Cedrus deodara: In vitro antileishmanial efficacy & immumomodulatory activity.

BACKGROUND & OBJECTIVES: The existing antileishmanial drugs for complete cure of visceral leishmaniasis (kala-azar) are limited. The available drugs are either toxic or less effective leading to disease relapse or conversion to post-kala-azar dermal leishmaniasis. Several herbal extracts have been shown to have antileishmanial activity, but a herbal drug may not always be safe. In the present study, the extract of Cedrus deodara leaves has been standardized and tested for immunomodulatory antileishmanial activities. METHODS: The extracts of C. deodara leaves with different solvents such as benzene, chloroform, ethyl acetate and methanol were made by soxhlation process. Solvents were removed under reduced pressure and temperature using rotary evaporator. The antileishmanial bioassay test was performed with in vitro maintained parasites. Immunomodulatory activity of different extracts was tested by flow cytometry. Standardization of the effective fraction was performed with Linalool as a marker compound through reverse-phase high-performance liquid chromatography. RESULTS: The extract with the use of benzene solvent showed strong antileishmanial activities within a dose 25-200 µg/ml culture with non-significant haemolytic activities and significant immunomodulant activities against the host cells. Linalool was found to be 1.29 per cent in the effective extract of C. deodara. INTERPRETATION & CONCLUSIONS: The antileishmanial activity of C. deodara, as assessed by bioassay testing on. LEISHMANIA DONOVANI: parasites and immunomodulatory effect of benzene extract of leaves on host cells indicated that it might be a potential new safe therapeutic target to cure the visceral leishmaniasis.

Safety assessment of selected medicinal food plants used in Ayurveda through CYP450 enzyme inhibition study.

BACKGROUND: Andrographis paniculata, Bacopa monnieri and Centella asiatica are mentioned in Ayurveda for the management of neurodegenerative disorders. These plants and their phytomolecules, such as andrographolide, bacoside A and asiaticoside, were studied for their inhibition potential on pooled CYP450 as well as human CYP3A4, CYP2D6, CYP2C9 and CYP1A2 by CYP-CO complex assay and fluorogenic assay respectively followed by IC50 determination. Quantification of bioactive compounds present in the extracts was done by RP-HPLC. Heavy metal content in the selected medicinal plants was determined by atomic absorption spectroscopy. RESULT: CYP-CO complex assay indicated significantly less inhibition potential than standard inhibitor (P < 0.05 and above). A. paniculata showed highest inhibitory activity against CYP3A4 and CYP2D6 (IC50 = 63.06 ± 1.35 µg mL-1 ; 88.80 ± 3.32 µg mL-1 ), whereas C. asiatica and B. monnieri showed least inhibitory activity against CYP1A2 (IC50 = 288.83 ± 1.61 µg mL-1 ) and CYP2C9 (184.68 ± 3.79 µg mL-1 ), respectively. In all cases the extract showed higher inhibition than the single bioactive compounds. The heavy metals content in the plant extracts were within the permissible limits. CONCLUSION: The findings suggested that selected food plants and bioactive compounds contributed negligible interaction potential with CYP isozymes and may not possess any harmful effect with regard to their therapeutic application. © 2016 Society of Chemical Industry.

Essential Oils of Some Potential Medicinal Plants and Their Wound Healing Activities.

The wound has been recognised as a deep cut or tearing of the epidermis, which is also referred to as trauma and harm to the body tissues. Healing of wounds requires a coordinated series of cellular processes, including cell attraction, proliferation, differentiation, and angiogenesis. These processes involve interactions between various cells, such as macrophages, endothelial cells, keratinocytes, fibroblasts, growth hormones, and proteases. The outcome of wounds can be fatal if not treated properly, resulting in chronic wounds, chronic pain, and even death. Wound healing is replacing missing tissue with tissue repairs and regeneration. Some local variables are the presence of tissue maceration, foreign objects, biofilm, hypoxia, ischemia, and wound infection. Sustained growth factor delivery, siRNA delivery, micro-RNA targeting, and stem cell therapy are all emerging possible therapeutic approaches for wound healing. Traditional approaches, such as Ayurveda, Siddha, and Unani medicines, are also being used for treatment. The therapeutic application of nanoformulations in wound infections has shown various beneficial effects. Several herbal medicines, especially essential oils have shown potential wound healing activities, such as lavender, tea tree, sesame, olive, etc. Various nanoparticles and their nanoformulations have been explored in wound healing therapy. The present review article highlights several aspects of essential oils for wound healing activity through a novel drug delivery system. Further, some patents on wound healing through herbal medicine have been listed.

Liposome Based Drug Delivery for the Management of Psoriasis - A Comprehensive Review.

Psoriasis has been considered as a chronic inflammatory skin disease which leads to the dysfunction of immune systems. According to the World Psoriasis Day consortium, psoriasis affects around 125 million individuals globally or about 2% to 3% of the overall population. Most of the conventional drug delivery systems primarily attempt to relieve symptoms of psoriasis and are ineffective in providing targeted action and higher bioavailability because of the drug's short half-life and instability, as well as they lack safety and efficacy. The shortcomings of conventional drug delivery systems give rise to the development of novel drug delivery systems which includes liposomes, transferosomes, ethosomes, niosomes, emulsomes, dendrimers, hydrogel, nanoparticles, etc. These novel formulations may enhance the therapeutic effects by changing physiological and pharmacokinetic parameters. Several research reports suggest that these novel drug delivery systems may enhance therapeutic effects which can be used as a promising approach for the treatment of psoriasis. The liposomes based drug delivery system have been considered as most promising vehicles for enhancing therapeutic potentials of drugs into or through the skin upon topical application. Liposomes have small unilamellar vesicles which may enhance the penetration ability through stratum corneum layer of skin. Therefore, present review article highlights on the different aspects of the liposomes as potential drug delivery system for the treatment of psoriasis.

A Comprehensive Review on Nanomedicine: Promising Approach for Treatment of Brain Tumor through Intranasal Administration.

Brain tumors have become one of the deadliest cancers; however, their treatment is still limited by conventional approaches. Brain tumors, among other CNS diseases, are the most lethal form of cancer due to ineffective diagnosis and profiling. The major limiting factor in treating brain tumors is the blood-brain barrier (BBB), and the required therapeutic concentration is not achieved. Hence, most drugs are prescribed at higher doses, which have several unwanted side effects. Nanotechnology has emerged as an interesting and promising new approach for treating neurological disorders, including brain tumors, with the potential to overcome concerns related to traditional therapeutic approaches. Moreover, biomimetic nanomaterials have been introduced to successfully cross the blood-brain barrier and be consumed by deep skin cancer for imaging brain tumors using multimodal functional nanostructures for more specific and reliable medical assessment. These nanomedicines can address several challenges by enhancing the bioavailability of therapeutics through controlled pharmacokinetics and pharmacodynamics. Further nasal drug delivery has been considered as an alternative approach for the brain's targeting for the treatment of several CNS diseases. A drug can be directly delivered to the brain by bypassing the BBB through intranasal administration. This review discusses intranasal nanomedicine-based therapies for brain tumor targeting, which can be explored from different perspectives.

Comprehensive Review on Phytoconstituents-based Nanomedicine for the Treatment of Atopic Dermatitis.

Atopic dermatitis (AD) is known as a chronic disease characterized by eczematous and pruritus skin lesions. The pathology behind atopic dermatitis etiology is loss of epidermal barrier, which prevents the production of protein filaggrin that can induce T-cell infiltration and inflammation. Treatment of AD is majorly based on limiting skin repair as well as reducing inflammation and itching. There are several remedies available for the treatment of AD, such as Janus kinase and calcineurin inhibitors, topical corticosteroids, and phosphodiesterase-4 inhibitors. The conventional formulations in the market have limited safety and efficacy. Hence, effective treatment of atopic dermatitis requires the development of novel, efficacious, reliable, and specific therapies. Recent research data have revealed that some naturally occurring medicinal plants have potential applications in the management of AD through different mechanisms. The nanotechnology-based therapeutics have gained a lot of attention in the last decade for the improvement in the activity of drugs having low absorption due to poor solubility, thus leading to lesser bioavailability. Therapies based on nanotechnology can be an effective way to overcome these obstacles. Due to their effective propensity to provide better drug diffusion and bioavailability as well as drug targeting potential at the desired site of action, these approaches may have decreased adverse drug effects, better penetration, and enhanced therapeutic efficacy. Hence, this review highlights the potential of phytoconstituents-based novel formulations for the treatment of atopic dermatitis. Furthermore, recent patents on therapeutic approaches to atopic dermatitis have also been briefly described.

Recent Developments in Drug Targets and Combination Therapy for the Clinical Management of Hypertension.

Raised blood pressure is the most common complication worldwide that may lead to atherosclerosis and ischemic heart disease. Unhealthy lifestyles, smoking, alcohol consumption, junk food, and genetic disorders are some of the causes of hypertension. To treat this condition, numerous antihypertensive medications are available, either alone or in combination, that work via various mechanisms of action. Combinational therapy provides a certain advantage over monotherapy in the sense that it acts in multi mechanism mode and minimal drug amount is required to elicit the desired therapeutic effect. Such therapy is given to patients with systolic blood pressure greater than 20 mmHg and/or diastolic blood pressure exceeding 10 mmHg beyond the normal range, as well as those suffering from severe cardiovascular disease. The selection of antihypertensive medications, such as calcium channel blockers, angiotensin-converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and low-dose diuretics, hinges on their ability to manage blood pressure effectively and reduce cardiovascular disease risks. This review provides insights into the diverse monotherapy and combination therapy approaches used for elevated blood pressure management. In addition, it offers an analysis of combination therapy versus monotherapy and discusses the current status of these therapies, from researchbased findings to clinical trials.

Recent Updates on the Development of Therapeutics for the Targeted Treatment of Alzheimer's Disease.

Alzheimer's disease (AD) is a complicated, multifaceted, irreversible, and incurable neurotoxic old age illness. Although NMDA (N-methyl D-aspartate)-receptor antagonists, cholinesterase repressors, and their pairings have been approved for the treatment, they are useful for short symptomatic relief. Researchers throughout the globe have been constantly working to uncover the therapy of Alzheimer's disease as new candidates must be determined, and newer treatment medicines must be developed. The aim of this review is to address recent advances in medication research along with new Alzheimer's disease therapy for diverse targets. Information was gathered utilizing a variety of internet resources as well as websites, such as ALZFORUM (alzforum.org) and clinicaltrials.gov. In contrast to other domains, the proposed medicines target amyloids (secretases, A42 generation, neuroinflammation, amyloid precipitation, and immunization), tau proteins (tau phosphorylation/aggregation and immunotherapy), and amyloid deposition. Despite tremendous advancement in our understanding of the underlying pathophysiology of Alzheimer's disease, the FDA (Food and Drug Administration) only approved aducanumab for diagnosis and treatment in 2003. Hence, novel treatment tactics are needed to find and develop therapeutic medicines to combat Alzheimer's disease.

Pharmaceutical and Pharmacokinetic Aspects of Nanoformulation Based Drug Delivery Systems for Anti-cancer Drugs.

Many nanodrug delivery systems used with various routes of administration have been developed recently. These may be dendrimers, nanocrystals, emulsions, liposomes, solid lipid nanoparticles, micelles, or polymeric nanoparticles. The nanodrug delivery systems may improve effectiveness, safety, physicochemical qualities, and pharmacokinetic/pharmacodynamic profile. Functionalized nanodrug delivery systems can increase the half-life, improve the bioavailability of orally administered pharmaceuticals, and target tissue distribution. By decreasing the number of dosage intervals required, increasing the magnitude of the intended pharmacological effects, and decreasing the severity of undesirable systemic side effects, nanodrug systems show promise for improving treatment adherence and clinical results. Nanodrugs have been demonstrated to exhibit cytotoxicity, oxidative stress, inflammation, and genotoxicity in vitro and in vivo; however, this attention has recently been refocused on their potentially harmful potential owing to their beneficial pharmacokinetic features for the treatment of cancer. Researchers require a more profound knowledge of the pharmacokinetic and safety aspects of nanodrugs and the limits of each administration route to continue creating safe and efficacious nanodrugs with high therapeutic potential. The benefits and risks associated with pharmacokinetics have been highlighted in this article, which describes the current state of nanodrug system development.

Herbal Medicines to Fight Against COVID-19: New Battle with an Old Weapon.

The world population has suffered as a result of the COVID-19 pandemic. The disease has become life-threatening in a very short time, harming citizens and the economic systems globally. The novel virus SARS-CoV-2 has been known as the causative agent of COVID-19. The SARS-CoV-2 is a single-stranded RNA virus having ~30 kb genomic components, which are 70% identical to SARS-CoV. The main process of the pathophysiology of COVID-19 has been associated with the interaction of a novel coronavirus with host cell receptor, angiotensin-converting enzyme-2 (ACE 2), by fusion. Therapeutic agents having serine protease inhibitors and ACE-2 blockers may be explored for the treatment by inhibiting the viral target such as Mpro, RdRp, PLpro, and helicase. Herbal medicine has a wide array of chemical entities with potential health benefits, including antiviral activity, which may be explored as an alternative treatment for COVID-19. The herbal bioactives like catechins, andrographolide, hesperidin, biorobin, scutellarein, silvestrol, shikonin, tryptanthrin, vitexin quercetin, myricetin, caffeic acid, psoralidin, luteolin, etc. have shown potential inhibitory effect against SARS-CoV-2. Recent research reports indicate that the various plant secondary metabolites have shown potential antiviral activities. The present review article highlights the recent information on the mechanism of actions and applications of herbal medicine in the treatment of COVID-19.

Nanoparticlized System: Promising Approach for the Management of Alzheimer's Disease through Intranasal Delivery.

Alzheimer's disease (AD) is a neurodegenerative brain problem and responsible for causing dementia in aged people. AD has become most common neurological disease in the elderly population worldwide and its treatment remains still challengeable. Therefore, there is a need of an efficient drug delivery system which can deliver the drug to the target site. Nasal drug delivery has been used since prehistoric times for the treatment of neurological disorders like Alzheimer's disease (AD). For delivering drug to the brain, blood brain barrier (BBB) is a major rate limiting factor for the drugs. The desired drug concentration could not be achieved through the conventional drug delivery system. Thus, nanocarrier based drug delivery systems are promising for delivering drug to brain. Nasal route is a most convenient for targeting drug to the brain. Several factors and mechanisms need to be considered for an effective delivery of drug to the brain particularly AD. Various nanoparticlized systems such as nanoparticles, liposomes, exosomes, phytosomes, nanoemulsion, nanosphere, etc. have been recognized as an effective drug delivery system for the management of AD. These nanocarriers have been proven with improved permeability as well as bioavailability of the anti-Alzheimer's drugs. Some novel drug delivery systems of anti-Alzheimer drugs are under investigation of different phase of clinical trials. Present article highlights on the nanotechnology based intranasal drug delivery system for the treatment of Alzheimer's disease. Furthermore, consequences of AD, transportation mechanism, clinical updates and recent patents on nose to brain delivery for AD have been discussed.

Exciting Potential of Nanoparticlized Lipidic System for Effective Treatment of Breast Cancer and Clinical Updates: A Translational Prospective.

Breast cancer (BC) is a multifactorial disease and becoming a major health issue in women throughout the globe. BC is a malignant type of cancer which results from transcriptional changes in proteins and genes. Besides the availability of modern medicines and detection tools, BC has become a topmost deadly disease and its cure still remains challenging. Nanotechnology based approaches are being employed for the diagnosis and treatment of BC at clinical stages. Nanosystems have a significant role in the study of the interaction of malignant cells with their microenvironment through receptor-based targeted approach. Nowadays, lipid-based nanocarriers are being popularized in the domain of pharmaceutical and medical biology for cancer therapy. Lipidic nanoparticlized systems (LNPs) have proven to have high loading efficiency, less toxicity, improved therapeutic efficacy, enhanced bioavailability and stability of the bioactive compounds compared to traditional drug delivery systems. In the present context, several LNPs based formulations have been undertaken in various phases of clinical trials in different countries. This review highlights the importance of chemotherapeutics based lipidic nanocarriers and their anticipated use for the treatment of BC. Furthermore, the clinical trials and future prospective of LNPs have been widely elaborated.

Intranasal Nanoemulsions for Direct Nose-to-Brain Delivery of Actives for CNS Disorders.

The treatment of various central nervous system (CNS) diseases has been challenging, despite the rapid development of several novel treatment approaches. The blood-brain barrier (BBB) is one of the major issues in the treatment of CNS diseases, having major role in the protection of the brain but simultaneously constituting the main limiting hurdle for drugs targeting the brain. Nasal drug delivery has gained significant interest for brain targeting over the past decades, wherein the drug is directly delivered to the brain by the trigeminal and olfactory pathway. Various novel and promising formulation approaches have been explored for drug targeting to the brain by nasal administration. Nanoemulsions have the potential to avoid problems, including low solubility, poor bioavailability, slow onset of action, and enzymatic degradation. The present review highlights research scenarios of nanoemulsions for nose-to-brain delivery for the management of CNS ailments classified on the basis of brain disorders and further identifies the areas that remain unexplored. The significance of the total dose delivered to the target region, biodistribution studies, and long-term toxicity studies have been identified as the key areas of future research.

Development of Ayurveda - Tradition to trend.

ETHNOPHARMACOLOGICAL RELEVANCE: Ayurveda entails a scientific tradition of harmonious living and its origin can be traced from ancient knowledge in Rigveda and Atharvaveda. Ayurveda is a traditional healthcare system of Indian medicine since ancient times. Several Ayurvedic medicines have been exploiting for treatment and management of various diseases in human beings. The several drugs have been developed and practiced from Ayurveda since ancient time to modern practice as 'tradition to trend'. The potential of Ayurvedic medicine needs to be explored further with modern scientific validation approaches for better therapeutic leads. AIM OF THE STUDY: The present study was aimed to explore the various aspects of Ayurveda and inspired drug discovery approaches for its promotion and development. MATERIALS AND METHODS: We have reviewed all the literature related to the history and application of Ayurvedic herbs. Various aspects for the quality control, standardization, chemo-profiling, and metabolite fingerprinting for quality evaluation of Ayurvedic drugs. The development of Ayurvedic drugs is gaining momentum with the perspectives of safety, efficacy and quality for promotion and management of human health. Scientific documentation, process validation and several others significant parameters are key points, which can ensure the quality, safety and effectiveness of Ayurvedic drugs. RESULTS: The present review highlights on the major goal of Ayurveda and their significant role in healthcare system. Ayurveda deals with several classical formulations including arka, asavas, aristas, churna, taila, vati, gutika, bhasma etc. There are several lead molecules that have been developed from the Ayurvedic herbs, which have various significant therapeutic activities. Chemo-profiling of Ayurvedic drug is essential in order to assess the quality of products. It deals with bioactive compound quantification, spurious and allied drug determination, chromatographic fingerprinting, standardization, stability and quality consistency of Ayurvedic products. CONCLUSIONS: Scientific validation and the documentation of Ayurvedic drugs are very essential for its quality evaluation and global acceptance. Therapeutic efficacy of Ayurvedic herbs may be enhanced with high quality, which can be achieved by identity, purity, safety, drug content, physical and biological properties. Ayurvedic medicines need be explored with the modern scientific approaches for its validation. Therefore, an attempt has been made in the present review to highlight the crucial aspects that need to be considered for the promotion and development of Ayurvedic medicine.

Enhancement of photoprotection potential of catechin loaded nanoemulsion gel against UVA induced oxidative stress.

The present study was aimed to develop a catechin (CA) loaded nanoemulsion based nano-gel for the protection of skin against ultraviolet radiation (UV) induced photo-damage and to ensure its enhanced skin permeability as well as bioavailability through transdermal route. The optimized nanoemulsion (CA-NE4) was prepared by spontaneous nano-emulsification method. It was composed of oil (ethyl oleate), Smix [surfactant (span 80) and co-surfactant (transcutol CG)] and aqueous system in an appropriate ratio of 15:62:23% w/w respectively. The CA-NE4 was characterized through assessment of droplet size, zeta potential, refractive index, transmission electron microscopy (TEM), UV, high performance thin layer chromatography (HPTLC) and Fourier transform infrared spectroscopy (FTIR) analysis. The average droplet size and zeta potential of CA-NE4 were found to be 98.6±1.01nm and -27.3±0.20mV respectively. The enhanced skin permeability was better with CA-NE4 based nano-gel (CA-NG4) [96.62%] compared to conventional gel (CA-CG) [53.01%] for a period of 24h. The enhanced % relative bioavailability (F) of CA (894.73), Cmax (93.79±6.19ngmL(-1)), AUC0-t∞ (2653.99±515.02nghmL(-1)) and Tmax (12.05±0.02h) was significantly obtained with CA-NG4 as compared to oral suspension for extended periods (72h). CA-NG4 could improve the level of cutaneous antioxidant enzymes like superoxide dismutase (SOD), glutathione peroxidase (GPX) and catalase (CAT) and reduce the level of thiobarbituric acid reactive substances (TBRAS) against oxidative stress induced by UVA. Nano-gel formulation of CA showed sustained release profile and enhanced photoprotection potential due to its improved permeability as well as bioavailability (P<0.05) compared to the conventional gel. Therefore, transdermal administration of nano-gel (CA-NG4) of CA offers a better way to develop the endogenous cutaneous protection system and thus could be an effective strategy for decreasing UV-induced oxidative damage in the skin tissues.

Metabolism-mediated interaction potential of standardized extract of Tinospora cordifolia through rat and human liver microsomes.

OBJECTIVE: Tinospora cordifolia is used for treatment of several diseases in Indian system of medicine. In the present study, the inhibition potential of T. cordifolia extracts and its constituent tinosporaside to cause herb-drug interactions through rat and human liver cytochrome enzymes was evaluated. MATERIALS AND METHODS: Bioactive compound was quantified through reverse phase high-performance liquid chromatography, to standardize the plant extracts and interaction potential of standardized extract. Interaction potential of the test sample was evaluated through cytochrome P450-carbon monoxide complex (CYP450-CO) assay with pooled rat liver microsome. Influence on individual recombinant human liver microsomes such as CYP3A4, CYP2D6, CYP2C9, and CYP1A2 isozymes was analyzed through fluorescence microplate assay, and respective IC50 values were determined. RESULTS: The content of tinosporaside was found to be 1.64% (w/w) in T. cordifolia extract. Concentration-dependent inhibition was observed through T. cordifolia extract. Observed IC50 (µg/ml) value was 136.45 (CYP3A4), 144.37 (CYP2D6), 127.55 (CYP2C9), and 141.82 (CYP1A2). Tinosporaside and extract showed higher IC50 (µg/ml) value than the known inhibitors. T. cordifolia extract showed significantly less interaction potential and indicates that the selected plant has not significant herb-drug interactions relating to the inhibition of major CYP450 isozymes. CONCLUSIONS: Plant extract showed significantly higher IC50 value than respective positive inhibitors against CYP3A4, 2D6, 2C9, and 1A2 isozymes. Consumption of T. cordifolia may not cause any adverse effects when consumed along with other xenobiotics.

CYP450 mediated inhibition potential of Swertia chirata: An herb from Indian traditional medicine.

ETHNOPHARMACOLOGICAL RELEVANCE: An Ayurvedic herb, Swertia chirata (SC) have been used in treating various ailments such as hyperglycemia, leishmania, liver infections, inflammation, abdominal pain, bacterial infection, malaria etc. in Indian Systems of Medicine (ISM). AIM OF THE STUDY: Study was designed to investigate the inhibition potential of the standardized SC extract along with its bioactive molecule ursolic acid on hepatic drug metabolizing isozymes (CYP3A4 and CYP2D6) and further some heavy metals were also analysed of the plant material. MATERIALS AND METHODS: The hydro-alcoholic extract was standardized with standard ursolic acid by reverse phase-high performance liquid chromatography (RP-HPLC) method and the heavy metals content were analyzed through atomic absorption spectroscopy (AAS). The effect of extract on rat liver microsome (RLM) and individual CYP isozymes (CYP3A4 and CYP2D6) was investigated through CYP450-CO complex assay and fluorescence microplate assay respectively. RESULTS: The content of ursolic acid was found to be 2.66% (w/w) in the SC extract and heavy metal contents along with trace elements were within the prescribed limits as per WHO guidelines. The inhibitory potential of SC extract on RLM was found to be 23.64±1.80%. CYP3A4 and CYP2D6 inhibitory effect of SC and ursolic acid (IC50: 197.49±2.68, 211.45±3.54 and IC50: 229.25±2.52, 212.66±1.26 µg/mL) was less as compared to that known inhibitors, ketoconazole and quinidine respectively. CONCLUSIONS: The current study revealed that S. chirata has less inhibition potential with two major drug metabolizing isozymes CYP3A4 and CYP2D6. SC extract and ursolic acid showed significantly (P<0.001) less inhibitory potential on RLM. The Ayurvedic herb (SC) has shown less inhibitory activity in a concentration dependent manner against the tested two CYP450 enzymes. The tested heavy metals and trace elements present SC was within limit. Therefore, the traditional use of S. chirata may be safe in respect of both tested isozymes.

Evaluation of Ubtan - A traditional indian skin care formulation.

ETHNOPHARMACOLOGICAL RELEVANCE: 'Ubtan' is a traditional herbal formulation in the Indian system of medicine being used in India and its subcontinent for a long time. Several commercial skin care formulations are marketed throughout this region as the name of Ubtan. Therefore, it is worthwhile to evaluate Ubtan in respect of its efficacy as skin care formulation. AIM OF THE STUDY: The present study was designed for the preparation of Ubtan and standardization through the chromatographic techniques by using suitable phyto-markers. Further, its antioxidant, sun protection factor (SPF) and anti-tyrosinase potential have been explored. MATERIALS AND METHODS: Four in-house formulations (UF-1, UF-2, UF-3 and UF-4) were prepared by mixing a varied quantity of each powdered plants, i.e. turmeric (Curcuma longa L.), Chickpea (Cicer arietinum L.) and sandalwood (Santalum album L.). Optimization of the formulations was made by evaluating its biological activity through in vitro assay. Evaluation of physicochemical properties of the optimized formulation (UF-1) has been carried out by analysis of pH, flow properties and stability. Moreover, RP-HPLC (reverse phase - high performance liquid chromatography) and HPTLC (high performance thin layer chromatography) standardization of UF-1 was performed for its quantitative and qualitative analysis. RESULTS: Ubtan formulations (UF-1to UF-4) showed free radical scavenging and ferric reducing potential. It may be due to its high phenolic and flavonoid content. Statistically, significant Pearson's correlation (r) was confirmed the positive correlation between phenolic content and SPF of the formulations. The tyrosinase inhibition study indicated that the formulations showed both diphenolase and monophenolase inhibitory activity. Among four formulations, UF-1 showed notable biological activity (p<0.05). The content of curcumin and ascorbic acid was found to be 1.6% and 2.1% w/w respectively in UF-1 through RP-HPLC estimation. Physiochemical properties of the UF-1 exhibited good flow rate and aqueous solubility. From the stability studies, it can be anticipated that the UF-1 was stable at 40°C for longer periods. Microbial load count and heavy metal content (lead-Pb, arsenic-As, mercury-Hg and cadmium-Cd) of the formulation was also within the permissible limit of a pharmacopeial standard. CONCLUSION: This scientific exploration helps to set the quality and safety standard of traditional cosmetic formulation, Ubtan and its further use as an herbal skin care product.

Enhanced permeability of ferulic acid loaded nanoemulsion based gel through skin against UVA mediated oxidative stress.

AIMS: The study was aimed to develop a ferulic acid (FA) loaded nanoemulsion based gel in order to ensure the enhanced permeability and maximum antioxidant activity against UVA induced oxidative stress in rat. MAIN METHODS: The optimized ferulic acid loaded nanoemulsion 3 (FA-NE3) was prepared by spontaneous nano-emulsification method with an appropriate ratio (20:30:50% w/w) of the oil (isostearyl isostearate), aqueous system and Smix [surfactant (labrasol) and co-surfactant (plurol isostearique)] respectively. FA-NE3 was characterized by measuring their droplet size, zeta potential, refractive index, transmission electron microscopy (TEM), ultraviolet (UV), fourier transform infrared spectroscopy (FTIR) and rheological characteristics. Ex vivo skin permeation and in vivo UVA protection activity of FA-NE3 based nano-gels (FA-NG3) along with placebo were studied through the rat skin. KEY FINDINGS: FA-NE3 exhibited sustained-release profile, better permeability and ultraviolet A (UVA) protection activity as compared to conventional dosage form. This phenomenon may be attributed towards increased solubility of the drug and enhanced permeability from nanoemulsion. FA-NE3 based nanogel (FA-NG3) could elevate the level of skin marker enzymes against oxidative stress mediated by UVA. SIGNIFICANCE: The gel formulation exhibited significant (P<0.01) skin permeability and antioxidant activity in the current investigations. The nanogel could be promising nanocarriers for topical delivery of FA in response to better skin protection activity against UVA rays in a sustained manner.

Interaction potential of Trigonella foenum graceum through cytochrome P450 mediated inhibition.

OBJECTIVE: The seeds of Trigonella foenum-graecum (TFG) (family: Leguminosae) are widely consumed both as a spice in food and Traditional Medicine in India. The present study was undertaken to evaluate the inhibitory effect of standardized extract of TFG and its major constituent trigonelline (TG) on rat liver microsome (RLM) and cytochrome P450 (CYP450) drug metabolizing isozymes (CYP3A4 and CYP2D6), which may indicate the possibility of a probable unwanted interaction. MATERIALS AND METHODS: Reverse phase-high performance liquid chromatography method was developed to standardize the hydroalcoholic seed extract with standard TG. The inhibitory potential of the extract and TG was evaluated on RLM and CYP isozymes using CYP450-carbon monoxide (CYP450-CO) complex assay and fluorescence assay, respectively. RESULTS: The content of TG in TFG was found to be 3.38% (w/w). The CYP-CO complex assay showed 23.32% inhibition on RLM. Fluorescence study revealed that the extract and the biomarker had some inhibition on CYP450 isozymes e.g. CYP3A4 and CYP2D6 (IC50 values of the extract: 102.65 ± 2.63-142.23 ± 2.61 µg/ml and TG: 168.73 ± 4.03-180.90 ± 2.49 µg/ml) which was very less compared to positive controls ketoconazole and quinidine. Inhibition potential of TFG was little higher than TG but very less compared to positive controls. CONCLUSIONS: From the present study, we may conclude that the TFG or TG has very less potential to inhibit the CYP isozymes (CYP3A4, CYP2D6), so administration of this plant extract or its biomarker TG may be safe.