Abstract
Purpose: Local anaesthesia in eyelid surgery carries inherent risks, which has spurned ongoing investigation to identify needleless alternatives. Nanomedicines (particles ranging between 10nm and 1000nm in size) have shown promise in the transcutaneous delivery of certain drugs. In this study, we explore the feasibility of nano-enabled lidocaine delivery across an artificial skin analogue.
Materials and Methods: Three different lidocaine-loaded nanocarriers were characterised. Diffusion studies were performed through cellulose membranes using customised Franz cells. The nanocarriers included polymeric micelles (PM) (Soluplus), solid lipid nanoparticles (SLN) [Tripalmitin: Lecithin: Labrasol: polysorbate-20: water; 3.33:1:40:1:4.67 w/w] and Self-nanoemulsifying drug delivery systems (SNEDDS) [Capryol-90: Transcutol: Labrasol; 1:3:6 w/w]. Particles were characterised in terms of size, zeta-potential and morphology. One-way analysis of variance (ANOVA) with post hoc Tukey tests were used to assess differences in permeation at a significance of p<0.05.
Results: Lidocaine loading was highest in SNEDDs (50 ± 2.1 mg g-1) compared with PMs (13.4 ± 0.6 mg ml-1) and SLNs (2.8±0.5 mg ml-1). All particles possessed a size below 150nm, illustrated good colloidal stability with a negative zeta-potential and a spherical morphology as demonstrated by transmission electron miscroscopy images. Cumulative lidocaine concentration after 6 hours was significant for both PMs (345.7+/-23.8 µg/cm2/h) and SNEDDS (224.8+/-118.2 µg/cm2/h) compared to SLNs (127.3+/-25.4 µg/cm2/h). However, SLNs provided controlled release of lidocaine with a linear gradient that continued to increase up to 6 hours.
Discussion: These results highlight the potential capability of nanoparticle lidocaine delivery in eyelid surgery. The achieved flux for all nanomedicines was higher than that reported for currently approved topical lidocaine formulations (including EMLA cream).
Materials and Methods: Three different lidocaine-loaded nanocarriers were characterised. Diffusion studies were performed through cellulose membranes using customised Franz cells. The nanocarriers included polymeric micelles (PM) (Soluplus), solid lipid nanoparticles (SLN) [Tripalmitin: Lecithin: Labrasol: polysorbate-20: water; 3.33:1:40:1:4.67 w/w] and Self-nanoemulsifying drug delivery systems (SNEDDS) [Capryol-90: Transcutol: Labrasol; 1:3:6 w/w]. Particles were characterised in terms of size, zeta-potential and morphology. One-way analysis of variance (ANOVA) with post hoc Tukey tests were used to assess differences in permeation at a significance of p<0.05.
Results: Lidocaine loading was highest in SNEDDs (50 ± 2.1 mg g-1) compared with PMs (13.4 ± 0.6 mg ml-1) and SLNs (2.8±0.5 mg ml-1). All particles possessed a size below 150nm, illustrated good colloidal stability with a negative zeta-potential and a spherical morphology as demonstrated by transmission electron miscroscopy images. Cumulative lidocaine concentration after 6 hours was significant for both PMs (345.7+/-23.8 µg/cm2/h) and SNEDDS (224.8+/-118.2 µg/cm2/h) compared to SLNs (127.3+/-25.4 µg/cm2/h). However, SLNs provided controlled release of lidocaine with a linear gradient that continued to increase up to 6 hours.
Discussion: These results highlight the potential capability of nanoparticle lidocaine delivery in eyelid surgery. The achieved flux for all nanomedicines was higher than that reported for currently approved topical lidocaine formulations (including EMLA cream).
| Original language | English |
|---|---|
| Pages (from-to) | 871-876 |
| Journal | British Journal of Ophthalmology |
| Volume | 100 |
| Issue number | 6 |
| Early online date | 16 Mar 2016 |
| DOIs | |
| Publication status | Published - Jun 2016 |
Keywords
- cellulose membranes
- Franz diffusion cells
- nanoparticles
- lidocaine
- eyelid surgery