首页> 外国专利> Synergistically acting amorphous calcium-polyphosphate nanospheres containing encapsulated retinol for therapeutic applications

Synergistically acting amorphous calcium-polyphosphate nanospheres containing encapsulated retinol for therapeutic applications

机译:含有胶囊化视黄醇的协同作用的无定形多磷酸钙钙纳米球,用于治疗应用

摘要

A method for the preparation of degradable amorphous retinoid/calcium-polyphosphate nanospheres comprises: (i) dissolving a retinoid and a calcium salt in an organic solvent; (ii) adding the retinoid calcium salt solution as produced in step (i) to an aqueous solution containing dissolved polyphosphate (polyp) salt and poly(ethylene glycol) or another lubricating coating material, and (iii) collecting washing with water , and drying of the nanospheres as formed. Preferably the retinoid is retinol. Preferably the chain length of the polyphosphate is in the range of about 3 to about 1000 phosphate units. Preferably the amorphous retinoid/calcium-polyphosphate nanospheres are for use in the treatment or prophylaxis of dermatological conditions, such as inflammatory skin disorders, acne, disorders of increased cell turnover such as psoriasis, skin cancers and photoaging. The amorphous retinol/calcium-polyphosphate nanospheres displayed the following: (i) Homogenous size in a range (~45 nm) optimal for cellular uptake by clathrin-mediated endocytosis; (ii) Synergistic effect of both components, retinol and polyphosphate, at non-effective concentrations of the individual components, on cell proliferation and collagen expression (types I, II, and III); (iii) Pronounced synergistic effect on expression of collagen type III; (iv) Disintegration by extracellular enzymatic hydrolysis; (v) Dual biological effect of polyP and retinol, both via the extracellular and via the intracellular route; and (vi) No cytotoxicity.
机译:一种制备可降解的非晶态类维生素A /多磷酸钙纳米球的方法,包括:(i)将类维生素A和钙盐溶解在有机溶剂中; (ii)将步骤(i)中制得的类维生素A钙盐溶液加入到含有溶解的聚磷酸盐(polyp)盐和聚(乙二醇)或另一种润滑性涂料的水溶液中,和(iii)用水洗涤并干燥形成的纳米球。优选地,类视黄醇是视黄醇。优选地,多磷酸盐的链长在约3至约1000个磷酸盐单元的范围内。优选地,无定形类维生素A /聚磷酸钙纳米球用于治疗或预防皮肤病,例如炎性皮肤疾病,痤疮,细胞更新增加的疾病例如牛皮癣,皮肤癌和光老化。非晶态视黄醇/聚磷酸钙纳米球显示以下内容:(i)均相大小(约45 nm),最适合网格蛋白介导的内吞作用吸收细胞; (ii)视黄醇和多磷酸盐两种成分在单独成分的非有效浓度下对细胞增殖和胶原蛋白表达的协同作用(I,II和III型); (iii)对III型胶原蛋白表达的明显协同作用; (iv)通过细胞外酶水解而分解; (v)polyP和视黄醇通过细胞外和细胞内途径的双重生物学效应; (vi)无细胞毒性。

著录项

  • 公开/公告号GB201502116D0

    专利类型

  • 公开/公告日2015-03-25

    原文格式PDF

  • 申请/专利权人 M�LLER WERNER E L;

    申请/专利号GB20150002116

  • 发明设计人

    申请日2015-02-09

  • 分类号A61K33/42;A61K8/24;A61K8/67;A61K9/51;A61K31/07;A61P17;A61P17/06;A61P17/10;A61Q17/04;A61Q19/08;

  • 国家 GB

  • 入库时间 2022-08-21 14:53:58

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号