Design of Passion Fruit Oil Emulgel for Topical Chrysin Delivery and Ex Vivo Evaluation of Skin Permeation by Photoacoustic Spectroscopy.

IF 3.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Bruna Gheller de Souza, Lidiane Vizioli de Castro Hoshino, Thalita Schilive Faccin, Mauro Luciano Baesso, Fernanda Belincanta Borghi-Pangoni, Marcos Luciano Bruschi
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Abstract

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 33-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.

百香果油乳状液外用白菊花素的设计及体外透皮光声光谱评价。
黄菊花素是一种对多种皮肤癌有效的类黄酮,但其溶解度、皮肤渗透性和生物利用度较差。乳凝胶作为一种创新的和有前途的策略,局部管理的菊花素,提供显着的优势超过现有的系统。百香果油(PFO)增强局部配方与改进的安全性,相容性和药物输送。然而,目前的乳液由于其表面活性剂、助表面活性剂和油性共溶剂的含量而引起了安全问题。本研究旨在开发含PFO的新型乳液,不含不安全的表面活性剂,用于外用给药。对大黄素及其辅料进行了ATR-FTIR和DSC分析。采用33因子设计,通过光声光谱(PAS)对配方进行初步的理化稳定性、力学和流变性能、金菊素体外释放谱、生物粘附性和离体皮肤渗透性评价。ATR-FTIR和DSC分析证实了菊花素与制剂辅料的相容性。配方F6、F11和F21的硬度(0.2006-0.4299 N)、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)、黏附性(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)相对标准偏差均小于9%。它们是具有屈服值、触变性和粘弹性的假塑性。Chrysin释放缓慢,受异常运输控制。PAS分析表明,金菊素可以渗透角质层和表皮,到达真皮层。所选择的乳液有望有效地局部应用,配方F21特别适合进一步的体外和体内生物学评估。
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来源期刊
AAPS PharmSciTech
AAPS PharmSciTech 医学-药学
CiteScore
6.80
自引率
3.00%
发文量
264
审稿时长
2.4 months
期刊介绍: AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.
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