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In Situ Liquid Crystal Gel as a Promising Strategy for Improving Ocular Administration of Dexamethasone: Preparation, Characterization, and Evaluation

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Abstract

The purpose of this study was to design an in situ liquid crystal gel (ISLG) as an ophthalmic drug delivery system for dexamethasone (DEX) to enhance its eye retention and ocular bioavailability. The in situ liquid crystal gels (ISLGs) were prepared using a phytantriol/PEG400/water (65:30:5, w/w) ternary system. Polarized light microscope (PLM), small-angle X-ray scattering (SAXS), and rheology analysis confirmed that the internal structure of the preparations was Pn3m cubic phase liquid crystal gels with pseudoplastic fluid properties. Meanwhile, in vitro release behavior of the preparations conforms to the Higuchi equation. Corneal penetration experiments showed that compared with DEX sodium phosphate eye drops, DEX-ISLGs(F2) produced a 5.45-fold increase in the Papp value, indicating a significant enhancement of corneal penetration. In addition, in vivo experiments have confirmed that the ISLGs have better biocompatibility and longer retention time in the cornea. Simultaneously, corneal hydration level, eye irritation experiments, and histological observations proved the safety of the preparations. Pharmacokinetic studies have shown that the ISLG could maintain the DEX concentration in aqueous humor for at least 12 h after administration, which significantly improves the bioavailability of the drug. Collectively, these results indicated that ISLG would be a potential drug carrier for the treatment of diabetic retinopathy (DR).

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Availability of Data and Material

The datasets used or analyzed during the current study are available from the corresponding author on reasonable request.

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Acknowledgements

The content is solely the responsibility of the authors and does not necessarily represent the official views of Anhui University of Chinese Medicine.

Funding

The authors gratefully acknowledge support from the National Natural Science Foundation of China (No.81803831)

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Authors and Affiliations

  1. School of Pharmacy, Anhui University of Chinese Medicine, No. 1, QianJiang Road, Hefei, Anhui, 230012, People’s Republic of China

    Wenqing Wu, Wenxuan Cao, Jingbao Chen, Ye Cai, Baoqi Dong & Xiaoqin Chu

  2. Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei, 230012, China

    Xiaoqin Chu

  3. Anhui Province Key Laboratory of Pharmaceutical Preparation Technology and Application, Hefei, 230012, China

    Xiaoqin Chu

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  1. Wenqing Wu
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  2. Wenxuan Cao
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Contributions

Wenqing Wu: She has a huge contribution to the design and writing of the experiment.

Wenxuan Cao and Jingbao Chen: collected and processed the experimental data.

Ye Cai and Baoqi Dong: final approval of the version to be published.

Xiaoqin Chu: contributed experimental design and writing and a lot of opinions.

Corresponding author

Correspondence to Xiaoqin Chu.

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Animals (certificate: AHUCM-rabbits-2020029) were purchased from Anhui Medical University Center (Hefei, China). All the experimental protocols were approved by the Committee on Ethics of Animal Experiments, Anhui University of Chinese Medicine (Hefei, China), and were conducted in compliance with the Guidelines for Animal Experiments of Anhui University of Chinese Medicine.

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Wu, W., Cao, W., Chen, J. et al. In Situ Liquid Crystal Gel as a Promising Strategy for Improving Ocular Administration of Dexamethasone: Preparation, Characterization, and Evaluation. AAPS PharmSciTech 23, 36 (2022). https://doi.org/10.1208/s12249-021-02193-6

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