Percutaneous Permeability Of Articaine Hydrochloride-loaded Destran-based Niosomes

ObjectiveTo study the transdermal behaviors and anesthetic effect of ART-HLD-BNs,explore its mechanism of action.Discuss the feasibility as oral topical anesthetic of ART-HLD-BNs.Content and methods1.Permeation characteristics studies of ART-HLD-BNs:Franz diffusion cell and depilated mouse skin were used to study the transdermal efficiency in vivo.The absorbency of the drug was detected and the velocity of drug release was counted by ultraviolet spectrophotometer.2.Anesthetic effect studies of ART-HLD-BNs:Rabbit cornea experiment and toad sciatic nerve experiment were applied to observe the rabbit corneal reflection and nerve action potentials in order to preliminarily explore the anesthetic effect of ART-HLD-BNs.3.Mechanism research of molecular biology of ART-HLD-BNs.By determining the pain related peptide--CGRP,SP,c-fos of gum,trigeminal ganglia and medulla oblongata to explore the mechanism of action of ART-HLD-BNs.Results1.The order of ART penetration flux value at 15min、30min、45min、1h、1.5h、2h、3h、4h、5h、6h、8h、10h、12h was as follows:ART-HLD-BNs>ART-CLs>ART-IJ(P<0.05).The permeation rate of ART-HLD-BNs was 1.37 times and 1.85 times as much as that of ART-CLs、ART-IJ.The calcein encapsulated in ART-HLD-BNs permeated the full thickness and the depth of penetration was 100um,which was deeper than that of ART-CLs which was deeper than that of ART-IJ.2.The time of absence of rabbit reflex was as follows:ART-HLD-BNs<ART-CLs<ART-IJ(P<0.05);the duration of anesthesia was:ART-HLD-BNs>ART-CLs>ART-IJ(P<0.05).The toad sciatic nerve block anesthesia of ART-HLD-BNs was stronger than those of ART-CLs and ART-IJ.3.Compared with formalin model group,SP,c-fos,CGRP protein quantitative determination of 30 min,60 min,90 min group were decreased while different parts the downtrend variesConclussions1.ART-HLD-BNs has strong permeability.The accumulative transdermal absorption quality Q values and skin penetration ratios of ART-HLD-BNs were better than those of ART-CLs and ART-IJ which provide good feasibility of being topical anesthesia.2.ART-HLD-BNs has good anesthesia effect.In rabbit cornea experiment,It shows faster onset and longer sustained time.3.ART-HLD-BNs has stronger inhibitory effect on the toad sciatic nerve.It has the advantages of rapid onset and long restricted time.4.ART-HLD-BNs has theory basis for mechanism,provides a better prospect to the research of oral topical anesthesia drug.