Bnyan, Ruba, Khan, Iftikhar, Ehtezazi, Touraj, Saleem, Imran, Gordon, Sarah, O’Neill, Francis and Roberts, Matthew (2019) Formulation and optimisation of novel transfersomes for sustained release of local anaesthetic. Journal of Pharmacy and Pharmacology, 71(10), pp. 1508-1519. ISSN (print) 0022-3573
Abstract
This study aims to investigate the effect of formulation parameters on the preparation of transfersomes as sustained-release delivery systems for lidocaine and to develop and validate a new high-performance liquid chromatography (HPLC) method for analysis. Taguchi design of experiment (DOE) was used to optimise lidocaine-loaded transfersomes in terms of phospholipid, edge activator (EA) and phospholipid : EA ratio. Transfersomes were characterised for size, polydispersity index (PDI), charge and entrapment efficiency (%EE). A HPLC method for lidocaine quantification was optimised and validated using a mobile phase of 30%v/v PBS (0.01 m) : 70%v/v Acetonitrile at a flow rate of 1 ml/min, detected at 255 nm with retention time of 2.84 min. The release of lidocaine from selected samples was assessed in vitro. Transfersomes were 200 nm in size, with PDI ~ 0.3. HPLC method was valid for linearity (0.1–2 mg/ml, R2 0.9999), accuracy, intermediate precision and repeatability according to ICH guidelines. The %EE was between 44% and 56% and dependent on the formulation parameters. Taguchi DOE showed the effect of factors was in the rank order : lipid : EA ratio ˃ EA type ˃ lipid type. Optimised transfersomes sustained the release of lidocaine over 24 h. Sustained-release, lidocaine-loaded transfersomes were successfully formulated and optimised using a DOE approach, and a new HPLC method for lidocaine analysis was developed and validated.
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