Diah Lia Aulifa, Annisa Hafizhah Saepudin, Priskila Margaretha, Miski Aghnia Khairinisa, Arif Budiman
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引用次数: 0
摘要
目的：提高药物溶解度对于配制水溶性差的药物，尤其是口服药物至关重要。将药物掺入介孔二氧化硅纳米颗粒（MSN）可提高药物的物理稳定性和溶解性，在制药行业得到广泛应用。因此，本研究旨在阐明水溶性差的药物在介孔二氧化硅纳米颗粒中的作用机制，并评估其对药物溶解和物理稳定性的影响：方法：以α-山莨菪碱（AM）为水溶性差的药物模型，以孔径为 45 Å（MSN45）和 120 Å（MSN120）的 MSN 为介孔材料。通过溶剂蒸发法制备了AM负载的MSN（AM/MSN45和AM/MSN120）：结果：AM/MSN45 和 AM/MSN120 的粉末 X 射线衍射图中观察到的光晕图案以及 DSC 曲线中 AM 的熔融峰和玻璃化转变峰的缺失证实了 AM/MSN45 和 AM/MSN120 的非晶化。这表明 AM 已成功掺入 MSN 中。傅立叶变换红外光谱测量结果表明，AM 的羰基与 MSN 的二氧化硅表面之间形成了氢键作用。在溶解试验中，AM 在 MSN 中的存在提高了溶解速度，并产生了 AM 的过饱和度。然而，MSN 孔径的不同会影响 AM 在 MSN 中的溶解情况。此外，在 25 oC 和 0% RH 条件下储存 30 d 后，它还保留了 X 射线光晕图案：总之，AM-负载介孔二氧化硅大大提高了溶解度和物理稳定性。
Characterization of Alpha Mangostin Loaded-Mesoporous Silica Nanoparticle and the Impact on Dissolution and Physical Stability.
Purpose: Improving drug solubility is crucial in formulating poorly water-soluble drugs, especially for oral administration. The incorporation of drugs into mesoporous silica nanoparticles (MSN) is widely used in the pharmaceutical industry to improve physical stability and solubility. Therefore, this study aimed to elucidate the mechanism of poorly water-soluble drugs within MSN, as well as evaluate the impact on the dissolution and physical stability.
Methods: Alpha mangostin (AM) was adopted as a model of a poorly water-soluble drug, while MSN with the pore size of 45 Å (MSN45) and 120 Å (MSN120) were used as Mesoporous materials. AM-loaded MSN (AM/MSN45 and AM/MSN120) was prepared by solvent evaporation method.
Results: The amorphization of AM/MSN45 and AM/MSN120 was confirmed by the halo pattern observed in the powder X-ray diffraction pattern and the absence of the melting peak and the glass transition of AM in the DSC curves. This signified the successful incorporation of AM into MSN. FT-IR measurements suggested the formation of hydrogen bond interaction between the carbonyl group of AM and the silica surface of MSN. In the dissolution test, the presence of the AM within MSN improved the dissolution rate and generated the supersaturation of AM. However, the difference of pores size of MSN could affect the dissolution profile of AM within MSN. Additionally, it retained the X-ray halo patterns after 30 d of storage at 25 oC and 0% RH.
Conclusion: In conclusion, AM-loaded mesoporous silica significantly improved the dissolution and physical stability.
期刊介绍：
Nanotechnology, Science and Applications is an international, peer-reviewed, Open Access journal that focuses on the science of nanotechnology in a wide range of industrial and academic applications. The journal is characterized by the rapid reporting of reviews, original research, and application studies across all sectors, including engineering, optics, bio-medicine, cosmetics, textiles, resource sustainability and science. Applied research into nano-materials, particles, nano-structures and fabrication, diagnostics and analytics, drug delivery and toxicology constitute the primary direction of the journal.
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