Rivastigmine-loaded in situ gelling nanostructured lipid carriers for nose to brain delivery

被引:60
|
作者
Wavikar, Preeti R. [1 ]
Vavia, Pradeep R. [1 ]
机构
[1] Inst Chem Technol, Dept Pharmaceut Sci & Technol, Ctr Novel Drug Delivery Syst, Bombay 400019, Maharashtra, India
关键词
Acetylcholine esterase enzyme inhibition; in situ gel; rheology; rivastigmine; texture analysis; ALZHEIMERS-DISEASE; GEL; NANOPARTICLES; VITRO; ACETYLCHOLINESTERASE; BEHAVIOR;
D O I
10.3109/08982104.2014.954129
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
In the current research work, rivastigmine (RV)-loaded in situ gelling nanostructured lipid carriers (NLCs) were developed for nose to brain delivery. NLCs were fabricated by ethanol injection method using glyceryl monosterate, Capmul MCM C8, Lecithin and Tween 80. NLCs showed average particle size of 123.2 +/- 2.3 nm with entrapment efficiency of 68.34 +/- 3.4%. DSC, XRD and IR studies showed complete amorphization and incorporation of the drug into nanoparticles. NLCs were incorporated into an in situ gelling system using 0.8% gellan gum and 15% Lutrol F 127. RV in situ gel showed excellent elasticity, rheology, mucoadhesion and adhesiveness to facilitate its adhesion to the upper nasal mucosa. NLC-based in situ gel showed a 2-fold increase in nasal permeation of the drug over plain RV solution. In situ gelling NLCs showed a 3-fold increase in enzyme inhibition efficacy.
引用
收藏
页码:141 / 149
页数:9
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