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Didymocarpous pedicellata R.Br. (Gesneriaceae), also known as stone flower, is a valuable medicinal plant growing in the subtropical Himalayas (India). It is traditionally used for treating kidney and bladder stones and is the main ingredient of herbal formulations used to treat kidney stones, such as Cystone and Safoof-e-Pathr Phori (SPP). The present study explored the antiurolithiatic effect of Didymocarpous pedicellata leaves (DPL) in urolithiasis caused by ethylene glycol in Wistar male rats. The EG-induced urolithiasis group exhibited significantly higher (P

Onychomycosis, the most prevailing affliction of the nail, accounts for approximately 90% of the toenail infection worldwide. Owing to this infection, the affected patients experience reduced quality of their life as its awful appearance undermines their daily activities and social interactions. Onychomycosis is notoriously strenuous to cure. Systemic therapy, though effective, possess severe complication of toxicities, contra-indication, and drug-drug interaction. Albeit topical therapy is favorable to its localized effect, its potency relates to the effective concentration of the antifungal drugs achieved at the infection site. An approach to accomplish this goal would be acquiring benefits from the terpenes as penetration enhancers from natural sources. This investigation aimed to study the effectiveness of six terpenes, namely safranal, lavandulol, rose oxide, 3-methyl-2-butene-1-ol, linalool, and limonene, as potential penetration enhancers for improved nail permeation of fluconazole through the human nail.Ex vivo permeation experiments were carried out by soaking the nail clippings of human volunteers in control and working solutions containing fluconazole (5 mg/ml) per se and fluconazole (5 mg/ml) with 6% of each terpene, including safranal, lavandulol, rose oxide, 3-methyl-2-butene-1-ol, linalool, and limonene, respectively, for 48 h. The amount of fluconazole in nail clippings was quantified using an HPLC method.Statistical analysis showed that fluconazole transungual permeation was influenced by the studied terpenes in the following order: safranallavandulol acetatelimonenerose oxide (p-value0.05) while the other terpenes showed no significant difference with the control group and safranal represents as the most effective permeation enhancer for the transungual delivery of fluconazole.It is concluded that the safranal can be successfully used as a safe and potential permeation enhancer to enhance the transungual delivery of fluconazole for the treatment of onychomycosis.

Monascus purpureus copiously yields beneficial secondary metabolites , including Monascus pigments, which are broadly used as food additives, as a nitrite substitute in meat products, and as a colorant in the food industry. Monascus yellow pigments (monascin and ankaflavin) have shown potential antidiabetic, antibacterial, anti-inflammatory, antidepressant, antibiotic, anticancer, and antiobesity activities. Cosmetic and textile industries are other areas where it has established its potential as a dye. This paper reviews the production methods of Monascus yellow pigments, biosynthesis of Monascus pigments from M. purpureus, factors affecting yellow pigment production during fermentation, and the pharmacological properties of monascin and ankaflavin.

β-Carotene is the most treasured provitamin A carotenoid molecule exhibiting antioxidant and coloring properties and significant applications in the food, pharmaceutical, and nutraceutical industries. β-Carotene has many biological functions within the human body; however, it is not synthesized within the human body, so its requirements are fulfilled through food and pharmaceuticals. Its manufacturing via chemical synthesis or extraction from plants offers low yields with excessive manufacturing expenses, which attracted the researchers toward microbial production of β-carotene. This alternative provides higher yield and low expenses and thus is more economical. Phaffia rhodozyma is a basidiomycetous yeast that is utilized to prevent cardiovascular diseases and cancer and to enhance immunity and antiaging in people. This paper reviews the methods of production of β-carotene, biosynthesis of β-carotene fromP. rhodozyma, factors affecting β-carotene production during fermentation, and pharmacological properties of β-carotene.

The present study delineates the development of a novel rugged and sensitive stability indicating risk-based HPLC method for the concurrent estimation of methotrexate (MTX) and baicalin (BCL) in dual drug-loaded-nanopharmaceuticals based on an analytical QbD approach. Preliminary screening trials along with systemic risk analysis were performed, endeavouring to explicate the critical method attributes namely pH, % orthophosphoric acid content and % acetonitrile content that influences critical quality attributes. Box-Behnken design (BBD) was utilized for the optimization of the tailing factor as response for methotrexate and baicalin in short run time. The chromatographic conditions were optimized by performing 17 experimental runs acquired from design expert software. The chromatographic conditions after the analysis of optimized zone within the confines of design space, were chosen as mobile phase water: acetonitrile adjusted to pH 3.0 with 0.05% orthophosphoric acid (60:40, %v/v), flow rate 1.0 ml/min using an analytical column C

The current research work describes the development of a rapid HPLC method for the concurrent detection of pregabalin and piperine in dual drug-loaded nanoformulations. The primary goal was to recognize the chromatographic conditions wherein propitious segregation of the integrants with quality peaks can be attained. An attempt to expound the target analytical profile was made to accomplish this goal, and critical method attributes (CMAs), viz. percentage acetonitrile content, injection volume and pH, which affect critical quality attributes (CQAs), were identified using systemic risk analysis. Box-Behnken design was employed to develop a relationship between CMAs and CQAs, which engenders an analytical design space. Efficient chromatographic separation for pregabalin and piperine was attained using an analytical C

Context Traditionally, Inula racemosa Hook. f. (Asteraceae) has been reported to be effective in cancer treatment which motivated the authors to explore the plant for novel anticancer compounds. Objective To isolate and characterize new cytotoxic phytoconstituents from I. racemosa roots. Materials and methods The column chromatography of I. racemosa ethyl acetate extract furnished a novel sesquiterpene lactone whose structure was established by NMR (1D/2D), ES-MS and its cytotoxic properties were assessed on HeLa, MDAMB-231, and A549 cell lines using MTT and LDH (lactate dehydrogenase) assays. Further, morphological changes were analyzed by flow cytometry, mitochondrial membrane potential, AO-EtBr dual staining, and comet assay. Molecular docking and simulation were performed using Glide and Desmond softwares, respectively, to validate the mechanism of action. Results The isolated compound was identified as racemolactone I (compound 1). Amongst the cell lines tested, considerable changes were observed in HeLa cells. Compound 1 (IC50 = 0.9 µg/mL) significantly decreased cell viability (82%) concomitantly with high LDH release (76%) at 15 µg/mL. Diverse morphological alterations along with significant increase (9.23%) in apoptotic cells and decrease in viable cells were observed. AO-EtBr dual staining also confirmed the presence of 20% apoptotic cells. A gradual decrease in mitochondrial membrane potential was observed. HeLa cells showed significantly increased comet tail length (48.4 µm), indicating broken DNA strands. In silico studies exhibited that compound 1 binds to the active site of Polo-like kinase-1 and forms a stable complex. Conclusions Racemolactone I was identified as potential anticancer agent, which can further be confirmed by in vivo investigations.

The present study delineates the preparation of piperine-loaded spanlastics (PIP-SPL) to improve piperine (PIP) solubility, bioavailability, and permeation through nasal mucosa for intranasal delivery. PIP-SPL was formulated using the thin-film hydration method and optimization was performed using Box–Behnken design (BBD). PIP-SPL optimized formulation (PIP-SPLopt) was characterized for polydispersity index (PDI), vesicle size, entrapment efficiency, zeta potential, and in vitro PIP release. For further evaluation, blood–brain distribution study, transmission electron microscopy (TEM), nasal permeation study, and confocal scanning laser microscopy (CLSM) were performed withal. The PIP-SPLopt presented spherical and sealed shape vesicles with a small vesicle size of 152.4 nm, entrapment efficiency of 72.93%, PDI of 0.1118, and in vitro release of 82.32%. The CLSM study unveiled that the developed formulation has greater permeation of PIP across the nasal mucosa in comparison with the PIP suspension. The blood–brain distribution study demonstrated higher Cmax and AUC0–24h of PIP-SPL via the intranasal route in comparison to PIP-SPL via oral administration. The in vivo study revealed that the PIP-SPL has good antiepileptic potential in comparison with the standard diazepam, which was evinced by seizure activity, neuromuscular coordination by rotarod test, biochemical estimation of oxidative stress markers, and histopathological studies. Furthermore, nasal toxicity study confirm that the developed PIP-SPL formulation is safer for intranasal application. The current investigation corroborated that the prepared spanlastic vesicle formulation is a treasured carrier for the PIP intranasal delivery for the management of epilepsy.

In the present work, a simple, rapid, reliable and accessible high-performance thin-layer chromatography (HPTLC) technique has been established for the concurrent quantification of plumbagin. The well-known medicinal plant, Plumbago zeylanica L., has been traditionally used to treat a variety of ailments in India and other countries. Chromatographic separation was conceded on pre-coated silica gel plates F254. The apposite mobile phase toluene‒acetic acid (9.0:0.5, V/V) was developed to expand the plates which separated components according to the marker compounds. Densitometric scanning was performed by CAMAG Scanner V and measured at wavelength 272 nm. The marker compounds were practically resolved with RF 0.44 ± 0.02 for plumbagin. Further, the antioxidant potential of the methanolic extract of P. zeylanica was also assessed with 1,1-diphenyl-2-picrylhydrazyl (DPPH) by using an ultraviolet (UV) spectrophotometer. The percentage inhibition of free radical was found to be 76.5%. The developed HPTLC method was validated for accuracy, linearity, precision and specificity. The extract has revealed considerable antioxidant activity. The reported existing phenolic and flavonoids compounds are responsible for the antioxidant activity of the plant extract as reported in the literature.

Herbal medicines therapy is appreciated by many research works because herbal drugs have relatively high therapeutic window, lower side effects and more cost effective. Guggulipid is an ethyl acetate extract of resin known as guggul from the tree Commiphora wightii / mukul (Arn.) Bhandari. Chemical analysis revealed that the compounds responsible for the major activities of gum guggul are the isomers E- and Z-guggulsterone. Guggul has been used for thousands of years in the treatment of arthritis, inflammation, obesity, cardiac protection, anti-ulcer, anti-epileptic and disorders of lipid metabolism. This review is an assortment of available information reported on its chemical, pharmacological and toxicological properties in various research studies. The available therapeutic properties of guggulipid make it suitable natural product for the treatment of various disorders like inflammation, pain, wounds, liver disorder and Acne etc. Graphical Abstract Graphical Abstract.

Background: A stability indicating high-performance thin layer chromatography (HPTLC) method was developed for the evaluation of fisetin (FIS) in active pharmaceutical ingredient (API) and marketed capsule formulation in accordance with the ICH guidelines. Methods: The mobile phase combination toluene: ethyl acetate: formic acid: methanol (3: 5.5: 1: 0.5 v/v/v/v) was optimized with the aid of AQbD approach. The absorbance mode at 254 nm was chosen for densitometric analysis as it gives a compact spot of FIS at Rf value of 0.74. Results: The R2 value obtained from the linear regression equation of calibration plots made by taking the spot in the concentration range of 100-1400 ng/spot was found to be 0.9993. The observed LOD and LOQ value was found to be 29.8 ng/spot and 98.5 ng/spot, respectively. The exposure of FIS to various stress conditions revealed the fact that the drug is stable in photochemical and dry heat stress conditions without any degradation. The drug-exposed to acidic, alkaline and oxidative stress was found to be degraded into different degradation products with the highest degradation was found in alkaline stress. All degradation products were observed to be fairly separated from well-resolved parent peak of FIS. Conclusion: The developed HPTLC method have shown well-resolved peaks and also shown good recovery in the compound FIS as well as FIS formulation.

The aim of the present study was to develop and characterize karanjin-loaded ethosomes-based gel formulation for enhanced topical delivery and effective therapy of skin acne. Karanjin-loaded ethosomes (K-ETH) presented a nanometric size of 140.87 ± 2.35 nm, entrapment of 71.41 ± 2.74% and enhanced permeation with 1.9 times increase in the flux and 2.4 times higher skin deposition compared to the hydro-ethanolic solution of karanjin. The DSC analysis confirmed successful entrapment of the karanjin within the ethosomes. The developed ethosomes were incorporated in the carbopol gel for adequate application on the skin surface. The ethosomal gel (K-EGF) also exhibited greater penetration in the rat skin as revealed by CLSM. The optimized K-EGF formulation was non-irritant to the skin as evident by Draize score test and histopathological examination. The highest zone of inhibition, 30.0 ± 1.52 mm and 36.22 ± 0.57 mm was produced by the K-EGF against Propionibacterium acnes and Staphylococcus epidermidis, respectively, indicating substantial antibacterial properties of the K-EGF. DPPH assay indicated its potent antioxidant effects. Substantial anti-inflammatory effects in the carrageenan-induced edema in the rat paw were evident with inhibition of rat paw edema by 66.66% and 70.37% upon application of K-EGF and standard anti-inflammatory agent, respectively. Anti-acne effects were also evident with K-EGF treatment with significant decrease in number and size of sebaceous gland units in dermis. Overall, the above findings vouch for a therapeutic opportunity to improve topical delivery of karanjin in acne treatment employing ethosomal gels as the promising carrier system. SUPPLEMENTARY INFORMATION: The online version contains supplementary material available at 10.1007/s13205-021-02978-3.

Fisetin loaded binary ethosomes were prepared and optimized using Box-Behnken design for dermal application to alleviate skin cancer. The prepared formulations were evaluated for vesicle size, entrapment efficiency and flux of fisetin. Additionally, the optimized formulation was further evaluated by transmission electron microscopy, confocal laser microscopy, vesicles-skin interaction, dermatokinetic study and DPPH (2, 2-diphenyl-1-picryl-hydrazyl) assay. The in vivo study was carried out for the evaluation of tumor incidence, pro-inflammatory cytokines such as TNF-α and IL-1α, lipid peroxidation values, glutathione content and catalase activity in mice. The optimized binary ethosomes formulation presented sealed unilamellar shaped vesicles, with vesicles size, entrapment efficiency and flux of 99.89 ± 3.24 nm, 89.23 ± 2.13% and 1.01 ± 0.03 µg/cm2/h respectively. The confocal images of rat skin clearly illustrated the deeper penetration of rhodamine B loaded binary ethosomes formulation. Further, the binary ethosomes gel treated rat skin showed substantial increase in CSkin max and AUC0-8 in comparison to rat skin treated with conventional gel. In vivo study revealed that the mice pre-treated with fisetin binary ethosomes gel caused marked decrease in the levels of TNF-α and IL-1α as compared to the mice exposed to UV only. Further the binary ethosomes gel treated mice group had demonstrated less percentage of tumour incidences (49%) as compared to mice treated with UV only (96% tumour incidence). The novelty of the work lies in successful optimization of formulation using Box-Behnken design and characterization of binary ethosomes carrier of fisetin and demonstration of improved dermal delivery of the same. The overall data suggest that the fisetin loaded binary ethosomes formulation is a potential dermal delivery system for the management of skin cancer.

Ganoderic acid has been known as a key bioactive constituent in Ganoderma lucidum, commonly used for preventing and treating hepatopathy of various etiologies. This study was designed to investigate the hepatoprotective and antioxidant activity of ganoderic acid loaded solid lipid nanoparticles in d -galactosamine induced hepatotoxicity in male Wistar rats. Ganoderic acid loaded solid lipid nanoparticles was prepared by solvent injection technique and prepared formulation was characterized for various parameters and final formulation evaluated for its hepatoprotective study in Wistar rats. The prepared optimized formulation presented particle size of 122.7 ± 8.6 nm with polydispersity index of 0.27 ± 0.03 and zeta potential of −18 ± 1.4 mV. The drug loading, entrapment efficiency and nanoparticle yield were found to be 21.6 ± 1.23%, 70.16 ± 3.21% and 60.5 ± 2.75%, respectively. In vitro release study of ganoderic acid from nanoparticles at pH 7.4 exhibited biphasic release pattern with an initial burst release followed by a sustained release. Treatment of rats with prepared formulation significantly restored the levels of serum hepatic markers and antioxidant enzymes as compared to free ganoderic acid in d -galactosamine induced hepatotoxicity in rats. Histopathological examination also supported a marked hepatoprotective effect of prepared formulation. In conclusion, nano-formulation of ganoderic acid has significantly attenuated markers of hepatic damage compared to free ganoderic acid and may represent a potential hepatoprotective nano-formulation for amelioration of d -galactosamine induced liver injury.

The current study involved the development and optimization of ethosomes formulation for topical delivery of thymoquinone for improved therapy in skin acne. Formulation was optimized based on vesicles size, entrapment efficiency and flux by applying “3-factor 3-level Box-Behnken design”. The optimized formulation was further evaluated for “anti-microbial, anti-inflammatory, anti-acne and skin irritation activity”. The optimized formulation had shown the vesicles size of 105.2 ± 8.0 nm, entrapment efficiency of 85.30 ± 6.30% and flux of 65.40 ± 7.6 μg/cm2/h. The penetration depth of rhodamine loaded ethosomes across rat skin was traced with confocal laser microscopy and it was noted that the plain rhodamine solution (control) remained confined to few micrometers (14.4 μm) depth only into rat skin, while the rhodamine loaded ethosomes formulation penetrate deeper up to 103.5 μm depth into rat skin. Antimicrobial study exhibited that the marketed allopathic gel, prepared ethosomes formulation, and marketed herbal gel have presented zone of inhibition of 29.0 ± 1.00 mm, 20.33 ± 0.57 mm, and 15.00 ± 1.73 mm respectively against S. Epidermidis. The in vivo anti-inflammatory activity demonstrated that the application of prepared ethosomes and marketed diclofenac gel formulation resulted in an inhibition of rat paw edema by 80.74% and 84.61% respectively in Wistar rats. Anti-acne study demonstrated that the developed ethosomes formulation had shown considerable effect on sebaceous glands units by reducing its glands number and size. Further skin irritation study revealed that the developed formulation was safe, less irritant and well tolerable formulation for topical delivery. It was concluded that the developed thymoquinone loaded ethosomes formulation can be used as an effective treatment option for acne vulgaris and various skin disorders.

Objective: The main objective of the current study was to perform pharmacognostical, physiochemical analysis and in vitro antioxidant activity of Tamarindus indica Linn. (Family: Fabaceae) fruit. Materials and Methods: The present study deals with pharmacognostical characters as identification parameters of the fruit, which were subjected to macro- and microscopical studies. Physiochemical analysis was performed as per World Health Organization–recommended parameters. Toxicological parameters such as heavy metals, aflatoxins, and pesticide residue and presence of microbial count were analyzed. This study also deals with the thin layer chromatography/high performance thin layer chromatography fingerprinting and antioxidant activity. Results: The microscopy study revealed the presence of epidermis, vascular bundles, parenchyma cells, mucilage fiber, starch grain, and nonlignified fibers. Physiochemical parameters such as loss on drying, moisture content, ash value, and extractive value were also determined. Heavy metal, aflatoxin, total microbial load, and pesticide residues were found to be variable but under the permissible limits. Conclusion: It is critical to analyze these parameters in each crude herbal drug before further processing to ensure their safety and efficacy for better approval at the international podium. This study revealed precise identification for the meticulous crude drug which will be valuable in detection and manage to adulterations of the raw material.

To select the best organic solvent and ideal extraction technique for isolation and quantitative estimation of ursolic acid from the leaves of Lantana camara (L. camara) by high performance thin layer chromatography (HPTLC). A sensitive, fast and reproducible HPTLC method was developed and validated for estimation of ursolic acid from the leaves of L. camara. Different leaves extracts of L. camara were prepared through different extraction methods (maceration, reflux, soxhlet and ultrasound assisted extraction technique) by using four different solvents of varying polarity such as ethanol, methanol, acetone and chloroform. The maximum % extract yield was obtained in methanol, so we select methonolic extract for HPTLC evaluation. The calibration plot of standard ursolic acid with respect to peak area showed an tremendous linear relationship in the concentration range of 1000–4000 ng/spot with a correlation coefficient r2 = 0.994. The separation was completed on precoated silica gel aluminium plates 60F254 using Toluene: Acetone: Formic Acid (7.8:2.2:0.15) as mobile phase which gives a compact spot of ursolic acid (Rf value 0.49). For the proposed method (Limit of Detection) LOD (561.85 ng/spot), (Limit of Quantification) LOQ (1702.58 ng/spt), recovery of drug (99.02–101.43%) and precision (0.4303–2.1576% RSD) was found to be satisfactory. It can be concluded on the basis of HPTLC results that methanol was found to be the best solvent and Soxhlet was found to be an ideal extraction technique for the isolation of ursolic acid from L. camara leaves for routine analysis. Keywords: Lantana camara, Ursolic acid, HPTLC, Extraction techniques

Solanum nigrum Linn. (Family: solanaceae), has medicinal values, commonly exploited for its active constituents which are of high pharmaceutical importance. The plant contains different type of natural compounds, and one of most important glycoalkaloid in S. nigrum is solasodine. Nodal segment of S. nigrum was cultured on MS media added with several concentrations of 2, 4-dichlorophenoxy acetic acid (2, 4- D) (0.5ppm –2ppm) for callus induction and development. For shoot induction, MS medium complemented with different dilutions of 6- benzyl adenine (6- BA) (0.5ppm–2ppm) was used. A novel, rapid, and simple high performance thin layer chromatographic method for quantitative estimation of triterpenoid glycoalkaloid. Solasodine was spotted on silica gel 60F254 TLC plate using chloroform: methanol (8.75: 1.25; v/v) as mobile phase. Anisaldehyde-sulfuric acid in methanol used as derivatizing reagent and quantified by densitometric study at 366 nm. This scheme was found to give a sharp and compact spot for the standard drug (Rf = 0.67 ± 0.04). The linearity of this method was found to be a range of 100-1000 ng per spot with LOD and LOQ of 23.78 ng per spot and 67.09 ng per spot; respectively. This method has shown recoveries of solasodine in the range from 98.23% -100.88 %, with low intra and inter-day % RSD. Statistical investigation of the data presented that the method is selective, accurate, precise and reproducible for the study of solasodine. The established and developed HPTLC method would be a significant parameter for the analysis of quality control method of herbal drugs and formulations.

Safoof-e-Pathar phori (SPP) is an Unani poly-herbomineral formulation, which has for a long time been used as a medicine due to its antiurolithiatic activity, as per the Unani Pharmacopoeia. This powder formulation is prepared using six different plant/mineral constituents. In this study, we explored the antiurolithiatic and antioxidant potentials of SPP (at 700 and 1,000 mg/kg) in albino Wistar rats with urolithiasis induced by 0.75% ethylene glycol (EG) and 1% ammonium chloride (AC). Long-term oral toxicity studies were performed according to the Organization for Economic Co-operation and Development (OECD) guidelines for 90 days at an oral dose of 700 mg/kg of SPP. The EG urolithiatic toxicant group had significantly higher levels of urinary calcium, serum creatinine, blood urea, and tissue lipid peroxidation and significantly (p< 0.001 vs control) lower levels of urinary sodium and potassium than the normal control group. Histopathological examination revealed the presence of refractile crystals in the tubular epithelial cell and damage to proximal tubular epithelium in the toxicant group but not in the SPP treatment groups. Treatment of SPP at 700 and 1,000 mg/kg significantly (p< 0.001 vs toxicant) lowered urinary calcium, serum creatinine, blood urea, and lipid peroxidation in urolithiatic rats, 21 days after induction of urolithiasis compared to the toxicant group. A long-term oral toxicity study revealed the normal growth of animals without any significant change in hematological, hepatic, and renal parameters; there was no evidence of abnormal histology of the heart, kidney, liver, spleen, or stomach tissues. These results suggest the usefulness of SPP as an antiurolithiatic and an antioxidant agent, and long-term daily oral consumption of SPP was found to be safe in albino Wistar rats for up to 3 months. Thus, SPP may be safe for clinical use as an antiurolithiatic formulation.

A new dimeric sesquiterpene named disesquicin (compound 1) was isolated from Inula racemosa roots by normal-phase MPLC (Medium Pressure Liquid Chromatography), and its structure was established by using extensive spectral analysis. Compound 1, when tested on different human cancer cell lines, showed marked cytotoxic activity (IC50 (&micro, g/mL): 5.99 (MDA-MB), 9.10 (HeLa), and 12.47 (A549)). Docking study revealed that it binds at the catalytic domain of PLK-1 and interacts with catalytic site residues Leu59, Gly60, Lys61, Gly62, Cys67, Ala80, Lys82, Leu130, Arg136, Ser137, Leu139, Glu140, Lys178, Gly180, Asn181, Phe183, and Asp194. The binding of compound 1 to PLK-1 is spontaneous in nature as evident by a free energy of&mdash, 8.930 kcal mol&minus, 1, corresponding to a binding affinity of 3.54 &times, 106 M&minus, 1. Results showed that compound 1 exhibited cytotoxic potential that was further confirmed by in vivo investigations.