Abstract
Objective: A transfersome is a drug delivery system that offers increased penetration for the transdermal delivery of drugs. The aim of this study wasto assess the application of transfersomes for transdermal delivery of andrographolide.Methods: The development of andrographolide transfersomes for transdermal delivery was conducted in two steps. The first step involved varyingratios of Span 80 and phospholipids to investigate the effect on transfersome deformability using four formulations (P1–P4). Afterward, a second stepinvolved varying ratios of andrographolide in transfersomes to investigate the influence on entrapment efficiency using four formulations (F1–F4).The selected transfersomes were then formulated into a gel dosage form. An in vitro penetration study was conducted by comparing the penetrationfluxes of the transfersome and non-transfersome andrographolide gels using Franz diffusion cells.Results: The results showed that formulation F4 had an entrapment efficiency of 97.02±0.01% and particle size (DV-average) of 524.02 nm. An in vitropenetration study of the andrographolide transfersome gels showed two phases of penetration, with a marked increase in both fluxes. In the firstphase, penetration flux was 23.26±2.34 and 1.28±0.82 μg/cm2·h for the transfersome and non-transfersome andrographolide gels, respectively.Conclusion: The results showed that the transfersome gel is a promising dosage system for transdermal delivery of andrographolide.
Highlights
Andrographolide is the main chemical constituent of the stem and leaves of Andrographis paniculata
Formulation and evaluation of andrographolide transfersomes Transfersomes F1–F4 formed colloidal dispersions that were white in color
Optimization and evaluation of andrographolide transfersomes Transfersomes were prepared by thin-film hydration, which is widely used in many studies, as this method is relatively easy to conduct in the laboratory setting [11,12,15]
Summary
Andrographolide is the main chemical constituent of the stem and leaves of Andrographis paniculata. Recent studies have reported the anticancer effects of andrographolide [2]. Andrographolide was characterized as having a low absolute oral bioavailability of 2.67%. Andrographolide is extensively metabolized in the duodenum and jejunum, and less so in the ileum and colon. The metabolism process results in an inactivated and sulfated form of andrographolide. High concentrations of sulfated andrographolide metabolites have been found in the liver, indicating extensive liver metabolism. The oral bioavailability of andrographolide is hindered by its poor absorption in the terminal ileum and colon due to the presence of efflux transporters. Oral administration of andrographolide at both low and high concentrations results in poor absolute oral bioavailability [3]
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