Formulation and optimisation of Ozenoxacin topical nano-emulgel including a comprehensive methodology to qualify and validate the critical parameters of an in-vitro release test method and ex-vivo permeation test

Abstract

Objective

The purpose of this study was to formulate, optimize Ozenoxacin topical nano-emulsion using factorial design followed by to prepare and evaluate nano-emulgel using validated in-vitro release testing (IVRT) technique for determination of Ozenoxacin release rate along with ex-vivo permeation testing (EVPT).

Significance: Nano-emulgel is a proven delivery system for poorly soluble substances works by enhancing the solubility and bioavailability. Factorial design provides a systematic and efficient means to study the effect of multiple factors on responses. IVRT is an USP compendia technique utilized for performance analysis of semi-solid formulations.

Methods

Nano-emulsion formulation optimization was done with factorial design, evaluated for globule size and % entrapment efficiency (EE). Nano-emulgels were characterized for assay, organic impurities, rheological behavior, IVRT, EVPT, and skin retention studies. IVRT validation was executed using vertical diffusion cells (VDCs).

Results

Ozenoxacin nano-emulsion was optimized with 1:1 ratio of Oil: S_mix, 3:1 ratio of Surfactant:Co-Surfactant, and 15000 RPM of homogenization speed which resulted 414.6 ± 5.2 nm globule size and 92.8 ± 2.1% entrapment efficiency. Results confirmed that IVRT and Reversed Phase – High Performance Liquid Chromatographic techniques were validated as per regulatory guidelines. In-vitro, ex-vivo drug release, and skin retention from the optimized nano-emulgel formulation was comparatively higher (∼1.5 times) than that from the innovator (OZANEX^TM) formulation.

Conclusions

Based on these results, Ozenoxacin nano-emulgel can be considered an effective alternative and was found to be stable at 40 °C/75% RH and 30 °C/75% RH storage condition for 6 months.

Keywords:

• Ozenoxacin
• nano-emulgel
• in-vitro release testing
• ex-vivo permeation testing
• skin retention
• vertical diffusion cells

Acknowledgments

Authors are thankful to Optimus Pharma Private Limited, Hyderabad for providing facilities to perform this research. One of the authors Amarnath Reddy Ramireddy is thankful to the Jawaharlal Nehru Technological University, Anantapur, for enrolling as a research scholar.

Ethical approval

The ex-vivo study was performed according to the institutional guidelines of the Animal Ethics Committee.

Author contributions

Amarnath Reddy Ramireddy: The acquisition, analysis, interpretation of data for the work and drafting of the work. Dilip Kumar Behara: The conception, design of the work, and final approval of the version to be published.

Data availability statement

All the relevant data are reported within the paper and or supplementary file. For additional details, data areavailable on request to the authors.

Disclosure statement

The authors declare that no potential conflicts of interest for this article's research, authorship, and/or publication.

Additional information

Funding

This research did not receive any specific grant from funding agencies in the public, commercial, or not-for-profit sectors.