用于局部递送白杨素的西番莲果油乳胶凝胶设计及通过光声光谱法进行的皮肤渗透体外评估。
Design of Passion Fruit Oil Emulgel for Topical Chrysin Delivery and Ex Vivo Evaluation of Skin Permeation by Photoacoustic Spectroscopy.
作者信息
de Souza Bruna Gheller, de Castro Hoshino Lidiane Vizioli, Faccin Thalita Schilive, Baesso Mauro Luciano, Borghi-Pangoni Fernanda Belincanta, Bruschi Marcos Luciano
机构信息
Laboratory of Research and Development of Drug Delivery Systems, Department of Pharmacy, Postgraduate Program in Pharmaceutical Sciences, State University of Maringa, Maringa, PR, Brazil.
Department of Physics, State University of Maringa, Maringa, PR, Brazil.
出版信息
AAPS PharmSciTech. 2025 Jun 27;26(6):173. doi: 10.1208/s12249-025-03164-x.
Chrysin, a flavonoid effective against various skin cancers, displays poor solubility, skin permeation, and bioavailability. Emulgel emerges as an innovative and promising strategy for the topical administration of chrysin, offering significant advantages over existing systems. Passion fruit oil (PFO) enhances topical formulations with improved safety, compatibility, and drug delivery. However, current emulgels raise safety concerns due to their surfactant, co-surfactant, and oily co-solvent content. This study aimed to develop innovative emulgel containing PFO, without unsafe surfactants, for the topical delivery of chrysin. ATR-FTIR and DSC analyses of chrysin and excipients were performed. A 3-factorial design was used, and the formulations were evaluated for preliminary physicochemical stability, mechanical and rheological properties, in-vitro release profile of chrysin, bioadhesion and ex-vivo skin permeation by photoacoustic spectroscopy (PAS). ATR-FTIR and DSC analyses confirmed the compatibility of chrysin with the formulation excipients. Formulations F6, F11, and F21 were stable and exhibited hardness (0.2006-0.4299 N), compressibility (1.4737-3.4300 N.mm), elasticity (0.9924 - 1.0034 mm), adhesiveness (0.8077-2.2217 N.mm), cohesiveness (0.7637 - 0.8733), softness index (0.0648 - 0.1525 N), and bioadhesive strength (0.0648 - 0.0754 N), both values with relative standard deviation less than 9%. They were pseudoplastic with yield value, thixotropy, and viscoelasticity. Chrysin release profile was slow and governed by anomalous transport. PAS analysis showed chrysin could permeate the stratum corneum and epidermis, reaching the dermal layer. The selected emulgels are promising for effective topical application, and the formulation F21 standing out in particular for further both in vitro and in vivo biological evaluations.
白杨素是一种对多种皮肤癌有效的黄酮类化合物,但溶解性、皮肤渗透性和生物利用度较差。乳化凝胶作为一种用于白杨素局部给药的创新且有前景的策略,相对于现有体系具有显著优势。西番莲果油(PFO)可增强局部制剂的安全性、相容性和药物递送效果。然而,目前的乳化凝胶因其表面活性剂、助表面活性剂和油性助溶剂成分而引发安全问题。本研究旨在开发不含不安全表面活性剂的含PFO的创新乳化凝胶,用于白杨素的局部递送。对白杨素和辅料进行了衰减全反射傅里叶变换红外光谱(ATR-FTIR)和差示扫描量热法(DSC)分析。采用三因素设计,并对制剂的初步物理化学稳定性、机械和流变学性质、白杨素的体外释放曲线、生物黏附性以及通过光声光谱法(PAS)进行的离体皮肤渗透性进行了评估。ATR-FTIR和DSC分析证实了白杨素与制剂辅料的相容性。制剂F6、F11和F21稳定,表现出硬度(0.2006 - 0.4299 N)、可压缩性(1.4737 - 3.4300 N·mm)、弹性(0.9924 - 1.0034 mm)、黏附性(0.8077 - 2.2217 N·mm)、内聚性(0.7637 - 0.8733)、柔软度指数(0.0648 - 0.1525 N)和生物黏附强度(0.0648 - 0.0754 N),两者值的相对标准偏差均小于9%。它们具有假塑性,并具有屈服值、触变性和黏弹性。白杨素的释放曲线缓慢且受异常转运控制。PAS分析表明白杨素可渗透角质层和表皮,到达真皮层。所选的乳化凝胶有望用于有效的局部应用,制剂F21尤其突出,值得进一步进行体外和体内生物学评估。