Enhancement of antifungal activity and transdermal delivery of 5-flucytosine via tailored spanlastic nanovesicles: statistical optimization, in-vitro characterization, and in-vivo biodistribution study.

Autor:	Safhi AY; Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, Saudi Arabia., Naveen NR; Department of Pharmaceutics, Sri Adichunchanagiri College of Pharmacy, Adichunchanagiri University, Mandya, Karnataka, India., Rolla KJ; Department of Biotechnology, Sri Indu Institute of Engineering, Hyderabad, Telangana, India., Bhavani PD; Department of Pharmaceutics, Vishnu Institute of Pharmaceutical Education and Research, Narsapur, Telangana, India., Kurakula M; Thermo Fisher Scientific, Bend, OR, United States., Hosny KM; Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia., Abualsunun WA; Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia., Alissa M; Department of Medical Laboratory Sciences, College of Applied Medical Sciences, Prince Sattam Bin Abdulaziz University, Al-Kharj, Saudi Arabia., Alsalhi A; Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan, Saudi Arabia., Alahmadi AA; Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Saudi Arabia., Zoghebi K; Department of Pharmaceutical Chemistry, College of Pharmacy, Jazan University, Jazan, Saudi Arabia., Halwaani AS; Central Lab for Neurosciences, King Abdulaziz University, Jeddah, Saudi Arabia., Ibrahim K R; Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt.
Jazyk:	angličtina
Zdroj:	Frontiers in pharmacology [Front Pharmacol] 2023 Dec 04; Vol. 14, pp. 1321517. Date of Electronic Publication: 2023 Dec 04 (Print Publication: 2023).
DOI:	10.3389/fphar.2023.1321517
Abstrakt:	Aim and background: This current study aimed to load 5-flucytosine (5-FCY) into spanlastic nanovesicles (SPLNs) to make the drug more efficient as an antifungal and also to load the 5-FCY into a hydrogel that would allow for enhanced transdermal permeation and improved patient compliance. Methods: The preparation of 5-FCY-SPLNs was optimized by using a central composite design that considered Span 60 (X1) and the edge activator Tween 80 (X2) as process variables in achieving the desired particle size and entrapment efficiency. A formulation containing 295.79 mg of Span 60 and 120.00 mg of Tween 80 was found to meet the prerequisites of the desirability method. The optimized 5-FCY-SPLN formulation was further formulated into a spanlastics gel (SPG) so that the 5-FCY-SPLNs could be delivered topically and characterized in terms of various parameters. Results: As required, the SPG had the desired elasticity, which can be credited to the physical characteristics of SPLNs. An ex-vivo permeation study showed that the greatest amount of 5-FCY penetrated per unit area (Q) (mg/cm 2 ) over time and the average flux (J) (mg/cm 2 /h) was at the end of 24 h. Drug release studies showed that the drug continued to be released until the end of 24 h and that the pattern was correlated with an ex-vivo permeation and distribution study. The biodistribution study showed that the 99mTc-labeled SFG that permeated the skin had a steadier release pattern, a longer duration of circulation with pulsatile behavior in the blood, and higher levels in the bloodstream than the oral 99mTc-SPNLs. Therefore, a 5-FCY transdermal hydrogel could possibly be a long-acting formula for maintenance treatment that could be given in smaller doses and less often than the oral formula. Competing Interests: Author MK was employed by Thermo Fisher Scientific. The remaining authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest. (Copyright © 2023 Safhi, Naveen, Rolla, Bhavani, Kurakula, Hosny, Abualsunun, Alissa, Alsalhi, Alahmadi, Zoghebi, Halwaani and Ibrahim K.)
Databáze:	MEDLINE
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