Gelation behavior, drug solubilization capacity and release kinetics of poloxamer 407 aqueous solutions: The combined effect of copolymer, cosolvent and hydrophobic drug

Gelation behavior, drug solubilization capacity and release kinetics of poloxamer 407 aqueous solutions: The combined effect of copolymer, cosolvent and hydrophobic drug
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DOI:
10.1016/j.molliq.2020.112639
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发表时间:
2020-04-01
影响因子:
6
通讯作者:
Medarevic, Dorde
Medarevic, Dorde
中科院分区:
化学2区
文献类型:
--
作者:
Djekic, Ljiljana;Calija, Bojan;Medarevic, Dorde

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该研究阐明了处方参数(共聚物(泊洛沙姆407(P407))、助溶剂(异丙醇)和疏水性药物(布洛芬)的相对含量)对P407水溶液在常见储存和局部给药条件下的凝胶化、应用特性、药物增溶能力和释放动力学的综合影响。布洛芬以5%的治疗浓度的存在增强了胶束体积分数的增加,并允许在P407浓度>= 15%时液体溶液的胶凝。光学显微镜、DSC分析和流变学测量指出,具有15-20%共聚物的P407凝胶能够控制无定形布洛芬颗粒的沉淀(
The study elucidated the combined effect of the formulation parameters (the relative contents of the copolymer (poloxamer 407 (P407)), the cosolvent (isopropyl alcohol), and the hydrophobic drug (ibuprofen)) on gelation, applicative properties, drug solubilization capacity and release kinetics of the P407 aqueous solutions under the common conditions of storage and topical administration. The presence of ibuprofen at a therapeutic concentration of 5% enhanced the increase in micellar volume fraction and allowed the gelation of the liquid solutions at P407 concentrations >= 15%. Light microscopy, DSC analysis, and theological measurements pointed that P407 gels with 15-20% of the copolymer enabled controled precipitation of amorphous ibuprofen particles (