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介孔硅纳米粒子促进口腔分散片中药品的溶解。

Mesoporous silica nanoparticles facilitating the dissolution of poorly soluble drugs in orodispersible films.

机构信息

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Artillerigatan 6A, 20520 Turku, Finland.

Pharmaceutical Sciences Laboratory, Faculty of Science and Engineering, Åbo Akademi University, Artillerigatan 6A, 20520 Turku, Finland.

出版信息

Eur J Pharm Sci. 2018 Sep 15;122:152-159. doi: 10.1016/j.ejps.2018.06.027. Epub 2018 Jul 5.

Abstract

Orodispersible films (ODF) are immediately dissolving/disintegrating intraoral dosage forms, presented as substitutes of conventional tablets or capsules to ease problems associated with swallowing. Efforts have been made to be able to exploit ODFs as dosage forms for poorly soluble drugs. In the last two decades, mesoporous silica nanoparticles (MSNs) have been extensively used in drug delivery applications to overcome solubility problems of drugs. The tunable features of MSNs make them suitable candidates as drug carriers and solubility enhancers. In this study, the feasibility of MSNs as a carrier of poorly soluble drugs, using prednisolone as a model drug, in ODFs was investigated. Our results revealed that the increased amount of MSNs in ODFs leads to shortening of the disintegration time of the films. Drug content investigations showed that low dose ODFs with prednisolone incorporation efficiencies higher than 80% could be produced. Furthermore, the prednisolone release profile from ODFs can be tuned with the incorporation of MSNs as drug carrier (MSN). The MSN incorporated ODFs yield with immediate release of drug from the ODF, whereby 90% of the prednisolone content could be released in the first minutes. By modifying the MSN design with copolymer surface coating, prednisolone (cop-MSN) release can be modulated into a two-step sustained release profile. To sum up, the MSNs platform does not only provide careful low dose incorporation into ODF with high efficiency, but it also aids in tuning the drug release profiles from ODFs.

摘要

口溶膜(ODF)是一种即刻溶解/崩解的口腔内给药剂型,可替代传统片剂或胶囊,以缓解吞咽相关问题。人们一直致力于将 ODF 用作难溶性药物的剂型。在过去的二十年中,介孔硅纳米粒子(MSNs)已广泛应用于药物传递应用中,以克服药物的溶解度问题。MSNs 的可调特性使其成为药物载体和增溶剂的合适候选物。在这项研究中,以泼尼松龙为模型药物,研究了 MSNs 作为难溶性药物载体在 ODF 中的可行性。我们的结果表明,ODF 中 MSNs 的增加量会导致薄膜崩解时间缩短。药物含量研究表明,可以制备出含泼尼松龙的低剂量 ODF,其载药量效率高于 80%。此外,通过将 MSNs 作为药物载体(MSN)掺入 ODF 中,可以调整泼尼松龙的释放曲线。载有 MSN 的 ODF 立即释放药物,在最初的几分钟内可以释放 90%的泼尼松龙含量。通过对 MSN 进行共聚表面涂层修饰,可以将泼尼松龙(cop-MSN)的释放调节为两步持续释放曲线。总之,MSNs 平台不仅可以为 ODF 提供精心设计的低剂量高效载药,还可以帮助调整 ODF 中的药物释放曲线。

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