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Exploring Penetration Ability of Carbonic Anhydrase Inhibitor–Loaded Ultradeformable Bilosome for Effective Ocular Application

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Abstract

Brinzolamide is an effective carbonic anhydrase inhibitor widely used in glaucoma therapy but limits its application due to inadequate aqueous solubility and permeability. The aim of the present research work is the development and characterization of brinzolamide-loaded ultradeformable bilosomes to enhance the corneal permeation of the drug. These ultradeformable bilosomes were prepared by ethanol injection method and evaluated for physicochemical properties, particle size, morphology, drug release, ultra-deformability, corneal permeation, and irritation potential. The optimized formulation exhibited an average particle size of 205.4 ± 2.04 nm with mono-dispersity (0.109 ± 0.002) and showed entrapment efficiency of 75.02 ± 0.017%, deformability index of 3.91, and release the drug in a sustained manner. The brinzolamide-loaded ultradeformable bilosomes released 76.29 ± 3.77% of the drug in 10 h that is 2.25 times higher than the free drug solution. The bilosomes were found non-irritant to eyes with a potential irritancy score of 0 in Hen’s egg-chorioallantoic membrane assay. Brinzolamide-loaded ultradeformable bilosomes showed 83.09 ± 5.1% of permeation in 6 h and trans-corneal permeability of 8.78 ± 0.14 cm/h during the ex vivo permeation study. The acquired findings clearly revealed that the brinzolamide-loaded ultradeformable bilosomes show promising output and are useful in glaucoma therapy.

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Acknowledgements

The authors would like to acknowledge the Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Hyderabad (Ministry of Chemical and Fertilizers, India) for providing extended facilities during this manuscript (manuscript communication no.: NIPER-H/2022).

Funding

The author (NKM) received a research grant from the Department of Science and Technology (DST), New Delhi (F. No. DST/NM/NS/2021/405) under the nanomission scheme.

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Author notes

  1. Vishnumaya S. Nair and Vaibhavi Srivastava contributed equally to this work.

Authors and Affiliations

  1. Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, Ministry of Chemical and Family Welfare, National Institute of Pharmaceutical Education and Research (NIPER), Telangana, 500 037, Hyderabad, India

    Vishnumaya S. Nair, Vaibhavi Srivastava, Valamla Bhavana, Rati Yadav, Naveen Rajana & Neelesh Kumar Mehra

  2. Department of Biological Science, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, Telangana, India

    Shashi Bala Singh

  3. Pharmaceutical Nanotechnology Research Laboratory, Department of Pharmaceutics, National Institute of Pharmaceutical Education and Research Hyderabad, Telangana, India

    Neelesh Kumar Mehra

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Contributions

Vishnumaya S. Nair and Vaibhavi Srivastava: investigation, data curation, visualization, and original draft writing.

Vishnumaya S. Nair and Neelesh Kumar Mehra: design and conceptualization.

Valamla Bhawana and Rati Yadav: reviewing, editing, and supervision.

N. K. Mehra and Shashi Bala Singh: supervision.

N. K. Mehra: guidance, acquired funding and approval of the original draft.

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Correspondence to Neelesh Kumar Mehra.

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Nair, V.S., Srivastava, V., Bhavana, V. et al. Exploring Penetration Ability of Carbonic Anhydrase Inhibitor–Loaded Ultradeformable Bilosome for Effective Ocular Application. AAPS PharmSciTech 24, 157 (2023). https://doi.org/10.1208/s12249-023-02617-5

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