OBJECTIVE: This study aimed to develop an anti-aging nanoformulation with Curcuma heyneana extract as bioactive substance.
BACKGROUND: Curcuma heyneana Valeton & Zipj extract has been proven in previous research to have antioxidant, anti-ageing, anti-inflammatory, and wound healing properties, which makes it a potential bioactive material for anti-ageing and sunscreen cosmetic products. Phytoantioxidants need to penetrate into deeper skin layers to ensure effectivity. Thus, a transdermal delivery system is needed to deliver the extract to a deeper skin layer.
OBJECTIVE: The objective of the study was to compare the permeability and anti-ageing activity of liposomal and ethosomal formulations of C. heynena rhizome ethanolic extract.
METHODS: In this study, C. heyneana extract was loaded into a phospholipid vesicular system in the form of liposome and ethosome formulations using the ethanolic injection method. The anti-ageing activity was assessed by analyzing the epidermal thickness, number of sunburn cells, distance between collagen fibres, and number of fibroblasts. While the histologic specimen scoring was carried out for the in vivo penetration study.
RESULTS: The ethosomal formulation had been found to have better penetration ability since it was able to reach the lower dermis area compared to the liposomes, which only reached the upper dermis. The ethosomal formulation of C. heyneana extract exhibited a better anti-ageing activity based on the parameters of epidermal thickness, sunburn cell count, fibroblast count, and the distance between collagen fibres in rat skin histology.
CONCLUSIONS: Ethosomes have been found to be a more proficient carrier system for transdermal delivery of C. heyneana extract compared to liposomes. Meanwhile, their penetration correlated with the effectivity of the formulation, suggesting that the vesicular system enhanced the penetration ability of the extract.

The present study is aimed to design ethosomes and transethosomes for topical administration of quercetin. To overcome quercetin low bioavailability, scarce solubility and poor permeability that hamper its pharmaceutical use, the drug was loaded in ethosomes and transethosomes based on different concentrations of phosphatidylcholine. Vesicle morphology was studied by cryogenic transmission electron microscopy, while size distribution and quercetin entrapment capacity were evaluated up to 3 months, respectively, by photon correlation spectroscopy and high-performance liquid chromatography. The antioxidant property was studied by photochemiluminescence test. Quercetin release and permeation was investigated in vitro, using Franz cells associated to different membranes. In vitro assays were conducted on human keratinocytes and melanoma cells to study the behavior of quercetin-loaded nano-vesicular forms with respect to cell migration and proliferation. The results evidenced that both phosphatidylcholine concentration and quercetin affected the vesicle size. Quercetin entrapment capacity, antioxidant activity and size stability were controlled using transethosomes produced by the highest amount of phosphatidylcholine. In vitro permeation studies revealed an enhancement of quercetin permeation in the case of transethosomes with respect to ethosomes. Notably, scratch wound and migration assays suggested the potential of quercetin loaded-transethosomes as adjuvant strategy for skin conditions.

Prescription of anti-inflammatory drugs may be considered as a promising strategy in chronic wound healing where the inflammatory disturbance has delayed the healing process. It seems that hydrocortisone 17-butyrate (HB17) would be promising in the form of a nano-formulation to enhance drug delivery efficacy. In the present study, transdermal delivery of nano-HB17 in combination with iontophoresis was investigated ex vivo. Ethosomal-HB17 was synthesised using lecithin, ethanol and cholesterol with a different ratio by hot method. The negative ethosomal-HB17 particle size was around 244 ± 4.3 nm with high stability of up to 30 days. Additionally, evaluated entrapment efficiency of HB17 in ethosomes by high performance liquid chromatography was 40.6 ± 2.21%. Moreover, the permeation speed and amount of H17B in complete-thickness rat skin in the presence and absence of iontophoresis showed that the penetration of free H17B and ethosomal-H17B formulations were zero and 7.98 μg/cm2 in 120 min, respectively. Whereas in the case of applying iontophoresis, permeation amount obtained was zero and 19.69 μg/cm2 in 30 min in free H17B and ethosomal-H17B formulations, respectively. It has been concluded that transdermal delivery of ethosomal-H17B is an effective strategy to enhance drug delivery and it will be improved when it is combined with iontophoresis.

BACKGROUND: To understand the cumulative effect of topical formulations after medication, evaluate the therapeutic effect of microneedle-assisted (MN-assisted) paeoniflorin-loaded ethosomes (TGP-E), and explore the potential for deep penetration of drugs, this paper uses microdialysis to systematically study the percutaneous pharmacokinetics of TGP-E.
METHODS: First, optical coherence tomography (OCT) was used to study the effectiveness of microneedle puncture. Second, a microdialysis method and a UPLC-MS method for determining the amount of paeoniflorin (Pae) in dialysate were established. Finally, the transdermal pharmacokinetics of TGP-E was studied using in vivo microdialysis in rats under the above MN-assisted conditions.
RESULTS: The optimal MN-assisted conditions were obtained at a microneedle length of 500 μm, a pressure of 3 N, and an action time of 3 min. The pharmacokinetic results demonstrated that the maximum drug concentration (Cmax) and the area under the curve (AUC) of the TGP-E gel were higher than the TGP-saline solution gel, and the mean retention time was lower. These indicated that microneedle can promote the entry of the ethosomes into the skin for in vivo experiments and greatly improve the possibility of deep penetration of the water-soluble Pae.
CONCLUSIONS: Therefore, the microneedle-ethosomes delivery system is a more ideal means for promoting the deep penetration of Pae. These findings may provide a reference for the combination of multiple penetration-enhancement ways to promote drug absorption, and also provide a new insight to realize the development of novel, safe, and more effective dosage forms and administration routes of drugs.