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Journal of Pharmaceutical Research

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Formulation and Evaluation of Controlled Release of Ocular Inserts
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Journal of Pharmaceutical Research

DOI: 10.18579/jopcr/v19.2.anuradha

Year: 2020, Volume: 19, Issue: 2, Pages: 17-23

Original Article

Formulation and Evaluation of Controlled Release of Ocular Inserts

MS Anuradha1, S Alladi1,∗

1Department of Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore, Karnataka, India

Creative Commons License

This work is licensed under a Creative Commons Attribution 4.0 International License.

Abstract

Moxifloxacin hydrochloride (Moxifloxacin HCl) is a fluoroquinolone antibiotic widely used in ocular infections. Traditional eye drops are limited by rapid drainage and low bioavailability. This study aimed to formulate stable ocular inserts that provide sustained drug release, enhance antimicrobial efficacy, ensure ocular safety, and establish a strong in vitro–in vivo correlation for predictable therapeutic performance. The λmax of Moxifloxacin HCl in distilled water and simulated tear fluid was 288.5 nm. Drug-polymer compatibility was established through Fourier Transform Infrared spectroscopy. The ocular inserts were prepared using polyvinyl alcohol as the reservoir and ethyl cellulose as the rate-controlling membrane. Physicochemical characteristics, in vitro release of drug in Franz diffusion cell, antimicrobial activity in agar diffusion test, in vivo efficacy in rabbit model, and irritation potential using the Draize test were evaluated. The release kinetics and stability of the drug were studied. Formulation FM6 exhibited uniform thickness of 0.298 ± 0.02 mm with pH 7.27 and drug content of 0.991 ± 0.06 mg. The in vitro release exhibited 99.1% drug delivery within five days with Higuchi kinetics (R2 = 0.991). FM6 exhibits severe antimicrobial activity and sterility. Sustained release and lack of ocular irritation have been established by in vivo studies. Accelerated stability tests did not show any degradation for 3 months. The current study successfully developed and optimised a new sustained-release ocular insert for Moxifloxacin HCl with extended antimicrobial activity and enhanced patient compliance.

Keywords: Moxifloxacin HCl, Ocular Insert, Sustained Release, In Vitro, In Vivo

References

  1. Mishra G, Gaudana R, Tamboli V, Mitra A. Recent Advances in Ocular Drug Delivery. Targeted Delivery of Small and Macromolecular Drugs. 2010;p. 421–453. Available from: https://www.researchgate.net/publication/300340102_Recent_Advances_in_Ocular_Drug_Delivery
  2. Saettone MF, Salminen L. Ocular inserts for topical delivery. Advanced Drug Delivery Reviews. 1995;16(1):95–106. Available from: https://dx.doi.org/10.1016/0169-409x(95)00014-x
  3. Ludwig A. The use of mucoadhesive polymers in ocular drug delivery. Advanced Drug Delivery Reviews. 2005;57(11):1595–1639. Available from: https://doi.org/10.1016/j.addr.2005.07.005
  5. O'brien TP. Evidence-based Review of Moxifloxacin. International Ophthalmology Clinics. 2006;46(4):61–72. Available from: https://pubmed.ncbi.nlm.nih.gov/17060792/
  6. Urtti A. Challenges and obstacles of ocular pharmacokinetics and drug delivery. Advanced Drug Delivery Reviews. 2006;58(11):1131–1135. Available from: https://dx.doi.org/10.1016/j.addr.2006.07.027
  7. Sahane N, Banarjee S, Gaikwad D, Jadhav S, Thorat R. Ocular inserts: a review. International Journal of Current Research and Review. 2010;2(1):3–16. Available from: https://ijcrr.com/uploads/2279_pdf.pdf
  8. Rozier A, Mazuel C, Grove J, Plazonnet B. Gelrite®: A novel, ion-activated, in-situ gelling polymer for ophthalmic vehicles. Effect on bioavailability of timolol. International Journal of Pharmaceutics. 1989;57(2):163–168. Available from: https://dx.doi.org/10.1016/0378-5173(89)90305-0
  9. Sultana Y, Aqil M, Ali A. Ocular inserts for controlled delivery of pefloxacin mesylate: Preparation and evaluation. Acta pharmaceutica. 2005;55(3):305–314. Available from: https://pubmed.ncbi.nlm.nih.gov/16375841/
  10. Patel UL, Chotai NP, Nagda CD. Design and evaluation of ocular drug delivery system for controlled delivery of gatifloxacin sesquehydrate: In vitro and in vivo evaluation. Pharmaceutical Development and Technology. 2012;17(1):15–22. Available from: https://pubmed.ncbi.nlm.nih.gov/20649410/
  11. Rao MV, Shyale S. Preparation and Evaluation of Ocular Inserts Containing Norfloxacin. Turkish Journal of Medical Sciences. 2004;34(4):239–246. Available from: https://journals.tubitak.gov.tr/medical/vol34/iss4/4/
  12. Patel D, Patel M, Patel N, Patel M. Preparation and evaluation of ocular insert containing brimonidine tratrate. International Journal of Pharmacy and Clinical Research. 2009;1(1):19–22. Available from: https://impactfactor.org/PDF/IJPCR/1/IJPCR,Vol1,Issue1,Article5.pdf
  13. Costa P, Lobo JMS. Modeling and comparison of dissolution profiles. European Journal of Pharmaceutical Sciences. 2001;13(2):123–133. Available from: https://dx.doi.org/10.1016/s0928-0987(01)00095-1
  14. Sankar V, Chandrasekaran A, Durga S, Geetha G, Ravichandran V, Vijayakumar A, et al. Design and evaluation of diclofenac sodium ophthalmic inserts. Acta Pharmaceutica Sciencia. 2006;48:5–10. Available from: https://actapharmsci.com/uploads/pdf/pdf_88.pdf#:~:text=Diclofenac%20sodium%20ophthalmic%20inserts%20were,of%20medicated%20inserts%20were%20evaluated.
  15. Tanwar Y, Patel D, Sisodia S. In vitro and in vivo evaluation of ocular inserts of ofloxacin. DARU Journal of Pharmaceutical Sciences. 2007;15(03):139–145. Available from: https://www.researchgate.net/publication/279559819_In_vitro_and_in_vivo_evaluation_of_ocular_inserts_of_ofloxacin
  16. Mishra D, Gilhotra RM. Development studies on gel-forming erodible ocular polymeric films of Gatifloxacin sesquehydrate. ACTA Pharmaceutica Sciencia. 2008;50(2):145–152. Available from: https://www.actapharmsci.com/uploads/pdf/pdf_315.pdf
  17. Wilhelmus KR. The Draize Eye Test. Survey of Ophthalmology. 2001;45(6):493–515. Available from: https://dx.doi.org/10.1016/s0039-6257(01)00211-9
  18. Gevariya HB, Patel JK, Girhepunje K, Pal R. Sustained ophthalmic delivery of levofloxacin from once a day ocuserts. International Journal of Pharmacy and Pharmaceutical Sciences. 2009;1(1):24–32. Available from: https://www.researchgate.net/publication/265084460_Sustained_ophthalmic_delivery_of_levofloxacin_from_once_a_day_ocuserts
  19. Upadhyaya N, Patidar A, Agrawal S, Gupta D. Development and evaluation of polymeric sustained release levofloxacin ocuserts. Research Journal of Pharmaceutical. 2011;2(3):411–420.
  20. Pawar P, Katara R, Majumdar D. Design and evaluation of moxifloxacin hydrochloride ocular inserts. Acta Pharmaceutica. 2012;62(1):93–104. Available from: https://dx.doi.org/10.2478/v10007-012-0002-5
  21. Mandal S, Thimmasetty MK, Prabhushankar G, Geetha M. Formulation and evaluation of an in situ gel-forming ophthalmic formulation of moxifloxacin hydrochloride. International Journal of Pharmaceutical Investigation. 2012;2(2):78–82. Available from: https://dx.doi.org/10.4103/2230-973x.100042
  24. Yellanki SK, Anna B, Kishan MR. Preparation and in vivo evaluation of sodium alginate-poly (vinyl alcohol) electrospun nanofibers of forskolin for glaucoma treatment. Pakistan Journal of Pharmaceutical Sciences. 2019;32(2):669–674. Available from: https://pubmed.ncbi.nlm.nih.gov/31081781/

Copyright

© 2025 Published by Krupanidhi College of Pharmacy. This is an open-access article under the CC BY-NC-ND license (https://creativecommons.org/licenses/by-nc-nd/4.0/) 

  • 04 June 2025

Year: 2020, Volume: 19, Issue: 2


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