Design and evaluation of in situ gel eye drops containing nanoparticles of Gemifloxacin Mesylate

Abstract

Traditional eye drops used for topically administering drugs have poor ocular bioavailability due to the biological barriers of the eye. There is an interest to design and develop novel drug delivery systems that would extend the precorneal residence time, reduce the frequency of administration and decrease dose-related toxicity. This study aimed to prepare Nanoparticles of Gemifloxacin Mesylate and incorporate them into an in situ gel. The nanoparticles were prepared by ionic gelation technique, using 3² factorial design. Sodium tripolyphosphate (STPP) was used to crosslink Chitosan. The optimized formulation of the nanoparticles (GF4) contained 0.15% Gemifloxacin Mesylate, 0.15% Chitosan and 0.20% STPP, producing 71 nm particle size and 81.11% entrapment efficiency. The prepared nanoparticles showed biphasic release, with an initial burst release of 15% in 1.0 hr and a cumulative drug release of 90.53% at the end of 24 hrs. After that, the prepared nanoparticles were incorporated into an in situ gel, using Poloxamer 407, producing a sustained drug release with efficient antimicrobial activity against gram-positive and gram-negative bacteria as confirmed by the cup plate method.

Keywords:

• Ocular drug delivery
• nanoparticles
• in situ gel
• Chitosan
• Poloxamer 407
• 3² factorial design
• antimicrobial activity

Acknowledgments

The authors extend their sincere appreciation to the Deanship of Scientific Research at King Khalid University, Saudi Arabia and Dean of scientific research of Zarqa university, Jordan for funding this work through Research Group. Project number RGP.2/251/43.

The Indian authors are very much thankful to J.J.C.E.Trust, Junagadh and Gujarat Technological University, Chandkheda, Ahmedabad

Disclosure statement

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Ethical approval

No Animals or Humans were involved in this work and hence no need of ethical approval.

Correction Statement

This article has been corrected with minor changes. These changes do not impact the academic content of the article.

Additional information

Funding

This Project was funded by King Khalid University, Saudi Arabia