OF POLYMER HYDROGELS
C. Caramella (1999)
10.1111/j.2042-7158.1985.tb05051.x
The effect of non‐ionic surfactant vesicle (niosome) entrapment on the absorption and distribution of methotrexate in mice
M. N. Azmin (1985)
10.7326/0003-4819-112-2-120
Systemic effects of medications used to treat glaucoma.
D. Everitt (1990)
10.1073/PNAS.75.9.4194
Procedure for preparation of liposomes with large internal aqueous space and high capture by reverse-phase evaporation.
F. Szoka (1978)
10.1023/A:1015891419676
Evaluation of Mucoadhesive Polymers in Ocular Drug Delivery. II. Polymer-Coated Vesicles
N. Davies (2004)
10.1016/J.IJPHARM.2003.09.016
Vesicular systems in ocular drug delivery: an overview.
I. P. Kaur (2004)
10.1016/S0140-6736(05)60473-4
Severe nausea and vomiting with timolol eye drops
Fhj Wolfhagen (1998)
10.1211/0022357044896
Development of a topical niosomal preparation of acetazolamide: preparation and evaluation
Deepika Aggarwal (2004)
10.1016/S0378-5173(98)00027-1
In vitro evaluation of the mucoadhesive properties of chitosan microspheres
P. He (1998)
10.1016/0378-5173(92)90340-8
Pilocarpine bioavailability from a mucoadhesive liposomal ophthalmic drug delivery system
A. M. Durrani (1992)
10.1016/S0378-5173(99)00003-4
Topical use of chitosan in ophthalmology: tolerance assessment and evaluation of precorneal retention.
O. Felt (1999)
10.1002/JPS.2600740407
Bioadhesive polymers as platforms for oral controlled drug delivery II: synthesis and evaluation of some swelling, water-insoluble bioadhesive polymers.
H. S. Ch'ng (1985)
10.1081/DDC-120002997
Penetration Enhancers and Ocular Bioadhesives: Two New Avenues for Ophthalmic Drug Delivery
I. P. Kaur (2002)



This paper is referenced by
10.1142/9781860949074_0006
Vesicles prepared from synthetic amphiphiles — polymeric vesicles and niosomes
I. Uchegbu (2006)
Natural and synthetic oil phase transition microemulsions for ocular delivery of tropicamide: efficacy and safety -
Heba I El Agamy (2015)
10.1016/j.ijpharm.2008.05.031
Effect of some formulation parameters on flurbiprofen encapsulation and release rates of niosomes prepared from proniosomes.
M. Mokhtar (2008)
10.1159/000131503
Effect of Different Biomedical Membranes on Alkali-Burned Cornea
Li-qun Du (2008)
10.1016/j.ijpharm.2010.06.015
Self-assembled liquid crystalline nanoparticles as a novel ophthalmic delivery system for dexamethasone: Improving preocular retention and ocular bioavailability.
L. Gan (2010)
FORMULATION AND EVALUATION OF ION ACTIVATED OCULAR GELS OF KETOROLAC TROMETHAMINE
Sirish Vodithala (2010)
10.1208/s12249-017-0780-7
Optimized Mucoadhesive Coated Niosomes as a Sustained Oral Delivery System of Famotidine
AL-Zahraa M. Khalifa (2017)
10.1080/03639045.2019.1579827
Natamycin niosomes as a promising ocular nanosized delivery system with ketorolac tromethamine for dual effects for treatment of candida rabbit keratitis; in vitro/in vivo and histopathological studies
M. El-Nabarawi (2019)
10.1007/978-3-319-47691-9
Ocular Drug Delivery: Advances, Challenges and Applications
Richard T. Addo (2016)
ENHANCEMENT OF ANTI­GLAUCOMA POTENTIAL BY NOVEL OCULAR DRUG DELIVERY SYSTEM
S. Gupta (2011)
10.1016/j.addr.2009.11.026
Chitosan-based nanostructures: a delivery platform for ocular therapeutics.
M. de la Fuente (2010)
NIOSOMAL DRUG DELIVERY SYSTEM: FORMULATION AND APPLICATIONS
V Linta (2017)
10.1002/APP.39788
In situ gelling ophthalmic drug delivery system: Formulation and evaluation
Neeraj Mittal (2014)
Available online through www.jpronline.info
S. Gupta (2009)
10.1248/BPB.34.945
Niosomes: a controlled and novel drug delivery system.
Rampal Rajera (2011)
Proniosomes for Penetration Enhancement in Transdermal System
Samita Singla (2012)
10.1016/j.exer.2013.04.007
Biodegradable nanoparticles for controlled subconjunctival delivery of latanoprost acid: in vitro and in vivo evaluation. Preliminary results.
Athanassios Giarmoukakis (2013)
10.1089/jop.2012.0200
Novel strategies for anterior segment ocular drug delivery.
K. Cholkar (2013)
10.2147/OPTH.S2032
Effect of water-in-oil microemulsions and lamellar liquid crystalline systems on the precorneal tear film of albino New Zealand rabbits
Judy Chan (2008)
Formulation and Evaluation of Domperidone Oral Proliposomal Powders
Shashidhar Bagam (2015)
Therapeutic Contact Lenses for Comfort Molecules
M. Ali (2007)
10.1586/17469899.2.2.309
Advances in the topical ocular drug delivery
Y. Sultana (2007)
10.3109/08982100903030255
Optimization of gatifloxacin liposomal hydrogel for enhanced transcorneal permeation
K. Hosny (2010)
10.1208/s12249-018-1025-0
Dapsone-Loaded Invasomes as a Potential Treatment of Acne: Preparation, Characterization, and In Vivo Skin Deposition Assay
M. El-nabarawi (2018)
10.15344/2394-1502/2014/105
In-vitro and In-vivo Evaluation of Niosomal Gel Containing Aceclofenac for Sustained Drug Delivery
Dina Fathalla (2014)
10.2174/138161209788923886
Nanocarriers in ocular drug delivery: an update review.
Sheetu Wadhwa (2009)
10.3109/21691401.2016.1160917
Medical management of glaucoma: focus on ophthalmologic drug delivery systems of timolol maleate
A. K. Sah (2017)
10.2165/00137696-200604030-00002
Contact lenses for drug delivery
C. Alvarez-Lorenzo (2006)
10.1016/J.EJPB.2006.01.004
Effects of N-trimethylchitosan on transcellular and paracellular transcorneal drug transport.
Y. Zambito (2006)
10.3109/03639045.2012.736515
Recent advances in ocular drug delivery
Djamila Achouri (2013)
10.1080/10601320601031416
Studies on Biopolymers for Ophthalmic Drug Delivery
S. Ramaiah (2007)
A REVIEW ON RECENT TRENDS IN NIOSOMAL ANTIGLAUCOMA DRUG DELIVERY SYSTEM
Hitesh B. Gevariya (2012)
See more
Semantic Scholar Logo Some data provided by SemanticScholar