FORMULATION AND OPTIMIZATION OF THERMOSENSITIVE IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OCULAR DRUG DELIVERY

Authors

  • Chitra Gupta Amity Institute of Pharmacy, Amity University Noida, UP, INDIA
  • Vijay Juyal Department of Pharmaceutical Sciences, Bhimtal Campus, Kumaun University, Nainital, Uttarakhand, India
  • Upendra Nagaich Amity Institute of Pharmacy, Amity University Noida, UP, INDIA

DOI:

https://doi.org/10.22159/ijap.2018v10i3.25083

Keywords:

Ocular in-situ gel, Pluronic F-127, Gellan-gum, Carbopol, Nil, Bioavailability

Abstract

Objective: The present study has focused on development and optimization of thermosensitive in-situ ocular drug delivery system for the treatment of conjunctivitis.

Methods: Thermosensitive in-situ hydrogel formulation of moxifloxacin hydrochloride was developed by dispensing variable concentration of pluronic F-127, gellan-gum, and carbopol in distilled water. Viscosity, gelation temperature and mean release time (MRT) were measured by using ‘Brookfield' viscometer LV-III (spindle no. 40), rheological techniques and dissolution apparatus respectively. Optimization for ideal formulation was carried by ‘Box–Behnken' design on the basis of prime factors of the formulation including viscosity, gelation temperature, and MRT. Moreover, the optimized formulation was evaluated for accelerated stability study by in vitro drug release, anti-microbial potential by ‘Kirby-Bauer disk diffusion' method and ocular irritancy assay were done by in vivo analysis.

Results: Optimised thermosensitive in-situ gel, when administered into cul-de-sac region of the eye, it was immediately transformed from sol to gel by multi-dimensional mechanism due to plurionic, gellan-gum, carbopol. The optimized formulation minimizes the chances of formulation failure as well as the concentration on individual polymer which dependence on a single mechanism of gelation. The final optimised formulation consists of plurionic (11.50% w/v), gellan-gum (0.32% w/v), carbopol (0.3% w/v), shows optimum therapeutic effect. Moreover, the accelerated stability study, anti-microbial potential, and ocular irritancy confirmed the biocompatibility of optimized in-situ drug-containing gel with high potency and stability.

Conclusion: Thus, optimized in-situ drug-containing gel with multifactorial approaches showed promising ocular formulation having minimum side effect and high therapeutic efficacy.

 

Downloads

Download data is not yet available.

References

Gariepy ER, Leroux JC. In situ-forming hydrogels-review of temperature-sensitive systems. Eur J Pharm Biopharm 2004;58:409-26.

Jeong B, Kim SW, Baeb YH. Thermosensitive sol-gel reversible hydrogels. Adv Drug Delivery Rev 2002;54:37-51.

Tang YF, Du YM, Hu XW, Shi XW, Kennedy JF. Rheological characterisation of a novel thermosensitive chitosan/poly(vinyl alcohol) blend hydrogel. Carbohydr Polym 2007;67:491-9.

Kumar S, Haglund BO, Himmelstein KJ. In situ-forming gels for ophthalmic drug delivery. J Ocul Pharmacol 1994;10:47-56.

Gurny R. Preliminary study of prolonged acting drug delivery system for the treatment of glaucoma. Pharm Acta Helv 1981;56:130-2.

Morsi N, Ghorab D, Refai H, Teba H. Preparation and evaluation of alginate/chitosan nanodispersions for ocular delivery. Int J Pharm Pharm Sci 2015;7:234-40.

Miller SC, Donovan MD. Effect of poloxamer 407 gel on the miotic activity of pilocarpine nitrate in rabbits. Int J Pharm 1982;12:147-52.

Desai SD, Blanchard J. In vitro evaluation of pluronic F127-based controlled-release ocular delivery systems for pilocarpine. J Pharm Sci 1988;87:226-30.

Rozier A, Manuel C, Groove J, Plazonnet B. Gelrite: a novel, ion-activated, in situ gelling polymer for ophthalmic vehicles. Effect on the bioavailability of timolol. Int J Pharm 1989;57:163-8.

Paulsson M, Hägerström H, Edsman K. Rheological studies of the gelation of deacetylated gellan-gum (Gelrite®) in physiological conditions. Eur J Pharm Sci 1999;9:99-105.

Joshi A, Ding S, Himmelstein KJ. Reversible gelation compositions and methods of use. US Patent 5252318; 1993.

Kumar S, Himmelstein KJ. Modification of in situ gelling behaviours of carbopol solutions by hydroxypropyl methylcellulose. J Pharm Sci 1995;84:344-8.

Oliphant CM, Green GM. Quinolones: a comprehensive review. Am Fam Physician 2002;65:455-64.

Grillon A, Schramm F, Kleinberg M, Jehl F. Comparative activity of ciprofloxacin, levofloxacin and moxifloxacin against Klebsiella pneumoniae, Pseudomonas aeruginosa and Stenotrophomonas maltophilia assessed by minimum inhibitory concentrations and time-kill studies. PLoS One 2016;11:0156690.

Gohel MC, Panchal MK. Novel use of similarity factors f2 and Sd for development of diltiazem HCl modified-release tablets using a 32 factorial design. Drug Dev Ind Pharm 2002;28:77-87.

Kadam AT, Jadhav RL, Salunke PB, Kadam SS. Design and evaluation of modified chitosan-based in situ gel for ocular drug delivery. Int J Pharm Pharm Sci 2017;9:87-91.

Choi HG, Oh YK, Kim CK. In situ gelling and mucoadhesive liquid suppository containing acetaminophen: enhanced bioavailability. Int J Pharm 1998;165:23-32.

Jan Hudzicki. Kirby-bauer disk diffusion susceptibility test protocol; 2009.

Mathews BR. Regulatory features of stability testing in Europe. Drug Dev Ind Pharm 1999;25:831-56.

Vijayanand P, Deepa A, Bhagavan Raju M. Development, characterization and evaluation of soft oral edible gel using gellan-gum. Int J Appl Pharm 2017;9:73-7.

Srivastava R, Srivastava S, Singh SP. Thermoreversible in-situ nasal gel formulations and their pharmaceutical evaluation for the treatment of allergic rhinitis containing extracts of moringa olifera and embeliaribes. Int J Appl Pharm 2017;9:16-20.

Published

07-05-2018

How to Cite

Gupta, C., Juyal, V., & Nagaich, U. (2018). FORMULATION AND OPTIMIZATION OF THERMOSENSITIVE IN-SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE FOR OCULAR DRUG DELIVERY. International Journal of Applied Pharmaceutics, 10(3), 123–130. https://doi.org/10.22159/ijap.2018v10i3.25083

Issue

Section

Original Article(s)