Sonophoresis mediated diffusion of caffeine loaded Transcutol® enriched cerosomes for topical management of cellulite

• Published in: European journal of pharmaceutical sciences Vol. 201; p. 106875
• Main Authors: Albash, Rofida, Abdelbari, Manar Adel, Elbesh, Rovan M., Khaleel, Eman F., Badi, Rehab Mustafa, Eldehna, Wagdy M., Elkaeed, Eslam B., El Hassab, Mahmoud A., Ahmed, Sara Mohamed, Mosallam, Shaimaa
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 01-10-2024
• Subjects: Administration, Cutaneous; Administration, Topical; Animals; Caffeine; Caffeine - administration & dosage; Caffeine - chemistry; Cellulite; Cellulite - therapy; Dermatokinetic study; Diffusion; Drug Liberation; Ethylene Glycols; Liposomes; Male; Particle Size; Rats; Rats, Wistar; Skin - metabolism; Skin Absorption; Sonophoresis; Transcutol® enriched cerosomes; Sonophoresis; Transcutol® enriched cerosomes; Dermatokinetic study; Cellulite; Caffeine
• ISSN: 0928-0987; 1879-0720; 1879-0720
• DOI: 10.1016/j.ejps.2024.106875

The goal of this research was to augment the deposition of caffeine loaded Transcutol® enriched cerosomes (TECs) gel for efficient topical treatment of cellulite utilizing the sonophoresis technique. Caffeine-loaded TECs were prepared using thin film hydration method applying 23 factorial design to study the impact of different factors, each with two levels on the entrapment efficiency (EE%), particle size (PS), polydispersity index (PDI), and zeta potential (ZP) of the formulated TECs. The studied factors were cetyl trimethyl ammonium bromide (CTAB) amount (mg) (X1), phosphatidylcholine (PC) amount (mg) (X2), and Transcutol® amount (mg) (X3). Design-Expert® software was utilized to determine the optimum TECs formulation. Afterward, the optimum TECs formulation was loaded into a gel and subjected to extra investigations. The optimum TECs formulation was (TEC5) which was prepared using 10 mg of CTAB, 150 mg of PC, and 10 mg of Transcutol®. TEC5 presented EE% of 87.44 ± 0.14 %, PS of 308.60 ± 13.38 nm, PDI of 0.455 ± 0.030, and ZP of 50.20 ± 1.55 mV. TEC5 had a fiber-like morphology, with elongated tubules of ceramide. Further, the optimum TECs formulation showed a high stability profile. Moreover, an in vivo dermatokinetic study showed superior deposition of caffeine from TEC5 gel coupled with the sonophoresis on rat skin compared to TEC5 gel and caffeine gel. Moreover, the histopathological study of TEC5 on rat skin confirmed the non-irritant nature of TEC 5 gel mediated by ultrasonic waves through the skin. Overall, the outcomes exposed the obvious superiority of sonophoresis delivered TECs-gel for topical delivery of caffeine for cellulite management.
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