Author(s): Raghad A. Dayoub, Antoun Laham

Email(s): dayoub.raghad.42@gmail.com

DOI: 10.52711/0974-360X.2023.00208   

Address: Raghad A. Dayoub*, Antoun Laham
Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, University of Damascus, Syria Arab Republic.
*Corresponding Author

Published In:   Volume - 16,      Issue - 3,     Year - 2023


ABSTRACT:
The anatomy physiology and biochemistry of the eye render this organ impervious to foreign substances. Ocusert system was firstly developed in 1975 in the USA. It is a flat, flexible, solid and semisolid device which consists of drug reservoir by using various polymers. In the present study Timolol maleate loaded ocular inserts were prepared using different polymers (Methylcellulose, Hydroxypropyl methylcellulose, Eudragit, Ethyl cellulose, Polyvinyl pyrrolidone) by solvent casting method for the treatment of glaucoma. Glycerin, Polyethylene glycol and Dibutyl phthalate were used as plasticizers in different ratios. The prime objective of ocuserts formulating is to enhance therapeutic effect through continuous controlled delivery of ophthalmically active drug to the eye. The physiochemical parameters like thickness, weight, surface pH, folding endurance, % moisture absorption, % moisture loss and drug content were evaluated. In-vitro drug release studies were carried out using a Franz diffusion cell like model. Drug-polymer interactions were investigated by Fourier transform infrared (FTIR) spectroscopy. It was found that the higher the polymer percentage in the formula, the greater the weight and thickness of the film. The mechanical properties of the films reveal that the formulations (F2, F3, F4, F5, F6, F7 and F8) were strong, elastic with smooth surface and appropriate weight for ocular use. In addition to having surface pH that matches the requirements of the ocular dosage forms. It has also been shown that the formulas with hydrophobic polymers have low ability to absorb moisture as well as low moisture content. F4 (Eudragit RL 100 10%) gave sustained drug release with most of the drug being released after 8 hours (95.331%). The release profile of F4 followed the Korsmeyer-Peppas model and correlation coefficient (R2 = 0.992). FTIR studies did not show any evidence of interaction between the drug and the polymers.


Cite this article:
Raghad A. Dayoub, Antoun Laham. Preparation and In-vitro Evaluation of Timolol Maleate Loaded Ocular inserts by using various polymers. Research Journal of Pharmacy and Technology 2023; 16(3):1259-1266. doi: 10.52711/0974-360X.2023.00208

Cite(Electronic):
Raghad A. Dayoub, Antoun Laham. Preparation and In-vitro Evaluation of Timolol Maleate Loaded Ocular inserts by using various polymers. Research Journal of Pharmacy and Technology 2023; 16(3):1259-1266. doi: 10.52711/0974-360X.2023.00208   Available on: https://www.rjptonline.org/AbstractView.aspx?PID=2023-16-3-44


REFERENCES:
1.    Darwhekar G, et al. Development and Optimization of Dorzolamide Hydrochloride and Timolol Maleate in Situ Gel for Glaucoma Treatment. Asian J. of Pharm. Ana. 2011 Oct-Dec 1(4):93-97.
2.    Allison K, et al. Epidemiology of Glaucoma: The Past, Present, and Predictions for the Future. Cureus. 2020 12(11). doi:10.7759/cureus.11686
3.    Yadav KS, et al. Glaucoma: Current treatment and impact of advanced drug delivery systems. Life Sci. 2019 Feb 221:362-376. doi:10.1016/j.lfs.2019.02.029
4.    Venkateswaran J, Venkataraman S. Pre-formulation study on API characterization of Brimonidine Tartrate, Timolol maleate and Dorzolamide Hydrochloride in Anti-glaucoma drugs. Research Journal of Pharmaceutical, Biological and Chemical Sciences. 2017 Jul-Aug 8(4):920-932.
5.    Mandour AA, et al. Review on analytical studies of some pharmaceutical compounds containing heterocyclic rings: brinzolamide, timolol maleate, flumethasone pivalate, and clioquinol. Futur J Pharm Sci. 2020 6(1). doi:10.1186/s43094-020-00068-4
6.    Mythili L, et al. Ocular Drug Delivery System – An Update Review. Research J. Pharm. and Tech. 2019 May 12(5). doi:10.5958/0974-360X.2019.00426.8
7.    Parveen N, Joshi H. Ocuserts: A Novel Formulation Approach in Drug Delivery System. Saudi J Med Pharm Sci. 2020 4929:420-425. doi:10.36348/sjmps.2020.v06i05.005
8.    Kompella UB, et al. Extraocular, periocular, and intraocular routes for sustained drug delivery for glaucoma. Progress in Retinal Eye Research. 2021 Sep 82. doi:10.1016/j.preteyeres.2020.100901
9.    Suresh PK, et al. Ocular implants as drug delivery device in opthalmic therapeutics: An overview. Research J. Pharm. and Tech. 2014 Jun 7(6):665-676.
10.    Kumar N, Sharma S. Design, formulation and evaluation of sustained ophthalmic delivery of ciprofloxacin from ocular inserts. Research J. Pharm. and Tech. 2013 6(3):285-286.
11.    Beena K. Ocular drug delivery system: Approaches to improve ocular bioavailability. GSC Biological and Pharmaceutical Sciences. 2019 6(3):1-10.
12.    Rathore KS, et al. Preparation and Characterization of Timolol Maleate Ocular Films. Int. J. PharmTech Res. 2010 2(3):1995-2000.
13.    Nair RV, et al. Ocular insert of Timolol Maleate using naturally occurring biodegradable polymer. J. Chem. Pharm. Res.  2015 7(7):476-485.
14.    Girish PK, Sreenivasa RM. Formulation and evaluation of extended release ocular inserts prepared from synthetic and natural biodegradable - biocompatible polymers. Research J. Pharm. and Tech. 2014 Jan 7(1):48-51.
15.    Dawaba HM, Dawaba AM. Development and evaluation of extended release ciprofloxacin HCl ocular inserts employing natural and synthetic film forming agents. J Pharm Investig. 2018 Jun. doi:10.1007/s40005-018-0400-x
16.    Jagdale S, et al. Optimization of Thermoreversible in Situ Nasal Gel of Timolol Maleate. Scientifica 2016. doi:10.1155/2016/6401267
17.    Karthikeyan D, et al. Design and Evaluation of Ofloxacin Extended Release Ocular Inserts For Once a Day Therapy. Research J. Pharm. and Tech. 2008 Oct-Dec 1(4):460-468.
18.    Dhaka M, et al. Preparation and assessment of ocular inserts containing sulbactum for controlled drug delivery. Journal of Drug Delivery & Therapeutics. 2020 10(1):66-71.
19.    Mujoriya RZ, Kshirsagar MD. Evaluation Study of Sustained Release Ocular Insert of Brimonidine Tartrate and Timolol. Res. J. Pharm. Dosage Form. & Tech. 2016 Oct-Dec 8(4)1-6.
20.    Karthikeyan D, et al. Development and Characterization of Modified Ocular Inserts with Improved Ocular Compatibility. Research J. Pharm. and Tech. 2008 Apr-Jun 1(2):93-99.
21.    Al-Juboori ZA, et al. Formulation and evaluation of ocular in-situ gelling system containing ciprofloxacin and naproxen sodium. Research J. Pharm. and Tech. 2021 14(1):91-95. doi:10.5958/0974-360X.2021.00017.2
22.    Shivhare UD. Effect of Combination of Hydrophilic an Hydrophobic Polymers on Trandermal Drug Delivery Systems Properties. Res. J. Pharm. Dosage Form. & Tech. 2011 3(5):203-209.
23.    Gajanan GV, et al. Methods for Evaluation of Ocular Insert with Classification and Uses in Various Eye Diseases - A Review. Asian J. Pharm. Tech. 2017 7(4):261-267. doi: 10.5958/2231-5713.2017.00038.1
24.    Gorle AP, Gattani SG. Design and Evaluation of Polymeric Ocular Drug Delivery System. Chem. Pharm. Bull. 2009 57(9):914-919.
25.    Valarmathi S, et al. In Vivo studies of Ophthalmic Ocular Insert Containing Aciclovir. Research J. Pharm. and Tech. 2017 10(7):2139-2142. doi: 10.5958/0974-360X.2017.00376.6
26.    Mohabe V, et al. Preparation and evaluation of captopril transdermal patches. Bull Pharm Res. 2011 1(2):47-52.
27.    Shafie A, Rady H. In vitro and In vivo Evaluation of Timolol Maleate Ocular Inserts Using Different Polymers. J Clin Exp Ophthalmo. 2012 3(8). doi:10.4172/2155-9570.1000246
28.    Al-Samman HB, Al-Laham A. Transdermal drug delivery system of sodium cromoglycate. Int. J. Pharm. Sci. Rev. Res. 2016 36(2):1-7.
29.    Mehta P, et al. Development and characterisation of electrospun timolol maleate-loaded polymeric contact lens coatings containing various permeation enhancers. International Journal of Pharmaceutics. 2017 532(1):408-420. doi:10.1016/j.ijpharm.2017.09.029
30.    Thakkar V, et al. Formulation and in Vitro - in Vivo Evaluations of Timolol Maleate Viscous Eye Drops for the Treatment of Glaucoma. Eur J Biomed Pharmaceu. 2016 Sep 3(9):573-585.

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.5958/0974-360X 

1.3
2021CiteScore
 
56th percentile
Powered by  Scopus


SCImago Journal & Country Rank

Journal Policies & Information


Recent Articles




Tags


Not Available