Enhancement of the Mechanical and Drug-Releasing Properties of Poloxamer 407 Hydrogels with Casein.
Enhancement of the Mechanical and Drug-Releasing Properties of Poloxamer 407 Hydrogels with Casein.
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酪蛋白对泊洛沙姆407水凝胶力学性能和药物释放性能的增强作用
DOI：
10.1007/s11095-021-03017-9
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发表时间：
2021-03
影响因子：
3.7
通讯作者：
Kohane DS
中科院分区：
文献类型：
--
作者：
Tundisi LL;Yang R;Borelli LPP;Alves T;Mehta M;Chaud MV;Mazzola PG;Kohane DS
局部疾病（例如皮肤疾病）的局部治疗相较于口服治疗具有优势，因为其全身药物分布更少（副作用也更少），无首过效应等。然而，患者对局部治疗的依从性可能较差，因为可能一天需要多次用药，且持续数月。在此我们提出一种局部控释制剂，它在体温下具有热响应凝胶特性且黏附性增强，使其更容易与身体保持接触。
该制剂包含两种辅料，泊洛沙姆407（P407）和酪蛋白。酪蛋白可通过分子缠结改变水凝胶的性质。此外，还对组织反应和药物释放曲线进行了评估。
酪蛋白浓度的变化影响黏附强度、黏度、机械性能和药物释放，这可能是由于酪蛋白和P407之间的疏水相互作用。对两种不同浓度的P407与两种不同浓度的酪蛋白进行了测试。含有5%和10%酪蛋白的制剂在48小时内释放80%的模型药物，而不含酪蛋白的制剂在约24小时内释放相同比例的药物。含10%酪蛋白的制剂的黏附强度几乎是不含酪蛋白的制剂的两倍。
添加酪蛋白改变了水凝胶的机械性能和药物释放速率。在体内短暂暴露后没有出现炎症或损伤。
Topical therapy of local disease (e.g. skin) is advantageous over oral therapy since there is less systemic drug distribution (so fewer side-effects), no first-pass effect, etc. However, patient compliance with topical therapy can be poor as it may require many applications a day and can last months. Here we propose a topical controlled release formulation with thermoresponsive gelation at body temperature and improved adhesiveness, making it easier to remain in contact with the body. The formulation contains two excipients, poloxamer 407 (P407) and casein. Casein can modify the properties of the hydrogel through molecular entanglement. In addition, tissue reaction and drug release profile were evaluated. Changes in casein concentration affected adhesive strength, viscosity, mechanical properties and drug release, presumably by hydrophobic interactions between casein and P407. Two different concentrations of P407 were tested with two different concentrations of casein. Formulations containing 5% and 10% casein released 80% of model drug in 48h, while formulations without casein released the same fraction in around 24h hours. Formulations with 10% casein had almost twice the adhesive strength of those without casein. Addition of casein modified the mechanical properties and drug release rate of the hydrogel. There was no inflammation or injury after brief exposure in vivo.
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影响因子：
3.9
作者：
Hambardzumyan, A;Aguié-Béghin, V;Douillard, R
通讯作者：
Douillard, R
影响因子：
5.8
作者：
Kessler, Anne;Menendez-Aguirre, Orquidea;Weiss, Jochen
通讯作者：
Weiss, Jochen
影响因子：
6.1
作者：
Portnaya, Irina;Ben-Shoshan, Einav;Danino, Dganit
通讯作者：
Danino, Dganit
影响因子：
3.3
作者：
Oshiro Junior, Joao Augusto;Carvalho, Flavia Chiva;Chiavacci, Leila Aparecida
通讯作者：
Chiavacci, Leila Aparecida
DOI：
10.1002/jbm.820060609
发表时间：
1972-01-01
期刊：
JOURNAL OF BIOMEDICAL MATERIALS RESEARCH
影响因子：
--
作者：
SCHMOLKA, IR
通讯作者：
SCHMOLKA, IR