Background: Delivering plant extract at high loading with intact antioxidants and efficient skin permeation always remains a challenge. To address this, we prepared a stable gel formulation containing nanoethosomes loaded with Achillea millefolium L. (AM) extract for topical drug delivery.Method: The AM extract was tested at first for phytochemical analysis, antioxidant activity, total phenolic and flavonoid content, and FTIR examination. The nanoethosomes containing AM extract were synthesized and characterized by size, surface charge, and morphology, and entrapment efficiency (EE) was determined. The optimized nanoethosomes were then incorporated to develop a topical gel formulation and subjected to skin for permeation, pH, viscosity, and organoleptic evaluation for up to three months.Results: The AM ethanolic extract demonstrated 88% free radical scavenging activity and notable phenolic and flavonoid contents of up to 123 mg GAE/g and 42 mg QE/g, respectively. The optimized nanoethosomes encapsulated with AM extract (240 nm) were spherical in shape, with −31.1 mV of surface charge, and showed considerable entrapment efficiency (90%). Furthermore, the selected topical gel remained stable during the study period. The Exvivo permeation study of ethosomal gel showed the highest release percentage of 79.8%.Conclusion: The study concludes that topical gel loaded with nanoethosomes containing AM extract is an encouraging approach for topical drug delivery.

The utilization of phytoconstituents in skin care products has emerged as a notable trend due to their recognized safety and therapeutic efficacy. However, the challenge lies in improving the effective delivery of phytoconstituents to specific tissues, primarily attributed to their poor solubility and low permeability. This study endeavors to address this challenge by developing, optimizing and characterizing Cucumis melo var. agrestis (CME) extract loaded nanoemulsion gel (CME-NEG), aiming to enhance the skin permeability and antifungal activity. Herein, nanoemulsions encapsulating the plant extract were prepared using ultrasonication technique and were characterized for droplet size, zeta potential, polydispersity index (PDI) and entrapment efficiency. Further, Fourier transform infrared spectroscopy (FTIR) and scanning electron microscopy (SEM) analysis were conducted to characterize the optimized CME extract loaded nanoemulsion (CME-NE 3) formulation. The optimized formulation was blended with Carbopol 940 gel to develop CME-NEG, which was evaluated for release kinetics, in vitro permeation and in vitro antifungal activity. High performance liquid chromatography (HPLC) analysis confirmed the presence of gallic acid, chlorogenic acid, 4-Hydroxy benzoic acid (HB acid), kaempferol, caffeic acid and quercetin. Findings of 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay showed that the ethanolic extract had highest antioxidant activity (88.88 %). The optimized formulation displayed smooth spherical nanodroplets with size of 175.5 ± 1.56 nm, zeta potential of −21.5 ± 0.12 mV, PDI of 0.192 ± 0.06, and highest entrapment efficiency (EE) of 91.35 ± 1.65 %. The release profile of CME-NE exhibited a controlled release characteristic and the release kinetic mechanism was best described by the Korsmeyer-Peppas (Kp) model. In a 24 h permeation study, it was observed that the in vitro permeation of CME-NEG was 58.63 %, significantly higher than that of CME extract loaded plain gel (CME-PG) with an enhancement ratio of 2.12. The prepared CME-NEG formulation also presented enhanced antifungal activity as compared to pure CME extract. In conclusion, the designed CME-NEG offers a promising topical drug delivery system with enhanced skin permeability and antifungal activity.

Emulgel is a new innovatory technique for drug development permitting controlled release of active ingredients for topical administration. We report a stable emulgel of 4% Piper nigrum extract (PNE) prepared using 80% ethanol. The PNE-loaded formulation had an antioxidant activity of 84% and tyrosinase inhibition was 82%. Prepared formulation rendered spherical-shaped globules with high zeta potential (−45.5 mV) indicative of a stable system. Total phenolic contents were 58.01 mg GAE/g of dry extract whereas total flavonoid content was 52.63 mg QE/g of dry extract. Sun protection factor for PNE-loaded emulgel was 7.512 and formulation was stable without any evidence of physical and chemical changes following 90 days of storage. Gas chromatography-mass spectroscopy (GC-MS) revealed seventeen bioactive compounds in the PNE including monoterpenoids, triterpenoids, a tertiary alcohol, fatty acid esters, and phytosterols. In silico studies of GC-MS identified compounds show higher binding affinity in comparison to standard kojic acid indicating tyrosinase inhibition. It can be concluded that PNE-loaded emulgel had prominent antioxidant and tyrosinase inhibition and can be utilized as a promising topical system for anti-aging skin formulation.

Alpha arbutin is a skin-whitening agent in cosmetics. Structurally, it is 4-hydroxyphenyl-α-glucopyranoside. Ethosomes encourage the formation of lamellar-shaped vesicles with improved solubility and entrapment of whitening agents. The objective of this study was to fabricate an optimized nanostructured ethosomal gel loaded with alpha arbutin for the treatment of skin pigmentation.

Antioxidants from natural sources are extensively attaining consideration to avert the skin from damage and aging caused by free radicals. Flaxseed (Linum usitatissimum L.), a natural therapeutic agent, was meant to be explored cosmeceutical by quantifying its potential phytoconstituents and to be incorporated into a microemulgel for topical use. Hydroalcoholic fractions (both methanolic and ethanolic; 80%) flaxseed extracts were subjected to phytochemical screening by quantifying total phenolic content (TPC), total flavonoid content (TFC), and high-performance liquid chromatography-ultraviolet (HPLC-UV), and for biological activities through 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay, tyrosinase inhibition assay, and sun protection factor (SPF). Ethanolic fraction was selected for further study by TPC (18.75 mg gallic acid equivalent/g) and TFC (1.34 mg quercetin equivalent/g). HPLC-UV analysis showed the existence of benzoic, quercetin, caffeic, vanillic, p-coumaric, gallic, cinnamic, syringic, and sinapic acids. Biological activities showed 87.00%, 72.00%, and 21.75 values for DPPH assay, tyrosinase inhibition, and SPF assays, respectively. An oil-in-water (OW) microemulsion containing the flaxseed extract, with 99.20 nm Zeta size, −19.3 Zeta potential and 0.434 polydispersity index was developed and incorporated in Carbopol-940 gel matrix to formulate an active microemulgel with 59.15% release in in vitro studies. The successfully formulated stable active microemulgel produced statistically significant effects (p < 0.05), in comparison to a placebo, on skin erythema, melanin, sebum, moisture, and elasticity, in a noninvasive in vivo study performed on 13 healthy human female volunteers. Other cosmeceutical products can also be formulated from flaxseed, making it a considerable candidate for further utilization in the pharmaceutical industry.