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通过溶剂蒸发法将药物包封于介孔二氧化硅中：对不同分子量药物在介孔二氧化硅中的特性进行的比较研究。

Encapsulation of drug into mesoporous silica by solvent evaporation: A comparative study of drug characterization in mesoporous silica with various molecular weights.

作者信息

Budiman Arif, Aulifa Diah Lia

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Universitas Padjadjaran, Jl. Raya Bandung-Sumedang Km. 21, Indonesia.

Department of Pharmaceutical Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Jl. Raya Bandung-Sumedang Km. 21, Indonesia.

出版信息

Heliyon. 2021 Dec 18;7(12):e08627. doi: 10.1016/j.heliyon.2021.e08627. eCollection 2021 Dec.

DOI:10.1016/j.heliyon.2021.e08627
PMID:35005278
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8715180/
Abstract

Mesoporous silica (MS) is a promising material as a drug carrier that is used in pharmaceutical applications. It was discovered that the incorporation of drugs into MS has the potential to improve their dissolution and bioavailability due to the large specific surface area. This study aimed to characterize the drugs with various molecular weights in MS as well as to elucidate their impact on the loading amount and the amorphization within MS. The solvent evaporation method was used to encapsulate itraconazole (ITZ), nifedipine (NIF), and nicotinamide (NIC), respectively, into MS. The result shows the absence of glass transition and the melting peak of ITZ, NIF, and SAC within MS signifying the successful encapsulation. A hallo pattern was found in ITZ and NIF within MS indicating the amorphization. The high molecular weight and the interaction between the drug with the silica surface is reportedly contributed to the formation of the amorphous state. Meanwhile, the characteristic diffraction peaks of NIC crystal were observed for NIC within MS. In conclusion, the molecular weight of the drug has a significant effect on the loading amount and the amorphization of the drug within MS.

摘要

介孔二氧化硅（MS）作为一种药物载体，在制药应用中是一种很有前景的材料。人们发现，由于比表面积大，将药物掺入MS有潜力提高其溶解性和生物利用度。本研究旨在表征MS中不同分子量的药物，并阐明它们对MS内载药量和非晶化的影响。采用溶剂蒸发法分别将伊曲康唑（ITZ）、硝苯地平（NIF）和烟酰胺（NIC）包封到MS中。结果表明，MS内ITZ、NIF和SAC没有玻璃化转变和熔融峰，表明包封成功。在MS内的ITZ和NIF中发现了晕圈图案，表明发生了非晶化。据报道，高分子量以及药物与二氧化硅表面之间的相互作用促成了非晶态的形成。同时，在MS内观察到NIC晶体的特征衍射峰。总之，药物的分子量对MS内药物的载药量和非晶化有显著影响。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/84f49daa13ac/gr12.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/664c49a6dfa9/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/84f49daa13ac/gr12.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/44c66f4ee07d/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/4163958dfbbb/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/781146854417/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/b753c2a7a95a/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/465fefbe93d4/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/805a2474adda/gr5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/76947e519b7f/gr6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/c1faa87706c5/gr7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/61bb58681f36/gr8.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/19c92544d20d/gr9.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/eac7cea10ada/gr10.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/664c49a6dfa9/gr11.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/399e/8715180/84f49daa13ac/gr12.jpg

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