FORMULATION AND EVALUATION OF IN SITU OCULAR GEL OF LEVOFLOXACIN
Abstract
Total of 8 formulations of in situ gels of Levofloxacin hydrochloride were prepared by pH triggered in situ gelling system using different polymers like sodium alginate as gelling agent, Noveon AA-1 polycarbophil and HPMC E50LV as viscosity enhancing agent and benzalkonium chloride as preservative. All the prepared formulations were clear and the visual appearance was found to be transparent. The pH of the prepared formulations was ranged between 6.50and 7.00. The drug content varied between 96.84 ± 0.396 and 99.65±0.489 % which indicated that the uniform distribution of drug was found in all the prepared formulations. Among all the formulations, the formulations A4 and A8 showed better gelling capacity. The shear rate on the preparation was large during the blinking stage. From the in vitro drug release profile the formulations A4 and A8 was selected as the best formulations and these formulations were used for further studies such as mechanism of drug release, sterility, antimicrobial efficacy, ocular irritation and accelerated stability. Both formulations provided good fit to the Higuchi model. According to this model, the drug release from these gels may be controlled by diffusion through the micro-pores. The selected formulations showed good anti-microbial action against the organisms and ocular irritation studies revealed that the selected formulations were good with non-irritation and there were no ocular damage or abnormal clinical signs. During and at the end of the accelerated stability study, the selected formulations did not undergo any chemical changes/interaction and remained stable during the study period and showed almost similar physical stability and drug content.
Key Words: Levofloxacin hydrochloride, in situ gels, in vitro drug release, Higuchi model, accelerated stability study.
Â
Downloads
References
2. Rajas NJ, Kavitha K, Gounder T, Mani T,In situopthalmic gels: a developing trend,Int J Pharma Sci Rev Res,2011; 7(1):8-14.
3. Rathore KS, In situ gelling ophthalmic drug delivery system: an overview, Int J Ph Pharma Sci, 2010, 2(4), 30-34.
4. Mohanambal E, Arun K,SathaliHA, Formulation and Evaluation of pH-triggered in situ Gelling System of Levofloxacin, Ind J Pharm Edu Res, 2011; 45(1):58-64.
5. Diren S, Zeynep FK,Bioavailability File: Levofloxacin, J PharmSci, 2007; 32:197-208.
6. Nayak NS, Bharani SS, Thakur RS, Formulation and evaluation of pH triggered in situ ophthalmic gel of Moxifloxacin hydrochloride,Int J Pharm PharmSci, 2012; 4(2):452-459.
7. Srividya, Rita MC, Amin PD, Sustained ocular delivery of Ofloxacin from a pH activated in situ gelling system, J Control Rel, 2001, 73, 205-211.
8. Gokulgandhi MR, Parikh JR, Barot MM, Modi DM. A pH activated in situ gel forming ocular drug delivery system used for tropicamide, Drug Delivery Technology, 2007; 5:44-49.
9. Zhidong L, Jiawei L, Shufang N, Hui L, Pingtian D, Weisan P, Study of HPMC/alginate based in situ gelling ocular delivery system for gatifloxacin. Int J Pharm, 2006; 315:12-17.
10. Indu PK, Manjit S, Meenakshi K, Preparation and evaluation of ocular formulations of acetazolamide, Int J Pharm, 2000, 199,119-127.
11. Pandit D, Bharathi A, Srinatha R, Singh S, Long acting ophthalmic preparations of indomethacin: Assessment of gel systems of alginate, Indian J Pharm Sci, 2007; 69:37-40.
12. Mandal S, Manjunath KMJ, Thimmasetty M, GL Prabhushankar, Geetha MS, Preparation and evaluation of an in situ gel forming ophthalmic preparations of moxifloxacin hydrochloride, International Journal of Pharmaceutical Investigation, 2012; 2 (2):78-82.
13. Higuchi T, Rate of release of medicaments from ointment bases containing drugs in suspension, J PharmSci, 1961, 50, 874-875.
14. Korsmeyer RW, Gurny R, Doelker E, Buri P and Peppas NA, Mechanism of potassium chloride release from compressed hydrophilic polymeric matrices: effect of entrapped air, JPharmSci, 1983; 72(10):1189-1191.
15. Controller of Publication, Indian Pharmacopoeia, Ministry of Health and Family Welfare, Government of India, New Delhi, 2007.
16. Draize J, Woodward G, Calvery O, Methods for the study of toxicity and irritation of substance applied locally to the skin surface and mucous membrane, J Pharm Col ExpTher, 1994; 82:377-390.
17. Mathews BR, Regulatory features of stability testing in Europe, Drug Dev Ind Pharm, 1999; 25:831-856.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).