FORMULATION AND EVALUATION OF CETIRIZINE HYDROCHLORIDE pH TRIGGED IN-SITU OCULAR GEL
DOI:
https://doi.org/10.22159/ijap.2023v15i2.46040Keywords:
Carbomer, HPMC, pH trigged in-situ ocular gel and bioavailability.Abstract
Objective: In the present research work, the aim was to prepare pH trigged in-situ ocular gel of Cetirizine Hydrochloride (CTZ) to improve its local bioavailability at the eye surface.
Methods: CTZ in-situ ocular gel was prepared by the pH-trigged method.In-situ CTZ ocular gel was prepared by a pH-sensitive gelling agent (Carbomer) with a one viscosity builder polymer (HPMC E4M).All formulation was evaluated for appearance, pH, viscosity at different pH, gelling capacity, % drug content, and drug release. Nine formulations were prepared and optimized successfully using 32 factorial designs. Optimization was done by DoE software version Version 13.0.10.064
Results: All nine formulations of in-situ ocular gel were subjected to evaluation. Out of 9 formulations, F3 had a good gelling capacity with the minimum amount of polymer. The appearance of the optimized formulation was translucent and homogenous. The pH of the F3 formulation is 5.55±0.07, which is good for maintaining formulation in the solution stage. Viscosity at 20 RPM of F3 formulation at pH 5.5 is 837.30±1.00 cps, this range of viscosity has good flow properties. Viscosity at 20 RPM of F3 formulation at pH 7.4 is 6800.74± 1.58cps, this range of viscosity has a good gelling capacity which helps to drug retain at the eye surface. Drug content is 100.16± 0.53%. Drug release at 300 min is 69.22 ± 2.12, it can say that the drug may be retained for more than 300 min at the eye surface which is good for reducing dosing frequency.,.
Conclusion: CTZ was successfully formulated in pH triggered in-situ gelling system using Carbomer 974P in combination with HPMC E4M. The prepared in-situ gel is easily converted from solution stage to gel stage at the pH of the eye so we can say that the drug in the in-situ ocular gel is more bioavailable than conventional ophthalmic solution In-vitro results indicated that the in-situ gel system is a viable alternative to conventional ocular drops by virtue of its ability to sustain drug release.
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References
Drug.com [Internet]. [Cited 20/12/2020]. Available from: https://www.drugs.com/history/zerviate.html
Shukr MH, Ismail S, El-Hossary GG, El-Shazly AH. Design and evaluation of mucoadhesive in-situ liposomal gel for sustained ocular delivery of travoprost using two steps factorial design. Journal of Drug Delivery Science and Technology. 2021; 61: 102333.
Balu A, Johnson T, Sundara R, Seetharaman S. Optimization and evaluation of temperature trig-gered in-situ gel formulation using design of experiments (DoE) and HET-CAM test. J Nanomed. 2020; 3(1): 1031.
Gupta C, Juya V, Nagaichm U. Formulation, optimization, and evaluation of in-situ gel of moxifloxacin hydrochloride for ophthalmic drug delivery, Int J App Pharm. 2019; 11(4): 147-158.
Kouchak M, Mahmoodzadeh M, Farrahi F. Designing of a pH-triggered carbopol®/hpmc in-situ gel for ocular delivery of dorzolamide hcl: in-vitro, in-vivo, and ex-vivo evaluation. AAPS PharmSciTech; 2019: 20(5): 210.
Hussain M. Temperature triggered in-situ gelling system for ocular antiviral drug. International Journal of Pharmaceutical Sciences and Research. 2019; 12(1): 281-291.
Li L, Guo D, Guo J, Song J. Thermosensitive in-situ forming gels for ophthalmic delivery of tea polyphenols. Journal of Drug Delivery Science and Technology. 2018; 46: 243-250.
Li P, Wang S, Chen H, Zhang S, Yu S, Li Y, Cui M, Pan W, Yang X. A novel ion-activated in-situ gelling ophthalmic delivery system based on kappa-carrageenan for acyclovir. Drug Development and Industrial Pharmacy. 2018; 44: 829-836.
Morsi N, Ibrahim M, Refai H. Nanoemulsion-based electrolyte triggered in-situ gel for ocular delivery of acetazolamide. European Journal of Pharmaceutical Sciences. 2017; 104: 302-314.
Ambikar RB, Bhosale AV. Development and characterization of diclofenac sodium loaded eudragit RS100 polymeric microsponge incorporated into in-situ gel for ophthalmic drug delivery system. International Journal of Pharmacy and Pharmaceutical Sciences. 2021; 13 (9):, 63-69.
Makwana SB, Patel VA, Parmar SJ. Development and characterization of in-situ gel for ophthalmic formulation containing ciprofloxacin hydrochloride. Results in Pharma Sciences. 2016; 6: 1-6.
Morsi N, Ghorab D, Refai H. Ketoroloac tromethamine loaded nanodispersion incorporated into thermosensitive in-situ gel for prolonged ocular delivery. International Journal of Pharmaceutics. 2016; 506: 57-67.
Patil S, Kadam A, Bandgar S, Patil S. Formulation and evaluation of an in-situ gel for ocular drug delivery of anticonjunctival drug. Cellulose Chem. Technol. 2015; 49 (1): 35-40.
Danilo A, Grazia SM, Barbara AM. Aqueous ophthalmic formulations based on azithromycin. WIPO Patent- WO 2014/181368.
National Liberal of Medicine [Internet]. [Cited 12/12/2019]. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2846103/
National Liberal of Medicine [Internet]. [Cited 20/12/2019]. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7978349/
Geethalakshmia A, Karkib R, Sagib P, Jhac SK, Pb VD. Temperature triggered in-situ gelling system for betaxolol in glaucoma. Journal of Applied Pharmaceutical Science, 2013; 3(02): 153-159.
Buchan B, Kay G, Heneghan A, Matthews KH, Cairns D. Gel formulations for treatment of the ophthalmic complications in cystinosis. International Journal of Pharmaceutics. 2010; 392 (1-2): 192-197.
Gupta H, Jain S, Mathur R Mishra P, Mishra AK. Sustained ocular drug delivery from a temperature and pH triggered novel in-situ gel system. Drug Delivery. 2007; 14: 507–515.
Rathore KS, Nema RK. An insight into ophthalmic drug delivery system. Int. J. Pharm. Sci. Drug. Res. 2009; 1: 1-5.
Patil JA, Patil B R. Formulation and evaluation of besifloxacin non-erodible ocular inserts. International Journal of Applied Pharmaceutics, 2022; 14(1): 148-155.
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