title: Nanovesicles system for rapid-onset sublingual delivery containing sodium tanshinone IIA sulfonate: in vitro and in vivo evaluation.
abstract: A novel formulation based on nanovesicles system for rapid-onset sublingual delivery of hydrophilic drug (sodium tanshinone IIA sulfonate, STS) was investigated. The nanovesicles system was composed of 1.5% soybean lecithin, 6% propylene glycol, and penetration enhancers (1% sodium dodecyl sulfate and 0.03% hyaluronan acid). The STS-loaded nanovesicles with an average diameter of 133 ± 9.04 nm and high entrapment efficiency of 85.65 ± 3.89% were characterized. The effects of permeation enhancers on the penetration of STS formulations were investigated using Franz diffusion cells in vitro, showing 86.1-235.8 times higher permeation rate than that of normal STS solution. The rapid symptom relief effect of the nanovesicles system on acute myocardial infarction rabbits was evaluated by in vivo study, ST-segment deviation(S and T wave abnormality in electrocardiogram) was attenuated markedly and rapidly within 5 min, infarct size of heart was significantly reduced and the biochemical indicators were substantially decreased, compared with the control groups (p < 0.05). This study provided a promising tool for the future sublingual delivery of hydrophilic compounds with the noninvasive and rapid onset clinical effect.
authors.affiliation: School of Food and pharmaceutical Engineering, Hubei University of Technology, Wuhan 430068, China. hongda74@yahoo.com.cn
authors.forename: Hongda
authors.initials: H
authors.lastname: Zhu
authors.forename: Jianjun
authors.initials: J
authors.lastname: Hao
authors.forename: Huabing
authors.initials: H
authors.lastname: Chen
authors.forename: Shanshan
authors.initials: S
authors.lastname: Jiang
authors.forename: Mingxing
authors.initials: M
authors.lastname: Liu
authors.forename: Honghao
authors.initials: H
authors.lastname: Sun
authors.forename: Huibi
authors.initials: H
authors.lastname: Xu
authors.forename: Jiemei
authors.initials: J
authors.lastname: Zhang
authors.forename: Xiangliang
authors.initials: X
authors.lastname: Yang
mesh_terms: D000286:Administration, Sublingual; D000818:Animals; D004337:Drug Carriers / Q000737:chemistry*; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D006321:Heart / Q000187:drug effects; D054709:Lecithins / Q000737:chemistry; D008297:Male; D009203:Myocardial Infarction / Q000188:drug therapy* / Q000473:pathology; D009206:Myocardium / Q000473:pathology; D049329:Nanostructures / Q000737:chemistry; D010616:Phenanthrenes / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000627:therapeutic use*; D019946:Propylene Glycol / Q000737:chemistry; D011817:Rabbits; D013025:Glycine max / Q000737:chemistry
chemical_list: D004337:Drug Carriers; D004365:Drugs, Chinese Herbal; D054709:Lecithins; D010616:Phenanthrenes; C024894:tanshinone II A sodium sulfonate; D019946:Propylene Glycol