Hyaluronan-modified transfersomes based hydrogel for enhanced transdermal delivery of indomethacin

• Main Authors: Ming Yuan (Author), Jiangxiu Niu (Author), Qinghan Xiao (Author), Huiyuan Ya (Author), Yansong Zhang (Author), Yanli Fan (Author), Lingmei Li (Author), Xueke Li (Author)
• Format: Book
• Published: Taylor & Francis Group, 2022-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.1080/10717544.2022.2053761; 1521-0464; 1071-7544
• Keywords: Transdermal drug delivery; transfersome; hydrogel; indomethacin; hyaluronan; Therapeutics. Pharmacology; RM1-950
• Source: Drug Delivery, Vol 29, Iss 1, Pp 1232-1242 (2022)

Hyaluronic acid (HA), as a hygroscopic and biocompatible molecule, has displayed unique permeation enhancement in transdermal delivery systems. Hence, indomethacin (IND) was encapsulated in HA-modified transfersomes (IND-HTs) to enhance transdermal IND delivery to reduce adverse effects in this study. The physiochemical properties of IND-HTs were characterized. Results showed that the prepared IND-HTs were spherical and revealed good entrapment efficiency (87.88 ± 2.03%), with a nanometric particle size (221.8 ± 93.34 nm). Then, IND-HTs were further incorporated into a carbopol 940 hydrogel (IND-HTs/Gel) to prolong retention capacity on the skin. The in vitro release and skin permeation experiments of IND-HTs/Gel were carried out with the Franz diffusion cells. It was found that IND-HTs/Gel exhibited sustained drug release, as well as superior drug permeation and flux across the skin. Confocal laser scanning microscopy showed improved penetration of HTs/Gel with a wider distribution and higher fluorescence intensity. The hematoxylin-eosin stained showed that HA improved the transdermal effect by changing the microstructure of skin layers and decreasing skin barrier function. In addition, IND-HTs/Gel showed significant analgesic activity in hot plate test and no potentially hazardous skin irritation. This study indicated that the developed IND-HTs/Gel could be a promising alternative to conventional oral delivery of IND by topical administration.