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Keratin Formed Bioadhesive Ophthalmic Gel for the Bacterial Conjunctivitis Treatment

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Abstract

Keratin has the potential to function as the gel matrix in an ophthalmic formulation for the encapsulation of the macrolide antibiotic azithromycin. The quality of this formulation was thoroughly evaluated through various analyses, such as in vitro release assessment, rheological examination, intraocular retention studies in rabbits, assessment of bacteriostatic efficacy, and safety evaluations. It is worth mentioning that the gel demonstrated shear thinning properties and exhibited characteristics of an elastic solid, thereby confirming its structural stability. The gel demonstrated a notable affinity for mucosal surfaces in comparison to traditional azithromycin aqueous solutions. In vitro release testing revealed that drug release transpired via diffusion mechanisms, following a first-order kinetic release pattern. Additionally, the formulated gel exhibited remarkable antibacterial efficacy against Staphylococcus aureus and Pseudomonas aeruginosa in bacteriostatic evaluations. Lastly, safety assessments confirmed that the gel eye drops induced minimal irritation and displayed no apparent cytotoxicity, indicating their good safety and biocompatibility for ocular application. Thus, these findings indicated that the prepared azithromycin gel eye drops complied with the requisite standards for ophthalmic preparations.

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Acknowledgements

The authors would like to thank NMPA Key Laboratory for Research and Evaluation of Pharmaceutical Preparations and Excipients, China Pharmaceutical University for providing the instruments and equipment related to the paper.

Funding

This work was supported by the Taizhou Science and Technology Supporting Agriculture Project (TN202006) and the Medical Science Research of Hebei Province (20230403).

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, 639 Longmian Avenue, Nanjing, 211198, China

    Mengjuan Sun, Mengrong Wang & Yan Shen

  2. School of Life Science & Technology China, Pharmaceutical University24# Tongjiaxiang , Nanjing, 210009, China

    Qian Li

  3. Ophthalmology Department, Hebei General Hospital, 348 Heping West Road, Shijiazhuang, 050057, China

    Jialin Niu & Yin Zhang

  4. Jiangsu Agri-animal Husbandry Vocational College, Taizhou, 225300, Jiangsu Province, China

    Xiaolan Chen & Yujuan Mao

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Contributions

M.S.: formal analysis, date curation, writing-original draft. J.N.: formal analysis, methodology, investigation. Y.Z.: formal analysis, methodology, date curation, validation. M.W. and Y.S.: characterization, software. Y.M., X.C., and Q.L.: conceptualization, methodology, resources, supervision, formal analysis, writing review and editing.

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Correspondence to Yujuan Mao or Qian Li.

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Sun, M., Niu, J., Zhang, Y. et al. Keratin Formed Bioadhesive Ophthalmic Gel for the Bacterial Conjunctivitis Treatment. AAPS PharmSciTech 25, 77 (2024). https://doi.org/10.1208/s12249-024-02772-3

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