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In vitro and In vivo Studies on a Novel Bioadhesive Colloidal System: Cationic Liposomes of Ibuprofen

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Abstract

The objective of this study was to develop an ocular drug delivery system built on the cationic liposomes, a novel bioadhesive colloidal system, which could enhance the precorneal residence time, ocular permeation, and bioavailability of ibuprofen. The optimal formulation of cationic liposomes prepared by ethanol injection method was ultimately confirmed by an orthogonal L9 (33) test design. In addition, γ-scintigraphic technology and the microdialysis technique were utilized in the assessment of in vivo precorneal retention capability and ocular bioavailability individually. In the end, we acquired the optimal formulation of ibuprofen cationic liposomes (Ibu-CL) by orthogonal test design, and the particle size and entrapment efficiency (EE%) were 121.0 ± 3.5 nm and 72.9 ± 3.4%, respectively. In comparison to ibuprofen eye drops (Ibu-ED), Ibu-CL could significantly prolong the T max to 100 min and the AUC to 1.53-folds, which indicated that the Ibu-CL could improve the precorneal retention time and bioavailability of ibuprofen. Consequently, these outcomes designated that the ibuprofen cationic liposomes we researched probably are a promising application in ocular drug delivery system.

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Acknowledgments

This study was supported by the program of supporting career development of young and middle-aged teachers from Shenyang Pharmaceutical University (ZQN2015011).

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China

    Xiumei Gai, Lizhen Cheng, Ting Li, Weisan Pan & Xinggang Yang

  2. Department of Pharmaceutical Engineering, School of Biomedical and Chemical Engineering, Liaoning Institute of Science and Technology, 176 Xianghuai Road, Benxi, 117004, China

    Dandan Liu

  3. Lianyungang TCM Branch of Jiangsu Union Technical Institute, Lianyungang, Jiangsu, 222006, China

    Yanyan Wang

  4. Jiangsu Kanion Pharmaceutical Co., Ltd, Lianyungang, Jiangsu, 222001, China

    Tuanjie Wang

  5. State Key Laboratory of New-tech for Chinese Medicine Pharmaceutical Process, Lianyungang, Jiangsu, 222001, China

    Tuanjie Wang

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  1. Xiumei Gai
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  2. Lizhen Cheng
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Correspondence to Xinggang Yang.

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Gai, X., Cheng, L., Li, T. et al. In vitro and In vivo Studies on a Novel Bioadhesive Colloidal System: Cationic Liposomes of Ibuprofen. AAPS PharmSciTech 19, 700–709 (2018). https://doi.org/10.1208/s12249-017-0872-4

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