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Design, Characterization, and Application of a pH-Triggered In Situ Gel for Ocular Delivery of Vinpocetine

  • Research Article
  • Theme: Formulation and Delivery of Natural Products
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Abstract

We developed a pH-triggered in situ gel (ISG) for ocular delivery of vinpocetine to achieve systemic absorption and a brain-targeting effect in rats. Carbopol acted as a gelling agent combined with hydroxypropyl methylcellulose (HPMC) as a viscosity-enhancing agent. The concentration of Carbopol (0.2%, w/v) and HPMC (1.5%, w/v) was optimized for the ISG system. The optimized formulation was evaluated for studies on release in vitro, rheology, differential scanning calorimetry, ocular irritation, residence time, and in vivo pharmacokinetics. The vinpocetine ISG stayed longer in rabbit eyes than vinpocetine ointment. In vivo pharmacokinetics showed that compared with vinpocetine ointment, vinpocetine ISG attained a peak plasma concentration and area under the curve that was 1–2 folds greater in rat plasma. The Drug Targeting Index (DTI) was 1.06 and 1.26 for vinpocetine ointment and vinpocetine ISG, respectively, after ocular administration, showing that vinpocetine ISG had better distribution in rat brain. These results revealed that a pH-triggered ISG system via ocular administration could be an alternative approach compared with traditional ophthalmic formulations.

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Funding

This study was funded by the Natural Science Foundation in Higher Education of Anhui Province (KJ2019A0454) and the Anhui Province “Special Support Plan” for the Second Batch of Innovative Leading Talents (The Second Batch).

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Authors and Affiliations

  1. Department of Pharmaceutics, College of Pharmacy, Anhui University of Chinese Medicine, No. 1, QianJiang Road, Hefei, AnHui, People’s Republic of China

    Qun Ma, Rui Luo, Huimin Zhang, Manman Dai, Luyu Bai, Qingsong Fei, Fang Lei & Ning He

  2. Institute of Pharmaceutics, Anhui Academy of Chinese Medical Sciences, Hefei, China

    Ning He

  3. Engineering Technology Research Center of Modernized Pharmaceutics, Hefei, Anhui Province, China

    Ning He

  4. Key Laboratory of Chinese Medicinal Formula, Hefei, Anhui Province, China

    Ning He

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  1. Qun Ma
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Correspondence to Ning He.

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Guest Editors: Harsh Chauhan, Abhijit Date and Sonali Dhindwal

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Ma, Q., Luo, R., Zhang, H. et al. Design, Characterization, and Application of a pH-Triggered In Situ Gel for Ocular Delivery of Vinpocetine. AAPS PharmSciTech 21, 253 (2020). https://doi.org/10.1208/s12249-020-01791-0

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  • DOI: https://doi.org/10.1208/s12249-020-01791-0

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