Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment
The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, sma...
| Main Authors: | , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2019-01-01
|
| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2019.1667451 |
| _version_ | 1819081408631537664 |
|---|---|
| author | Wang Xingqi Zhang Yong Li Xing Wang Yang Huang Jie Hu Rongfeng Gui Shuangying Chu Xiaoqin |
| author_facet | Wang Xingqi Zhang Yong Li Xing Wang Yang Huang Jie Hu Rongfeng Gui Shuangying Chu Xiaoqin |
| author_sort | Wang Xingqi |
| collection | DOAJ |
| description | The objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q2 and H2 phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q2 and H2 gel produces a 5.25-fold and 6.23-fold increase in the Papp value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma. |
| first_indexed | 2024-12-21T20:00:18Z |
| format | Article |
| id | doaj.art-7f7ca486819546acbcea6d708e69ef0f |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-21T20:00:18Z |
| publishDate | 2019-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-7f7ca486819546acbcea6d708e69ef0f2022-12-21T18:52:00ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642019-01-0126195296410.1080/10717544.2019.16674511667451Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatmentWang Xingqi0Zhang Yong1Li Xing2Wang Yang3Huang Jie4Hu Rongfeng5Gui Shuangying6Chu Xiaoqin7Anhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineAnhui University of Chinese MedicineThe objective of this work was to investigate phytantriol-based liquid crystal (LC) gels including cubic (Q2) and hexagonal (H2) phase for ocular delivery of pilocarpine nitrate (PN) to treat glaucoma. The gels were produced by a vortex method and confirmed by crossed polarized light microscopy, small-angle X-ray scattering, and rheological measurements. Moreover, the release behaviors and permeation results of PN from the gels were estimated using in vitro studies. Finally, the anti-glaucoma effect of LC gels was evaluated by in vivo animal experiments. The inner structure of the gels was Pn3m-type Q2 and H2 phase, and both of them showed pseudoplastic fluid properties based on characterization techniques. In vitro release profiles suggested that PN could be sustainably released from LC gels within 48 h. Compared with eye drops, Q2 and H2 gel produces a 5.25-fold and 6.23-fold increase in the Papp value (p < .05), respectively, leading to a significant enhancement of corneal penetration. Furthermore, a good biocompatibility and longer residence time on precorneal for LC gels confirmed by in vivo animal experiment. Pharmacokinetic studies showed that LC gels could maintain PN concentration in aqueous humor for at least 12 h after administration and remarkably improve the bioavailability of drug. Additionally, in vivo pharmacodynamics studies indicated that LC gels had a more significant intraocular pressure-lowering and miotic effect compared to eye drops. These research findings hinted that LC gels would be a promising pharmaceutical strategy for ocular application to enhance the efficacy of anti-glaucoma.http://dx.doi.org/10.1080/10717544.2019.1667451phytantriolliquid crystal gelsocular deliveryiop-loweringanti-glaucoma |
| spellingShingle | Wang Xingqi Zhang Yong Li Xing Wang Yang Huang Jie Hu Rongfeng Gui Shuangying Chu Xiaoqin Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment Drug Delivery phytantriol liquid crystal gels ocular delivery iop-lowering anti-glaucoma |
| title | Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment |
| title_full | Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment |
| title_fullStr | Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment |
| title_full_unstemmed | Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment |
| title_short | Cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti-glaucoma treatment |
| title_sort | cubic and hexagonal liquid crystal gels for ocular delivery with enhanced effect of pilocarpine nitrate on anti glaucoma treatment |
| topic | phytantriol liquid crystal gels ocular delivery iop-lowering anti-glaucoma |
| url | http://dx.doi.org/10.1080/10717544.2019.1667451 |
| work_keys_str_mv | AT wangxingqi cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT zhangyong cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT lixing cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT wangyang cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT huangjie cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT hurongfeng cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT guishuangying cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment AT chuxiaoqin cubicandhexagonalliquidcrystalgelsforoculardeliverywithenhancedeffectofpilocarpinenitrateonantiglaucomatreatment |