Analytical and physicochemical characterisation of the senile cataract drug dipeptide β-alanyl-L-histidine (carnosine)

被引:19
|
作者
Abdelkader, Hamdy [1 ,3 ]
Swinden, Julian [1 ]
Pierscionek, Barbara K. [2 ]
Alany, Raid G. [1 ,4 ]
机构
[1] Univ Kingston, Sch Pharm & Chem, Drug Discovery Delivery & Patient DDDPC Theme, London, England
[2] Univ Kingston, Fac Sci Engn & Comp, Vis Cognit & Neurosci Theme, London, England
[3] Menia Univ, Fac Pharm, Dept Pharmaceut, Mina, Egypt
[4] Univ Auckland, Sch Pharm, Auckland 1, New Zealand
关键词
L-carnosine; Senile cataract; Histidine; Dipeptide; Ocular delivery; DELIVERY;
D O I
10.1016/j.jpba.2015.05.025
中图分类号
O65 [分析化学];
学科分类号
070302 ; 081704 ;
摘要
This study presents a simple but sensitive HPLC chromatographic method with a stability-indicating assay for determination and physicochemical characterisation of L-carnosine, a promising senile cataract prophylactic agent. Chromatographic analysis was conducted using a reverse phase (RP)-HPLC system and an isocratic mobile phase of 98% v/v trifluoroacetic acid (0.1% v/v) and 2% v/v acetonitrile with detection at 220 nm. L-carnosine was subjected to stress conditions to force its degradation using chemical and thermal agents and was subsequently detected from its degradation products using ESI-MS. The lipophilicity of the drug and 1:1 drug to phospholipid complex (PC) mol/mol was determined by estimating the partition coefficient (P). Lipophilicity was greatly enhanced when L-carnosine was formulated as a phospholipid complex using the solvent evaporation method. L-carnosine-phospholipid complex could be a promising approach for effective delivery to the human lens as offers a potential novel treatment for senile cataract. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:241 / 246
页数:6
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