Ketorolac Tromethamine for Sustained Ocular Delivery; Novel In-Situ Gels Development and Evaluation

Authors

  • Rohit Kumar Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.
  • Vandana Sharma Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.
  • Mukesh Sharma Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.
  • S. L Soni Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

DOI:

https://doi.org/10.22270/ajprd.v9i4.984

Keywords:

Ketorolac tromethamine ,In-situ gels , Ocular delivery , Bio adhesive in-situ gelling , Draize test , Sustained release.

Abstract

Objective: Ophthalmic ketorolac is used to treat itchy eyes caused by allergies. It also is used to treat swelling and redness (inflammation) that can occur after cataract surgery. Ketorolac is in a class of medications called nonsteroidal anti-inflammatory drugs (NSAIDs).

Methods: Ocular bioavailability is always poor from conventional ophthalmic drops due to spillage and nasolachrymal drainage. Ocular in situ gels can increase the drug residence time thus increasing bioavailability. Polyacrylic acid (Carbopol 934) was used as the gelling agent in combination with hydroxypropylmethylcellulose (Methocel K4M) which acted as a viscosity enhancing agent. Compatibility studies of the drug excipients were carried out using differential scanning calorimetry. The prepared formulations were characterized for clarity, pH, drug content, sol-to-gel transition by scanning electron microscopy, in-vitro and in-vivo drug release, ocular irritation and stability.

Results: FTIR spectras revealed that, there was no interaction between LEV and excipients. The formulated gels were transparent, uniform in consistency and had spreadability with a pH range of 7.1 to 7.4. Rheological studies revealed that the formulations were psuedoplastic in nature, drug content of sterile in situ gels was found to be 92-98%.Release kinetic study showed that the formulation followed first order diffusion controlled and the optimized formulations was having good antibacterial efficacy.

Conclusion: The said promising formulation (F4) would be able to offer benefits such as increase residence time, prolonged drug release, reduction in frequency of administration and thereby definitely prove to improve the patient compliance.

 

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Author Biographies

Rohit Kumar, Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Vandana Sharma, Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Mukesh Sharma, Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

S. L Soni, Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

Department of Pharmaceutics, Arya College of Pharmacy, Jaipur, 302028, Rajasthan, India.

References

1. Grass GM, Robinson JR. Relationship of chemical structure to corneal penetration and influence of low-viscosity solution on ocular bioavailability. J Pharm Sci. 1984; 73:1021–7.
2. Martin RG, Jolly RP, Megha B, Dharmesh MM. A pH-triggered In situ gel-forming ophthalmic drug delivery system for tropicamide. Drug Delivery technology 2007; 44-49.
3. Jain D, Carvalho E, Banerjee R, Biodegradable hybrid polymeric membranes for ocular drug delivery. Acta Biomater 2010; 6(4):1370-1379.
4. Zignani M, Tabatabay C, Gurny R, Topical semi-solid drug delivery: kinetics and tolerance of ophthalmic hydrogels. Advanced Drug Delivery Reviews1995; 16(1):51-60.
5. Jadhav Pankaja, Yadav Adhikraob, Design, Development and Characterization of Ketorolac Tromethamine Nanosuspension Loaded In-Situ Mucoadhesive Ocular Gel. Journal of Drug Delivery and Therapeutics. 2019; 9(4-s) 203.
6. H. O. Ho, H. L. Su, T. Tsai, et al. The preparation and characterization of solid dispersions on pellets using a fluidized-bed system. Int. J. Pharm., 1996; 139: 223-229.
A. Gomez-Carracedo, C. A. Lorenzo, J. L. Gomez-Amoza, et al. Glass transitions and viscoelastic properties of Carbopol® and Noveon® compacts. Int. J. Pharm., 2004; 274: 233-243.
7. P. V. Devarajan, S. P. Gore, S. V. Chavan. HPTLC determination of ketorolac tromethamine. J. Pharm. Biomed. Anal., 2000, 22: 679-683.
8. Chunjie WU, Hongyi QI, Chen W, Huang C. Preparation and evaluation of a carbopo /HPMC-based in situ gelling ophthalmic system for puerarin. The pharmaceutical society of Japan 2007; 127(1):183-191.
9. Abraham S, Furtado S, Bharath S, Basavaraj BV, Deveswaran R, Madhavan V. Sustained ophthalmic delivery of ofloxacin from an ion- activated in situ gelling system. Pak. J. Pharm. Sci 2009; 175 - 179.
10. Satish kumar P et al Insitu Ophthalmic gel of Ciprofloxacin Hydrochloride for once a day sustained delivery. Drug Development and Industrial Pharmacy, 2008; 34:445–452.
11. Sultana , et al. Evaluation of carbopomethl cellulose based sustained release ocular delivery system for pefloxacin mesylate using rabbit eye modal. Pharm. Dev. Technol. 2006; 11:313-319.
12. Khan N, aqil M, imam SS, ali A, development and evalution of a novel in situ gel of sparfloxacin for sustaqined ocular drug delivery: in vitro and ec vivo characterization. Pharm dev technol 2015; 20(6):662-9.
13. LI J, Zhao H, Okele Cl, et al. Comparison of systemic absorption between ofloxacin ophthalmic in situ gels and administration to rabbit eyes by HPLC-MS/MS. Int J pharm 2013; 450(1-2):104-13.
14. Devasani SR, Dev A, Rathod S, Deshmukh G. an Overview of 2016; 3(1):60-9.
15. Katarina Edsman, Johan Carlfors Rheological evaluation of poloxamer as an in situ gel for ophthalmic use. European Journal of Pharmaceutical Sciences, 1998; 6:105–112 (1a, 2 a).
16. Satish kumar P. Jain, Sejal P. Shah, Namita S. Rajadhyaksha, Pirthi Pal Singh P. S., and Purnima D. Amin. Insitu Ophthalmic gel of Ciprofloxacin Hydrochloride for once a day sustained delivery. Drug Development and Industrial Pharmacy, 2008; 34:445–452.
17. Pharmacopoeia of the United States of America, 23rd ed. Mack Publishing Co. Pennsylvania. 1995; 1360-1364.
18. Jones D, Lawlor M and Woolfson A: Examination of the flow rheological and textural properties of polymer gels composed of poly (methylvinylether-comaleic anhydride) and poly (vinylpyrrolidone): rheological and mathematical interpretation of textural parameters. Journal of Pharmaceutical Sciences 2002; 91: 2090-2101.
19. Le Bourlais CA, Treupel-Acar L, Rhodes CT, Sado PA and Leverge R. New ophthalmic drug delivery systems. Drug Dev. Ind. Pharm. 1995; 21:19.
20. Jones D, Woolfson A and Brown A: Textural, viscoelastic and mucoadhesive properties of pharmaceutical gels composed of cellulose polymers. International Journal of Pharmaceutics 1997; 151:223-233.
21. Doijad RC, Manvi FV and Malleswara Rao VS. Sustained ophthalmic delivery of gatifloxacin from In situ gelling system. Ind. Pharm. Sci. 2006; 68: 814-818.
22. Edsman K, Carlfors J and Harju K. Rheological evaluation and ocular contact time of some carbomers gels for ophthalmic use. Int. J. Pharm. 1996; 137: 233.
A. K. Dash, Z. Gong, D. W. Miller, et al. Development of a rectal nicotine delivery system for the treatment of ulcerative colitis. Int. J. Pharm., 1999; 190: 21-34.
23. L. A. Kanis, F. C. Viel, J. S. Crespo, et al. Study of poly(oxyethylene oxide)/carbopol blends through thermal analysis and infrared spectroscopy. Polymer., 2000; 41:3303-3309.
24. J-K. Park, D-W. Kim, C-H. Kim, et al. Effect of drying conditions in the glass transition of poly(acrylic acid). Polym. Eng. Sci., 1991; 31: 867-872. A A. Gomez-Carracedo, C.
25. Lorenzo, J. L. Gomez-Amoza, et al. Glass transitions and viscoelastic properties of Carbopol® and Noveon® compacts. Int. J. Pharm., 2004; 274: 233-243.

Published

2021-08-15

How to Cite

Kumar, R., Sharma, V., Sharma, M., & Soni, S. L. (2021). Ketorolac Tromethamine for Sustained Ocular Delivery; Novel In-Situ Gels Development and Evaluation. Asian Journal of Pharmaceutical Research and Development, 9(4), 21–30. https://doi.org/10.22270/ajprd.v9i4.984

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