Liposomal-based lidocaine formulation for the improvement of infiltrative buccal anaesthesia

This study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scatte...

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Bibliographic Details
Published in:Journal of liposome research 2019-01, Vol.29 (1), p.66-72
Main Authors: de Almeida, Ana Cláudia Pedreira, Pinto, Luciana Matos Alves, Alves, Giuliana Piovesan, Ribeiro, Lígia Nunes de Morais, Santana, Maria Helena Andrade, Cereda, Cíntia Maria Saia, Fraceto, Leonardo Fernandes, de Paula, Eneida
Format: Article
Language:English
Subjects:
Administration, Buccal
Anesthetics, Local - administration & dosage
Animals
dentistry
Drug Compounding
Drug Delivery Systems
drug-delivery
hydrogenated soybean phosphatidylcholine
infraorbital nerve blockade
lidocaine
Lidocaine - administration & dosage
Liposomes
Liposomes - chemistry
Male
Rats
Rats, Wistar
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Summary:This study describes the encapsulation of the local anaesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering, nanoparticle tracking analysis and transmission electron microscopy. A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anaesthetic effect of liposomal LDC 2% (LUV LDC ) was compared to LDC 2% solution without (LDC PLAIN ) or with the vasoconstrictor epinephrine (1:100 000) (LDC VASO ), in rat infraorbital nerve blockade model. The structural characterization revealed liposomes with spherical shape, average size distribution of 250 nm and low polydispersity even after LDC incorporation. Zeta potential laid around -30 mV and the number of suspended liposomal particles was in the range of 10 12 vesicles/mL. Also the addition of cryoprotectant (mannitol) did not provoke structural changes in liposomes properties. In vitro release profile of LDC from LUV fits well with a biexponential model, in which the LDC encapsulated (EE% = 24%) was responsible for an increase of 67% in the release time in relation to LDC PLAIN (p 
ISSN:0898-2104
1532-2394
DOI:10.1080/08982104.2018.1483947