In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions

被引:53
|
作者
Gonzalez-Pizarro, Roberto [1 ]
Carvajal-Vidal, Paulina [1 ]
Halbault Bellowa, Lyda [1 ]
Cristina Calpena, Ana [1 ,2 ]
Espina, Marta [1 ,2 ]
Luisa Garcia, Maria [1 ,2 ]
机构
[1] Univ Barcelona, Dept Pharm Pharmaceut Technol & Phys Chem, Fac Pharm & Food Sci, E-08028 Barcelona, Spain
[2] Univ Barcelona, Inst Nanosci & Nanotechnol IN2UB, Barcelona, Spain
关键词
Fluorometholone; PLGA nanoparticles; Ocular anti-inflammatory; Poloxamer; 407; Thermosensitive; In-situ gelling; Gel; DRUG-DELIVERY; PLGA NANOPARTICLES; EX-VIVO; NANOSPHERES; DESIGN; CORTICOSTEROIDS; FORMULATIONS; TOXICITY; CARRIERS; SYSTEM;
D O I
10.1016/j.colsurfb.2018.11.065
中图分类号
Q6 [生物物理学];
学科分类号
071011 ;
摘要
Thermosensitive gels have been developed and optimized in such a way that they become gels at corneal temperature and with a viscosity that allows the adequate release of the Fluorometholone (FMT)-loaded PLGA nanoparticles (NPs) in order to improve ocular anti-inflammatory efficacy against a commercial formulation. It has been shown that gels avoid burst release of the drug in the first hours with a slow and increasing profile after administration. NPs have maintained their average size and spherical shape within the gels as confirmed by transmission electron microscopy (TEM). In turn, the in-situ gelling of the formulations allows the administration in eye drops dosage form due to its state of sol at temperatures below 25 degrees C. Ocular tolerance studies have shown that no formulation causes eye irritation. The administration of the developed formulations has improved the precomeal residence time reflected in the ocular bioavailability, where deep tissues as aqueous humour and crystalline were reached. In conclusion, the use of thermosensitive gels for the topical application of NPs has demonstrated their effectiveness in the acute and preventive treatment of ocular inflammatory conditions.
引用
收藏
页码:365 / 374
页数:10
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