Formulation and optimisation of novel transfersomes for sustained release of local anaesthetic

Bnyan, Ruba, Khan, Iftikhar, Ehtezazi, Touraj, Saleem, Imran, Gordon, Sarah, O’Neill, Francis and Roberts, Matthew ORCID: 0000-0002-7257-9379
(2019) Formulation and optimisation of novel transfersomes for sustained release of local anaesthetic. Journal of Pharmacy and Pharmacology, 71 (10). 1508 - 1519.

[img] Text
Final Accepted Manuscript 250719.pdf - Accepted Version

Download (1MB) | Preview


<jats:title>Abstract</jats:title> <jats:sec> <jats:title>Objective</jats:title> <jats:p>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.</jats:p> </jats:sec> <jats:sec> <jats:title>Method</jats:title> <jats:p>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.</jats:p> </jats:sec> <jats:sec> <jats:title>Key findings</jats:title> <jats:p>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.</jats:p> </jats:sec> <jats:sec> <jats:title>Conclusion</jats:title> <jats:p>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.</jats:p> </jats:sec>

Item Type: Article
Depositing User: Symplectic Admin
Date Deposited: 23 Jan 2020 09:56
Last Modified: 10 Feb 2021 03:10
DOI: 10.1111/jphp.13149