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用喷雾干燥粉末替代原有液体混悬剂的局部纳米药物,提高了维甲酸的光稳定性,且无疗效损失。

Improved tretinoin photostability in a topical nanomedicine replacing original liquid suspension with spray-dried powder with no loss of effectiveness.

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal de Santa Maria, Santa Maria, RS, Brazil.

出版信息

Drug Dev Ind Pharm. 2013 Apr;39(4):579-86. doi: 10.3109/03639045.2012.691510. Epub 2012 Jun 15.

Abstract

OBJECTIVE

The use of spray-dried powders containing tretinoin-loaded nanocapsules instead of the original liquid suspension, aimed at the preparation of dermatological nanomedicines with improved photostability, was investigated.

METHODS

Powders were prepared using lactose as a drying adjuvant. Hydrogels were prepared using two approaches: dispersing Carbopol Ultrez 10 in an aqueous redispersion of the powder or incorporating the powder in previously formed hydrogels.

RESULTS AND DISCUSSION

The photodegradation of tretinoin in hydrogels prepared with the powders showed similar half-life times (around 19.5 h) compared to preparations with the original liquid nanocapsules (20.7 ± 1.4 h), regardless of the preparation approach. In addition, the topical nanomedicines prepared with the spray-dried powders presented a significant improvement in tretinoin photostability compared to the formulation containing the non-encapsulated drug.

CONCLUSION

This study verified that the addition of the spray-dried powders containing tretinoin-loaded lipid-core nanocapsules to hydrogels did not influence the photoprotection of the drug compared with the preparation procedure using the original liquid suspension.

摘要

目的

研究使用载有维 A 酸的纳米胶囊的喷雾干燥粉末代替原始的液体混悬剂,旨在制备具有改善的光稳定性的皮肤科纳米药物。

方法

使用乳糖作为干燥助剂制备粉末。水凝胶通过两种方法制备:将 Carbopol Ultrez 10 分散在粉末的水性再分散液中,或在先前形成的水凝胶中加入粉末。

结果与讨论

与用原始液体纳米胶囊制备的制剂(20.7 ± 1.4 h)相比,用粉末制备的水凝胶中维 A 酸的光降解半衰期相似(约 19.5 h),无论制备方法如何。此外,与含有非包封药物的制剂相比,用喷雾干燥粉末制备的局部纳米药物显著提高了维 A 酸的光稳定性。

结论

这项研究证实,与使用原始液体混悬剂的制备程序相比,将含有载有维 A 酸的脂质核纳米胶囊的喷雾干燥粉末添加到水凝胶中并不会影响药物的光保护作用。

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