Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritanc and high bioavailability
文献类型：期刊论文
| 作者 | Han Shun3; Shen Jinqiu2; Gan Yong3 ; Geng Haiming1; Zhang Xinxin3; Zhu Chunliu3; Gan Li3
|
| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2010 |
| 卷号 | 31期号:8页码:990 |
| 关键词 | flurbiprofen cubosomes ocular drug delivery systems corneal permeability ocular irritation |
| ISSN号 | 1671-4083 |
| 英文摘要 | Aim: To develop a novel vehicle based on cubosomes as an ophthalmic drug delivery system for flurbiprofen (FB) to reduce ocular irritancy and improve bioavailability. Methods: FB-loaded cubosomes were prepared using hot and high-pressure homogenization. Cubos Omes were then characterized by particle size, zeta potential, encapsulation efficiency, particle morphology, inner cubic structure and in vitro release. Corneal permeation was evaluated using modified Franz-type cells. Ocular irritation was then evaluated using both the Draize method and histological examination. The ocular pharmacokinetics of FB was determined using microdialysis. Results: The particle size of each cubosome formulation was about 150 nm. A bicontinuous cubic phase of cubic P-type was determined using cryo-transmission electron microscopy (cryo-TEM) observation and small angle X-ray scattering (SAXS) analysis. In vitro corneal permeation study revealed that FB formulated in cubosomes exhibited 2.5-fold (F1) and 2.0-fold (F2) increase in Papp compared with FB PBS. In the ocular irritation test, irritation scores for each group were less than 2, indicating that all formulations exhibited excellent ocular tolerance. Histological examination revealed that neither the structure nor the integrity of the cornea was visibly affected after incubation with FB cubosomes. The AUC of FB administered as FB cubosome F2 was 486.36±38.93 ng·mL~(-1)·min·pg~(-1), which was significantly higher than that of FB Na eye drops (P<0.01). Compared with FB Na eye drops, the T_(max) of FB cubosome F2 was about 1.6-fold higher and the MRT was also significantly longer (P<0.001). Conclusion: This novel low-irritant vehicle based on cubosomes might be a promising system for effective ocular drug delivery |
| 语种 | 英语 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/304901]  |
| 专题 | 中国科学院上海药物研究所 |
| 作者单位 | 1.Wuhan Wuyao Science & Technology Co Ltd 2.School of Pharmacy, China Pharma-ceutical University 3.中国科学院上海药物研究所 |
| 推荐引用方式 GB/T 7714 | Han Shun,Shen Jinqiu,Gan Yong,et al. Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritanc and high bioavailability[J]. ACTA PHARMACOLOGICA SINICA,2010,31(8):990. |
| APA | Han Shun.,Shen Jinqiu.,Gan Yong.,Geng Haiming.,Zhang Xinxin.,...&Gan Li.(2010).Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritanc and high bioavailability.ACTA PHARMACOLOGICA SINICA,31(8),990. |
| MLA | Han Shun,et al."Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritanc and high bioavailability".ACTA PHARMACOLOGICA SINICA 31.8(2010):990. |
入库方式： OAI收割
来源：上海药物研究所
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