Home Levofloxacin loaded gelrite-cellulose polymer based sustained ocular drug delivery: formulation, optimization and biological study
Article
Licensed
Unlicensed Requires Authentication

Levofloxacin loaded gelrite-cellulose polymer based sustained ocular drug delivery: formulation, optimization and biological study

  • Mohammed Aslam , Syed Sarim Imam , Mohammed Aqil EMAIL logo , Yasmin Sultana and Asgar Ali
Published/Copyright: January 12, 2016
Become an author with De Gruyter Brill

Abstract

In the present work, levofloxacin in situ gel formulation was developed using gelrite as a gelling agent in combination with hydroxy propyl methyl cellulose. The developed formulations were evaluated for physicochemical parameters, in vitro release, ex vivo transcorneal study, sterility testing, antimicrobial efficacy, ocular irritation study, histopathological and stability evaluation. The in vitro drug release study showed the extended drug release up to 12 h, and the best fit kinetic model was found to be Peppas model (R2=0.9654), suggesting a Fickian diffusion process. The developed formulations showed optimized physicochemical results for all parameters. The optimized formulation showed therapeutically efficacious antimicrobial activity. Hens egg test-chorioallantoin membrane assay (HET-CAM) showed a mean score of 0.33 up to 24 h, which indicated the non-irritant property of the developed formulation. This non-irritant and stable in situ gel formulation of levofloxacin was found to be promising and safe for use as ocular delivery. The degradation rate constant and shelf life of developed optimized formulation (F14) were found to be low (1.213×10-4 at 25°C) and 2.14 years, respectively. This renders them favorable for ocular use as they would gel once in contact with the tear fluid, thus reducing nasolacrimal drainage, but would thin upon shearing, preventing ocular irritation and therefore induced lacrimation.


Corresponding author: Mohammed Aqil, Faculty of Pharmacy, Hamdard University, New Delhi 110 062, India, e-mail:

Acknowledgments

The authors are thankful to Promed Pvt. Limited, for providing the gift sample of LEV. The authors are also thankful to Jamia Hamdard for providing the necessary facility. The author (M. Aslam) is thankful to UGC, New Delhi, for providing the fellowship during his study.

  1. Conflict of interest statement: The authors declare no conflicts of interest.

References

[1] Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. J. Drug Target. 2011, 19, 409–417.10.3109/1061186X.2010.504268Search in Google Scholar PubMed

[2] Rupenthal ID, Colin RG, Raid GA. Int. J. Pharm. 2011, 411, 69–77.10.1016/j.ijpharm.2011.03.042Search in Google Scholar PubMed

[3] Almeida H, Amaral MH, Labao P, Sousa LJM. Expert Opin. Drug Deliv. 2013, 10, 1223–1237.10.1517/17425247.2013.796360Search in Google Scholar PubMed

[4] Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G, Jain S. AAPS Pharm. Sci. Tech. 2009, 10, 540–546.10.1208/s12249-009-9238-xSearch in Google Scholar PubMed PubMed Central

[5] Krauland AH, Leitner VM, Bernkop-Schnurch A. J. Pharm. Sci. 2003, 92, 1234–1241.10.1002/jps.10371Search in Google Scholar PubMed

[6] Balasubramaniam J, Kant S, Pandit JK. Acta Pharm. 2003, 53, 251–261.Search in Google Scholar

[7] Balasubramaniam J, Pandit JK. Drug Deliv. 2003, 10, 185–191.10.1080/713840402Search in Google Scholar PubMed

[8] Sultana Y, Aqil M, Ali A, Zafar S. Pharm. Dev. Tech. 2006, 11, 313–319.10.1080/10837450600767698Search in Google Scholar PubMed

[9] Kalam MA, Sultana Y, Samad A, Ali A, Aqil M, Sharma M, Mishra AK. J. Disp. Sci. Tech. 2008, 29, 89–96.10.1080/01932690701688482Search in Google Scholar

[10] Keating GM. Drugs 2009, 69, 1267–1286.10.2165/00003495-200969090-00009Search in Google Scholar PubMed

[11] Gupta H, Aqil M, Khar RK, Ali A, Bhatnagar A, Mittal G. Nanomed. Nanotech. Biol. Med. 2010, 6, 324–333.10.1016/j.nano.2009.10.004Search in Google Scholar PubMed

[12] Lin H, Sung KC. J. Control Rel. 2000, 69, 379–388.10.1016/S0168-3659(00)00329-1Search in Google Scholar

[13] Khan N, Aqil M, Ameeduzzafar, Imam SS, Ali A. Pharm. Dev. Tech. 2014, 1–8.Search in Google Scholar

[14] Naresh A, Vipin S, Vijay KB, Atul G, Monika H, Jyoti S, Kunal N. Rasayan J. Chem. 2008, 1, 564–566.Search in Google Scholar

[15] Srividya B, Cardoza RM, Amin PD. J. Control Rel. 2001, 73, 205–211.10.1016/S0168-3659(01)00279-6Search in Google Scholar

[16] Gupta H, Jain S, Mathur R, Mishra P, Mishra AK, Velpandian T. Drug Deliv. 2007, 14, 507–515.10.1080/10717540701606426Search in Google Scholar

[17] Sindhu A, Sharon F, Bharath S, Basavaraj BV, Deveswaran R, Madhavan V. Pak. J. Pharm. Sci. 2009, 22, 175–179.Search in Google Scholar

[18] Spielmann H, Liebsch M, Moldenhauer F, Holzhütter HG, Bagley DM, Lipman JM, Pape WJ, Miltenburger H, de Silva O, Hofer H, Steiling W. Food Chem. Toxicol. 1997, 35, 39–66.10.1016/S0278-6915(96)00103-2Search in Google Scholar

[19] Luepke NP. Food Chem. Toxicol. 1985, 23, 287–291.10.1016/0278-6915(85)90030-4Search in Google Scholar

[20] Velpandian T, Bankoti R, Humayun S, Ravi AK, Kumari SS, Biswas NR. Ind. J. Exp. Biol. 2006, 44, 387–391.Search in Google Scholar

[21] Ameeduzzafar, Ali J, Bhatnagar A, Kumar N, Ali A. Int. J. Bio. Macromol. 2014, 65, 479–491.10.1016/j.ijbiomac.2014.02.002Search in Google Scholar PubMed

Received: 2015-5-16
Accepted: 2015-10-2
Published Online: 2016-1-12
Published in Print: 2016-10-1

©2016 Walter de Gruyter GmbH, Berlin/Boston

Downloaded on 13.9.2025 from https://www.degruyterbrill.com/document/doi/10.1515/polyeng-2015-0218/html
Scroll to top button