亲爱的研友该休息了!由于当前在线用户较少,发布求助请尽量完整的填写文献信息,科研通机器人24小时在线,伴您度过漫漫科研夜!身体可是革命的本钱,早点休息,好梦!

In situ gel-forming oil as rectally delivering platform of hydrophobic therapeutics for ulcerative colitis therapy

溃疡性结肠炎 体内 泊洛沙姆 化学 药物输送 色谱法 医学 病理 疾病 有机化学 共聚物 生物 生物技术 聚合物
作者
Ying‐Zheng Zhao,Jiawei Xu,Jianxun Shangguan,Hanxiao Pan,Kaili Lu,Sunkuan Hu,He‐Lin Xu
出处
期刊:International Journal of Pharmaceutics [Elsevier]
卷期号:642: 123149-123149 被引量:3
标识
DOI:10.1016/j.ijpharm.2023.123149
摘要

Because of their poor water-soluble properties and non-specific distribution, most hydrophobic therapeutics had limited benefit for patients with ulcerative colitis. Herein, an in-situ oil-based gel has been developed as a rectal delivery vehicle for these therapeutics. In situ gel-forming oil (BBLG) was composed of soybean phosphatidyl choline (40%, w/w), glyceryl dioleate (50%, w/w), and ethanol (10%, w/w). The hydrophobic laquinimod (LAQ) as a model drug was easily dissolved in gel-forming oil and its solubility was reaching to 7 ± 0.1 mg/mL. Importantly, upon contact with the colonic fluids, the gel-forming oil was quickly transited to a semi-solid gel, adhering to the inflamed colon mucosa and forming a protective barrier. Transmission Electron Microscopy showed that the gel network was arranged by the connected lipid spheres and LAQ was non-crystally encapsulated into the lipid spheres. Moreover, the universal adhesive test showed that the adhesive force and the adhesive energy of BBLG toward fresh colon tissues were 711 ± 12 mN and 25 ± 2 J/m2, which was 2.14-fold and 5-fold higher than that of the marketed Poloxamer 407 gel, respectively. Meanwhile, in vivo imaging confirmed that the retention time of BBLG in the colon lumen was more than 8 h after rectal administration. In vivo animal studies showed that BBLG also greatly enhanced the therapeutic impact of LAQ on TNBS-treated rats with ulcerative colitis, as evidenced by reduced disease activity index (DAI) scores and weight loss. Moreover, the colonic inflammation was significantly alleviated and the goblet cells were obliviously restored after treatment. Importantly, the gut mucosa barrier was largely repaired without any formation of fibrosis remodeling. Conclusively, in situ liquid gel may be a potential delivery system of hydrophobic medicines for ulcerative colitis.
最长约 10秒,即可获得该文献文件

科研通智能强力驱动
Strongly Powered by AbleSci AI
更新
大幅提高文件上传限制,最高150M (2024-4-1)

科研通是完全免费的文献互助平台,具备全网最快的应助速度,最高的求助完成率。 对每一个文献求助,科研通都将尽心尽力,给求助人一个满意的交代。
实时播报
27秒前
45秒前
实力不允许完成签到 ,获得积分10
57秒前
完美耦合完成签到,获得积分10
1分钟前
1437594843完成签到 ,获得积分10
1分钟前
Owen应助zz采纳,获得10
6分钟前
小二郎应助科研通管家采纳,获得30
6分钟前
LIVE完成签到,获得积分10
6分钟前
8分钟前
8分钟前
lizhang发布了新的文献求助10
8分钟前
hilygogo完成签到,获得积分10
8分钟前
露露完成签到,获得积分10
11分钟前
houha233发布了新的文献求助10
11分钟前
12分钟前
宁异勿同完成签到,获得积分10
12分钟前
12分钟前
科研通AI2S应助踏实的芸遥采纳,获得30
12分钟前
13分钟前
13分钟前
poki完成签到 ,获得积分10
13分钟前
zz发布了新的文献求助10
13分钟前
13分钟前
13分钟前
houha233完成签到,获得积分10
13分钟前
14分钟前
xuhanghang发布了新的文献求助10
15分钟前
空曲完成签到 ,获得积分10
17分钟前
17分钟前
大模型应助zz采纳,获得10
18分钟前
木森ab发布了新的文献求助10
18分钟前
JamesPei应助木森ab采纳,获得10
18分钟前
木森ab完成签到,获得积分20
18分钟前
朱朱完成签到,获得积分10
18分钟前
大个应助朱朱采纳,获得10
18分钟前
April完成签到 ,获得积分10
19分钟前
古炮完成签到 ,获得积分10
22分钟前
香蕉觅云应助Zephyr采纳,获得30
22分钟前
23分钟前
hhhhhhhhhh完成签到 ,获得积分10
24分钟前
高分求助中
The Oxford Handbook of Social Cognition (Second Edition, 2024) 1050
Kinetics of the Esterification Between 2-[(4-hydroxybutoxy)carbonyl] Benzoic Acid with 1,4-Butanediol: Tetrabutyl Orthotitanate as Catalyst 1000
The Young builders of New china : the visit of the delegation of the WFDY to the Chinese People's Republic 1000
Rechtsphilosophie 1000
юрские динозавры восточного забайкалья 800
English Wealden Fossils 700
Handbook of Qualitative Cross-Cultural Research Methods 600
热门求助领域 (近24小时)
化学 医学 生物 材料科学 工程类 有机化学 生物化学 物理 内科学 纳米技术 计算机科学 化学工程 复合材料 基因 遗传学 催化作用 物理化学 免疫学 量子力学 细胞生物学
热门帖子
关注 科研通微信公众号,转发送积分 3139600
求助须知:如何正确求助?哪些是违规求助? 2790479
关于积分的说明 7795340
捐赠科研通 2446926
什么是DOI,文献DOI怎么找? 1301511
科研通“疑难数据库(出版商)”最低求助积分说明 626259
版权声明 601176