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 ORCID: 0000-0002-6009-1026 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 0022-3573, 2042-7158

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Abstract

Objective: 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. Method: 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. Key findings: 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. Conclusion: 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.

Item Type:	Article
Uncontrolled Keywords:	design of experiment, HPLC, local anaesthetic, sustained release, transfersomes
Depositing User:	Symplectic Admin
Date Deposited:	23 Jan 2020 09:56
Last Modified:	16 Jun 2026 04:46
DOI:	10.1111/jphp.13149
Related Websites:	Author Publisher
URI:	https://livrepository.liverpool.ac.uk/id/eprint/3071592
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