Sphaeranthus indicus L. is a medicinal herb having widespread traditional uses for treating common ailments. The present research work aims to explore the in-depth phytochemical composition and in vitro reactivity of six different polarity solvents (methanol, n-hexane, benzene, chloroform, ethyl acetate, and n-butanol) extracts/fractions of S. indicus flowers. The phytochemical composition was accomplished by determining total bioactive contents, HPLC-PDA polyphenolic quantification, and UHPLC-MS secondary metabolomics. The reactivity of the phenolic compounds was tested through the following biochemical assays: antioxidant (DPPH, ABTS, FRAP, CUPRAC, phosphomolybdenum, and metal chelation) and enzyme inhibition (AChE, BChE, α-glucosidase, α-amylase, urease, and tyrosinase) assays were performed. The methanol extract showed the highest values for phenolic (94.07 mg GAE/g extract) and flavonoid (78.7 mg QE/g extract) contents and was also the most active for α-glucosidase inhibition as well as radical scavenging and reducing power potential. HPLC-PDA analysis quantified rutin, naringenin, chlorogenic acid, 3-hydroxybenzoic acid, gallic acid, and epicatechin in a significant amount. UHPLC-MS analysis of methanol and ethyl acetate extracts revealed the presence of well-known phytocompounds; most of these were phenolic, flavonoid, and glycoside derivatives. The ethyl acetate fraction exhibited the highest inhibition against tyrosinase and urease, while the n-hexane fraction was most active for α-amylase. Moreover, principal component analysis highlighted the positive correlation between bioactive compounds and the tested extracts. Overall, S. indicus flower extracts were found to contain important phytochemicals, hence could be further explored to discover novel bioactive compounds that could be a valid starting point for future pharmaceutical and nutraceuticals applications.
Complex multiple emulsions have an excellent ability to fill large volumes of functional cosmetic agents. This study was aimed to encapsulate large volume of green tea in classical multiple emulsion and to compare its stability with a multiple emulsion without green tea extract. Multiple emulsions were developed using Cetyl dimethicone copolyol as lipophilic emulsifier and classic polysorbate-80 as hydrophilic emulsifier. Multiple emulsions were evaluated for various physicochemical aspects like conductivity, pH, microscopic analysis, rheology and these characteristics were followed for a period of 30 days in different storage conditions. In vitro and in vivo skin protection tests were also performed for both kinds of multiple emulsions i.e. with active (MeA) and without active (MeB). Both formulations showed comparable characteristics regarding various physicochemical characteristics in different storage conditions. Rheological analysis showed that formulations showed pseudo plastic behavior upon continuous shear stress. Results of in vitro and in vivo skin protection data have revealed that the active formulation has comparable skin protection effects to that of control formulation. It was presumed that stable multiple emulsions could be a promising choice for topical application of green tea but multiple emulsions presented in this study need improvement in the formula, concluded on the basis of pH, conductivity and apparent viscosity data.
The SARS COV-2 and its variants are spreading around the world at an alarming speed, due to its higher transmissibility and the conformational changes caused by mutations. The resulting COVID-19 pandemic has imposed severe health consequences on human health. Several countries of the world including Pakistan have studied its genome extensively and provided productive findings. In the current study, the mCSM, DynaMut2, and I-Mutant servers were used to analyze the effect of identified mutations on the structural stability of spike protein however, the molecular docking and simulations approaches were used to evaluate the dynamics of the bonding network between the wild-type and mutant spike proteins with furin. We addressed the mutational modifications that have occurred in the spike protein of SARS-COV-2 that were found in 215 Pakistani's isolates of COVID-19 patients to study the influence of mutations on the stability of the protein and its interaction with the host cell. We found 7 single amino acid substitute mutations in various domains that reside in spike protein. The H49Y, N74K, G181V, and G446V were found in the S1 domain while the D614A, V622F, and Q677H mutations were found in the central helices of the spike protein. Based on the observation, G181V, G446V, D614A, and V622F mutants were found highly destabilizing and responsible for structural perturbation. Protein-protein docking and molecular simulation analysis with that of furin have predicted that all the mutants enhanced the binding efficiency however, the V622F mutant has greatly altered the binding capacity which is further verified by the KD value (7.1 E-14) and therefore may enhance the spike protein cleavage by Furin and increase the rate of infectivity by SARS-CoV-2. On the other hand, the total binding energy for each complex was calculated which revealed -50.57 kcal/mol for the wild type, for G181V -52.69 kcal/mol, for G446V -56.44 kcal/mol, for D614A -59.78 kcal/mol while for V622F the TBE was calculated to be -85.84 kcal/mol. Overall, the current finding shows that these mutations have increased the binding of Furin for spike protein and shows that D614A and V622F have significant effects on the binding and infectivity.
Currently, the use of natural compounds obtained from plants tremendously increased due to their promising therapeutic properties. The aim of this study was to formulate a stable emulgel formulation loaded with Cinnamomum tamala (CT) extract. The antioxidant activity of plant extract was determined by DPPH inhibition assay. The extract was successfully loaded into an emulgels using different concentrations of carbopol-940, liquid paraffin, emulsifying agents and preservatives. Preliminary stability study was performed of 17 CT emulgel formulations at accelerated temperature of 50 °C for 2-months. Organoleptic evaluation, centrifugation, globule size, pH, electrical conductivity and rheological studies were performed for a period of 90-days at different temperature including 8, 25, 40 and 40 °C ±75% RH. The CT extract showed promising antioxidant activity of about 81%. On the other hand, the CT loaded emulgel formulation displayed high physical stability at all tested conditions of temperature and time. However, slight decrease in pH and minimum increase in conductivity was observed at 40 and 40 °C±75% RH. The rheological examination of CT emulgel indicated the flow index values of all the samples kept at different temperatures were less than 1, demonstrated non-newtonian and pseudo-plastic nature of CT emulgel. Taken together, the CT emulgel formulation has been evinced to be an excellent addition in the field of topical formulations.
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. Different ethosomal suspensions of alpha arbutin were prepared by the cold method. Invitro evaluation included zeta potential, droplet size analysis, polydispersity index, entrapment efficiency (EE), scanning electron microscopy (SEM) and Fourier transform infrared (FTIR) spectroscopy. Stability studies of the optimized ethosomal and control gels were performed for three months under different temperature conditions. The optimized ethosomal gel loaded with alpha arbutin was further analyzed on human volunteers for skin benefits by measuring melanin level, moisture content and elasticity. It was concluded that the optimized formulation had a size, zeta potential, polydispersity index and entrapment efficiency of 196.87 nm, -45.140 mV, 0.217 and 93.458343%, respectively. Scanning electron microscopy (SEM) depicted spherical ethosomal vesicles. Stability data was obtained in terms of pH and conductivity. Rheological analysis revealed non-Newtonian flow. The cumulative drug permeated for ethosomal gel was 78.4%. Moreover, encapsulation of alpha arbutin causes significant improvement in skin melanin, moisture content and elasticity. The overall findings suggested that the arbutin-loaded ethosomal formulation was stable and could be a better approach than conventional formulation for cosmeceutical purposes such as for depigmentation and moisturizing effects.
This research aimed to enhance dermal delivery and optimize depigmentation therapy by designing mesoporous silica nanoparticles (MSNs) encapsulating azelaic acid (AZA) within a gel matrix. The MSNs were prepared using the sol-gel method. After subsequent processes, including acid extraction and drug loading, were then elucidated through PDI, size, zeta-potential, entrapment efficiency, nitrogen adsorption assay, FE-SEM, thermogravimetric analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, X-ray diffraction, and tyrosinase inhibition assay, were employed to assess the formulation.
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