用纳米沉淀法包封异烟肼

A. Galiyeva, Y. Tazhbayev, T. Zhumagaliyeva, A.Т. Daribay
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摘要

高分子材料作为药物载体具有延长药物作用时间、减少药物副作用等优点。在这项研究中,我们考虑了用纳米沉淀法制备抗结核药物(ATD)异烟肼的聚乳酸-羟基乙酸酯(PLGA)聚合物纳米颗粒的方法。通过改变溶剂-非溶剂性质、药/聚合物比和稳定剂浓度等参数,获得了高分子纳米载体。确定了平均粒径取决于非溶剂的类型。当使用醇时,平均尺寸依次增大:乙醇<异丙醇<异丁醇。溶剂类型是决定纳米颗粒形成及其最终特性的重要因素。随着药物/聚合物比的增加,纳米颗粒的平均尺寸也增加。所得纳米颗粒的大小从93 ~ 869 nm不等。热重法和差示扫描量热法分析证实了药物与聚合物基质的结合。此外,还研究了聚合物在不同pH下的降解及异烟肼从聚合物基质中释放的程度。研究表明,纳米沉淀法不仅可用于疏水药物,也可用于亲水药物。
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Encapsulation of Isoniazid in Polylactide-Co-Glycolide Nanoparticles by Nanoprecipitation
The use of polymeric materials as drug carriers has several advantages, such as prolongation of drug action, reduction of drug side effects. In this study, we have considered the methods for the preparation of polylac-tide-co-glycolide (PLGA) polymeric nanoparticles with the anti-tuberculosis drug (ATD) isoniazid by nano-precipitation. Polymeric nanocarriers were obtained by varying individual parameters such as nature of sol-vent and non-solvent, drug/polymer ratio, and stabilizer concentration. It was determined that the average par-ticle size depends on the type of non-solvent. When alcohols were used, the average size increased in the se-quence: ethanol < isopropanol < isobutanol. The type of solvent is an important factor for the formation of nanoparticles and their final characteristics. With an increase in the drug/polymer ratio, the average size of nanoparticles also increased. The size of obtained nanoparticles varied from 93 to 869 nm. Thermogravi-metric and differential scanning calorimetry analyses were carried out to confirm the incorporation of the drug into the polymer matrix. In addition, polymer degradation and the degree of release of isoniazid from the polymeric matrix at different pH were studied. It has been shown that the nanoprecipitation method can be used not only for hydrophobic, but also for hydrophilic drugs.
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