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Cationic Polyelectrolyte Nanocapsules of Moxifloxacin for Microbial Keratitis Therapy: Development, Characterization, and Pharmacodynamic Study

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Abstract

Microbial keratitis (MK) is a vision-threatening disease and the fourth leading cause of blindness worldwide. In this work, we aim to develop moxifloxacin (MXN)-loaded chitosan-based cationic mucoadhesive polyelectrolyte nanocapsules (PENs) for the effective treatment of MK. PENs were formulated by polyelectrolyte complex coacervation method and characterized for their particle size, surface charge, morphology, mucoadhesive property, in-vitro and ex-vivo release, ocular tolerance, and antimicrobial efficacy studies. The pharmacodynamic study was conducted on rabbit eye model of induced keratitis and it is compared with marketed formulation (MF). Developed PENs showed the size range from 230.7 ± 0.64 to 249.0 ± 0.49 nm and positive surface charge, spherical shape along with appropriate physico-chemical parameters. Both in-vitro and ex-vivo examination concludes that PENs having more efficiency in sustained release of MXN compared to MF. Ocular irritation studies demonstrated that no corneal damage or ocular irritation. The in-vivo study proved that the anti-bacterial efficacy of PENs was improved when compared with MF. These results suggested that PENs are a feasible choice for MK therapy because of their ability to enhance ocular retention of loaded MXN through interaction with the corneal surface of the mucous membrane.

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Acknowledgement

The authors deeply recognize the help of the Department of University Institute of Pharmacy and the SOS in Physics and Astrophysics, Pt. Ravishankar Shukla University, Raipur, Chhattisgarh, India, for carrying out the particle size specification and DSC pattern of the samples respectively. The authors acknowledge the support of Department of metallurgical engineering, National Institute of Technology, Raipur, Chhattisgarh, India for performing the XRD analysis samples. The authors were indebted to acknowledge Department of Anatomy, AIIMS, New Delhi, India for performing TEM images of samples. The authors would like to record their truthful thanks to the Department of Biotechnology, Guru Ghasidas University, Bilaspur to accomplish the antimicrobial efficacy studies. The authors were ever grateful to Orex Pharma Pvt. Ltd. (Mumbai, India) for supplying the gift sample.

Funding

Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur (C.G), Chhattisgarh, India has provided financial support in the form of a fellowship to carry out the research work.

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  1. Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, Chhattisgarh, 495009, India

    Parasuraman Mohan & Karthikeyan Kesavan

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Mohan, P., Kesavan, K. Cationic Polyelectrolyte Nanocapsules of Moxifloxacin for Microbial Keratitis Therapy: Development, Characterization, and Pharmacodynamic Study. AAPS PharmSciTech 22, 195 (2021). https://doi.org/10.1208/s12249-021-02039-1

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