title: Analytical and physicochemical characterisation of the senile cataract drug dipeptide β-alanyl-L-histidine (carnosine).
abstract: 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.
authors.affiliation: Drug Discovery, Delivery and Patient (DDDPC) Theme, School of Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, London, UK; Department of Pharmaceutics, Faculty of Pharmacy, Minia University, Mina, Egypt. Electronic address: h.abdelkader@kingston.ac.uk.
authors.forename: Hamdy
authors.initials: H
authors.lastname: Abdelkader
authors.affiliation: Drug Discovery, Delivery and Patient (DDDPC) Theme, School of Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, London, UK.
authors.forename: Julian
authors.initials: J
authors.lastname: Swinden
authors.affiliation: Vision Cognition and Neuroscience Theme, Faculty of Science, Engineering and Computing, Kingston University London, Kingston upon Thames, London, UK.
authors.forename: Barbara K
authors.initials: BK
authors.lastname: Pierscionek
authors.affiliation: Drug Discovery, Delivery and Patient (DDDPC) Theme, School of Pharmacy and Chemistry, Kingston University London, Kingston upon Thames, London, UK; School of Pharmacy, The University of Auckland, Auckland, New Zealand.
authors.forename: Raid G
authors.initials: RG
authors.lastname: Alany
mesh_terms: D000097:Acetonitriles / Q000737:chemistry; D002336:Carnosine / Q000032:analysis* / Q000737:chemistry; D002386:Cataract / Q000188:drug therapy*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007908:Lens, Crystalline / Q000187:drug effects; D016014:Linear Models; D000442:Octanols / Q000737:chemistry; D010100:Oxygen / Q000737:chemistry; D010743:Phospholipids / Q000737:chemistry; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization; D013696:Temperature
chemical_list: D000097:Acetonitriles; D000442:Octanols; D010743:Phospholipids; D002336:Carnosine; D010100:Oxygen; C032159:acetonitrile
keywords: Dipeptide; Histidine; L-carnosine; Ocular delivery; Senile cataract