Otto Daniel P, Otto Anja, de Villiers Melgardt M
Research Focus Area for Chemical Resource Beneficiation, Faculty of Natural and Agricultural Sciences, North-West University, Potchefstroom 2531, South Africa.
School of Pharmacy, Pharmaceutical Sciences Division, University of Wisconsin-Madison, 777 Highland Ave, Madison, WI 53705, USA.
Pharmaceutics. 2022 Mar 2;14(3):554. doi: 10.3390/pharmaceutics14030554.
Griseofulvin is a poorly water-soluble drug administered orally to treat topical fungal infections of the skin and hair. However, oral administration leads to poor and unpredictable drug pharmacokinetics. Additionally, griseofulvin is unstable in the presence of light. A layer-by-layer (LbL) nanocoating approach was employed to curb these shortcomings by stabilizing emulsions, lyophilized emulsions, and reconstituted emulsions with a layer each of whey protein, and either hyaluronic acid, amylopectin, or alginic acid, which captured the drug. The coating materials are biological, environmentally benign, and plentiful. Photostability studies indicated that the LbL particles afforded 6 h of protection of the topical application. In vitro absorption studies showed that griseofulvin concentrated preferentially in the stratum corneum, with virtually no transdermal delivery. Therefore, LbL-nanocoated emulsions, lyophilized particles, and reconstituted lyophilized emulsions can produce a viable topical delivery system to treat superficial fungal infections.
灰黄霉素是一种水溶性较差的药物,口服用于治疗皮肤和毛发的局部真菌感染。然而,口服给药会导致药物药代动力学不佳且不可预测。此外,灰黄霉素在光照下不稳定。采用层层(LbL)纳米包衣方法来克服这些缺点,通过用乳清蛋白层以及透明质酸、支链淀粉或海藻酸层稳定乳液、冻干乳液和复乳来包裹药物。包衣材料具有生物性、环境友好且来源丰富。光稳定性研究表明,层层颗粒为局部应用提供了6小时的保护。体外吸收研究表明,灰黄霉素优先集中在角质层,几乎没有透皮递送。因此,层层纳米包衣乳液、冻干颗粒和复乳冻干乳液可以产生一种可行的局部给药系统来治疗浅表真菌感染。