Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritancy and high bioavailability
文献类型：期刊论文
| 作者 | Han, Shun2; Shen, Jin-qiu3; Gan, Yong2 ; Geng, Hai-ming1; Zhang, Xin-xin2; Zhu, Chun-liu2; Gan, Li2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2010-08 |
| 卷号 | 31期号:8页码:990-998 |
| 关键词 | flurbiprofen cubosomes ocular drug delivery systems corneal permeability ocular irritation |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2010.98 |
| 文献子类 | Article |
| 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. Cubosomes 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 P(app) 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.mu g(-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. |
| WOS关键词 | LIPID-WATER PHASES ; OCULAR TOLERANCE ; ESTER PRODRUGS ; IN-VITRO ; SYSTEMS ; DISPERSIONS ; NANOPARTICLES ; PENETRATION ; TRANSPORT ; RELEASE |
| 资助项目 | National Science & Technology Major Project[2009ZX09301-001] ; National Basic Research Program of China[2009CB930300] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000280617100014 |
| 出版者 | SHANGHAI INST MATERIA MEDICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278805]  |
| 专题 | 药物制剂研究中心 |
| 通讯作者 | Gan, Li |
| 作者单位 | 1.Wuhan Wuyao Sci & Technol Co Ltd, Wuhan 430033, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.China Pharmaceut Univ, Sch Pharm, Nanjing 210009, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Han, Shun,Shen, Jin-qiu,Gan, Yong,et al. Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritancy and high bioavailability[J]. ACTA PHARMACOLOGICA SINICA,2010,31(8):990-998. |
| APA | Han, Shun.,Shen, Jin-qiu.,Gan, Yong.,Geng, Hai-ming.,Zhang, Xin-xin.,...&Gan, Li.(2010).Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritancy and high bioavailability.ACTA PHARMACOLOGICA SINICA,31(8),990-998. |
| MLA | Han, Shun,et al."Novel vehicle based on cubosomes for ophthalmic delivery of flurbiprofen with low irritancy and high bioavailability".ACTA PHARMACOLOGICA SINICA 31.8(2010):990-998. |
入库方式： OAI收割
来源：上海药物研究所
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