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载有格列齐特的聚二甲基硅氧烷有机-无机复合药物贮库

Polydimethylsiloxane Organic-Inorganic Composite Drug Reservoir with Gliclazide.

机构信息

Curtin Medical School, Curtin University, Bentley 6102, Australia.

Curtin Health Innovation Research Institute, Curtin University, Bentley 6102, Australia.

出版信息

Int J Mol Sci. 2024 Apr 3;25(7):3991. doi: 10.3390/ijms25073991.

Abstract

A novel organic-inorganic gliclazide-loaded composite bead was developed by an ionic gelation process using acidified CaCl, chitosan and tetraethylorthosilicate (TEOS) as a crosslinker. The beads were manufactured by crosslinking an inorganic silicone elastomer (-OH terminated polydimethylsiloxane, PDMS) with TEOS at different ratios before grafting onto an organic backbone (Na-alginate) using a 3 factorial experimental design. Gliclazide's encapsulation efficiency (EE%) and drug release over 8 h (% DR 8 h) were set as dependent responses for the optimisation of a pharmaceutical formula (herein referred to as 'G op') by response surface methodology. EE % and %DR 8 h of G op were 93.48% ± 0.19 and 70.29% ± 0.18, respectively. G op exhibited a controlled release of gliclazide that follows the Korsmeyer-Peppas kinetic model (R = 0.95) with super case II transport and pH-dependent swelling behaviour. In vitro testing of G op showed 92.17% ± 1.18 cell viability upon testing on C2C12 myoblasts, indicating the compatibility of this novel biomaterial platform with skeletal muscle drug delivery.

摘要

采用离子凝胶法,以酸化的 CaCl2、壳聚糖和正硅酸乙酯(TEOS)为交联剂,制备了一种新型的有机-无机格列齐特载药复合微球。通过在不同比例下用 TEOS 交联无机硅弹性体(-OH 封端的聚二甲基硅氧烷,PDMS),然后使用 3 因子实验设计将其接枝到有机主链(海藻酸钠 Na)上,制备了微球。格列齐特的包封效率(EE%)和 8 小时内的药物释放率(%DR 8 h)被设定为依赖响应,通过响应面法对药物配方(此处称为“G op”)进行优化。G op 的 EE%和%DR 8 h 分别为 93.48%±0.19 和 70.29%±0.18。G op 表现出格列齐特的控制释放,遵循 Korsmeyer-Peppas 动力学模型(R = 0.95),具有超二级传输和 pH 依赖性溶胀行为。G op 的体外测试结果表明,在 C2C12 成肌细胞上测试时,细胞活力为 92.17%±1.18%,表明这种新型生物材料平台与骨骼肌药物输送的相容性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/06c1/11012350/6c30c2bed305/ijms-25-03991-g001.jpg

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