Voriconazole (VRC) is a broad-spectrum antifungal agent belonging to BCS class II (biopharmaceutical classification system). Despite many efforts to enhance its solubility, this primary issue still remains challenging for formulation scientists. Transethosomes (TELs) are one of the potential innovative nano-carriers for improving the solubility and permeation of poorly soluble and permeable drugs. We herein report voriconazole-loaded transethosomes (VRCT) fabricated by the cold method and followed by their incorporation into carbopol 940 as a gel. The prepared VRCT were evaluated for % yield, % entrapment efficiency (EE), surface morphology, possible chemical interaction, particle size, zeta potential, and polydispersity index (PDI). The optimized formulation had a particle size of 228.2 nm, a zeta potential of −26.5 mV, and a PDI of 0.45 with enhanced % EE. Rheology, spreadability, extrudability, in vitro release, skin permeation, molecular docking, antifungal, and antileishmanial activity were also assessed for VRCT and VRC loaded transethosomal gel (VTEG). Ex-vivo permeation using rat skin depicted a transdermal flux of 22.8 µg/cm²/h with enhanced efficiency up to 4-fold. A two-fold reduction in inhibitory as well as fungicidal concentration was observed against various fungal strains by VRCT and VTEG besides similar results against L-donovani. The development of transethosomal formulation can serve as an efficient drug delivery system through a topical route with enhanced efficacy and better patient compliance.

Tioconazole (TCZ) is a broad-spectrum fungicidal BCS class II drug with reported activity against Candida albicans, dermatophytes, and certain Staphylococci bacteria. We report the use of TCZ-loaded transethosomes (TEs) to overcome the skin’s barrier function. TCZ-loaded TEs were fabricated by using a cold method with slight modification. Box–Behnken composite design was utilized to investigate the effect of independent variables. The fabricated TEs were assessed with various physicochemical characterizations. The optimized formulation of TCZ-loaded TEs was incorporated into gel and evaluated for pH, conductivity, drug content, spreadability, rheology, in vitro permeation, ex vivo permeation, and in vitro and in vivo antifungal activity. The fabricated TCZ-loaded TEs had a % EE of 60.56 to 86.13, with particle sizes ranging from 219.1 to 757.1 nm. The SEM images showed spherically shaped vesicles. The % drug permeation was between 77.01 and 92.03. The kinetic analysis of all release profiles followed Higuchi’s diffusion model. The FTIR, DSC, and XRD analysis showed no significant chemical interactions between the drug and excipients. A significantly higher antifungal activity was observed for TCZ-loaded transethosomal gel in comparison to the control. The in vivo antifungal study on albino rats indicated that TCZ-loaded transethosomal gel showed a comparable therapeutic effect in comparison to the market brand Canesten^®. Molecular docking demonstrated that the TCZ in the TE composition was surrounded by hydrophobic excipients with increased overall hydrophobicity and better permeation. Therefore, TCZ in the form of transethosomal gel can serve as an effective drug delivery system, having the ability to penetrate the skin and overcome the stratum corneum barrier with improved efficacy.

Objective: The current study aimed to provide preliminary insights into potential biopharmaceutical applications of Carica papaya seed extract by evaluating its phytochemical and biological profiles. Furthermore, the study aimed to develop a stable oil‐in‐water (O/W) emulsion for the effective delivery of antioxidant‐rich biologicals for cosmetic purposes. Methods: The hydroethanolic (ethanol 80%: 20% water) extract of C. papaya seeds was prepared via maceration technique. The chemical composition was carried out through preliminary phytochemical screening and estimation of total phenolic contents (TPC) and total flavonoid contents (TFC). The biological profile of the extract was explored using various in‐vitro antioxidant methods. The homogenization procedure was used to create a cream of O/W and various tests were applied to assess the stability of the emulsion. By keeping the emulsion at different storage conditions (8 ± 0.5°C, 25 ± 0.5°C, 40 ± 0.5°C, and 40 ± 0.5°C ± 75% relative humidity [RH]) for a period of 28 days), the physical stability parameters of the emulsion, including pH, viscosity, centrifugation, phase separation, and conductivity, as well as rheological parameters and organoleptic parameters (odor, color, liquefaction, and creaming), were assessed. Results: The preliminary phytochemical screening assay revealed the presence of various plant secondary metabolites including alkaloids, phenolics, flavonoids, tannins, saponins, and quinones. The extract was found to be rich in TPC and TFC. The in vitro antioxidant study gave maximum activity in the DPPH method. The plant extract containing cosmetic cream exhibited remarkable stability during the entire research. Data gathered indicated that no phase separation or liquefaction was seen after the experimental period. Throughout the experimental period, a small variation in the pH and conductivity values of the base and formulation was seen. Conclusion: The findings suggest that the seed extract of C. papaya is a rich source of polyphenols with antioxidant potential and can be a promising alternative for the treatment of various ailments. The stability of emulsion paves the way for its utilization as a carrier for the delivery of 3% C. papaya seed extract and applications in cosmetics products.

Background: Despite extensive research over the decades, cancer therapy is still a great challenge because of the non-specific delivery of chemotherapeutic agents, which could be overcome by limiting the distribution of chemotherapeutic agents toward cancer cells. Objective: To reduce the cytolytic effects against cancer cells, graphene oxide (GO) nanoparticles (NPs) can load anticancer medicines and genetic tools. Methodology: During the current study, folic-acid-conjugated graphene oxide (Fa-GO) hybrid mucoadhesive chitosan (CS)-based hydrogel beads were fabricated through an “ion-gelation process”, which allows for regulated medication release at malignant pH. Results: The fabricated chitosan–alginate (SA-CS) hydrogel beads were examined using surface morphology, optical microscopy, XRD, FTIR, and homogeneity analysis techniques. The size analysis indicated that the size of the Fa-GO was up to 554.2 ± 95.14 nm, whereas the beads were of a micrometer size. The folic acid conjugation was confirmed by NMR. The results showed that the craggy edges of the graphene oxide were successfully encapsulated in a polymeric matrix. The mucoadhesive properties were enhanced with the increase in the CS concentration. The nanohybrid SA-CS beads exhibited good swelling properties, and the drug release was 68.29% at pH 5.6 during a 24 h investigation. The accelerated stability study, according to ICH guidelines, indicated that the hydrogel beads have a shelf-life of more than two years. Conclusions: Based on the achieved results, it can be concluded that this novel gastro-retentive delivery system may be a viable and different way to improve the stomach retention of anticancer agents and enhance their therapeutic effectiveness.

BackgroundThe potential as a depigmenting agent, sun protection, and healthy benefits is indicated by the sun protection factor, radical scavenging, and tyrosinase inhibitory activities of Alpinia galanga (wild). AimsA stable emulgel containing A .galanga (wild) extract is prepared. This emulgel is then characterized by in vitro evaluation and identification of contents by LC-ESI-MS2. In vivo performance is counted in terms of moisturizing, melanin level, erythema, sebum, skin fine pores and large pores analysis, and other related physiological skin parameters. MethodsDPPH radical scavenging activity, total phenolic and flavonoid counts were used to measure the free radical scavenging and tyrosinase inhibitory capability of A .galanga (wild) extract, respectively. LC-ESI-MS2 used for phytochemical analysis. Emulgels synthesize, and their globule size, Ultracentrifugation, pH, and conductivity were all evaluated. Among the developed formulations, the optimal emulgels formulation underwent 90-day stability tests for organoleptic characteristics and rheology at 8 degrees C, 25 degrees C, 40 degrees C, and 40 degrees C + 75% RH (relative humidity). Using sebumeter (R), mexameter (R), and corneometer (R), changes in skin physiological parameters were assessed over the course of 12 weeks in 13 healthy male, Asian volunteers. VisioFace (R) is used for computational analysis of high-resolution pictures to determine the % area, fine pore counts, and large pore counts of the skin. ResultsThe antioxidant, tyrosinase inhibitory potential and counts of total phenolic and flavonoids of A .galanga (wild) extract were impressive (85%, 75%, and 48.0 mg GAE/g and 14.37 mg quercetin/g, respectively). In terms of stability evaluation, globule size (0.7528 +/- 0.192 mu m). Optimized A .galanga (wild) ethanol aqueous (AGEA) extract loaded emulgel was stable in terms of organoleptic and in vitro evaluation. The AGEA formulation significantly reduced the amount of sebum, erythema, fine pore counts, large pore counts, fine pore % area and large pores area percentage while significantly improved the moisture and elasticity of the skin. ConclusionA stable A .galanga (wild) extract loaded emulgel was successfully produced that improved the skin physiological parameters in terms of skin's sebum, erythema, moisturizing, melanin, and pores.