Nanostructured lipid carriers for intraocular brimonidine localisation: development, in-vitro and in-vivo evaluation

被引：32
作者：
El-Salamouni, Noha S. [1 ]
Farid, Ragwa M. [1 ,2 ]
El-Kamel, Amal H. [2 ]
El-Gamal, Safaa S. [2 ]
机构：
[1] Pharos Univ Alexandria, Dept Pharmaceut, Fac Pharm & Drug Mfg, Alexandria, Egypt
[2] Alexandria Univ, Dept Pharmaceut, Fac Pharm, Alexandria, Egypt
来源：
JOURNAL OF MICROENCAPSULATION | 2018年 / 35卷 / 01期
关键词：
Glaucoma; nanostructured lipid carriers; solid lipid nanoparticles; ocular targeting; ocular histology; brimonidine; OCULAR DRUG-DELIVERY; NANOPARTICLES SLN; CAPRA-HIRCUS; PART II; DESIGN; EYE; MATRICES; RELEASE; SYSTEM; GATIFLOXACIN;
D O I：
10.1080/02652048.2018.1425753
中图分类号：
O69 [应用化学];
学科分类号：
081704 ;
摘要：
Brimonidine ocular hypotensive effect can be enhanced by increasing residence time and corneal penetration. The current work aimed to formulate, evaluate and compare nanostructured lipid carriers (NLCs) to solid lipid nanoparticles (SLNs) and commercial eye drops for controlled brimonidine delivery. NLCs prepared by modified high shear homogenisation were spherical with a mean size of 151.97 +/- 1.98nm, negative zeta potential (ZP) of -44.2 +/- 7.81mV, % entrapment efficiency (EE) of 83.631 +/- 0.495% and low crystallinity index (CI) (17.12%), indicating a better drug incorporation. Moreover, they kept stable during storage at 4 degrees C for 3months. Permeability coefficient of NLCs was 1.227 folds higher than that of SLNs. Histological examination revealed localisation of NLCs in the anterior ocular chamber. NLCs revealed the most sustained and highest intraocular pressure (IOP) lowering activity (-13.14 +/- 1.28mmHg) in rabbits. In conclusion, NLCs is a promising approach for IOP reduction compared to eye drops and SLNs.
引用
收藏
页码：102 / 113
页数：12
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