Decoding Therapeutic Applications of Quercetin: Recent Advancements in Nanotechnological Strategies.

For centuries, people have used herbal medicine to treat a diversity of health complications and as a natural substance, they have a favourable effect on our health. Herbal ingredients can be utilized as lead molecules in the innovation and development of a new drug. Flavonoids are a class of chemical compounds with diverse phenolic structures, and they are found in a wide variety of foods, including fruits, vegetables, cereals, bark, roots, stems, flowers, tea, and wine. Quercetin is the most prevalent polyphenolic bioflavonoid or flavonoid. Quercetin is found in many food products and has demonstrated a wide range of pharmacological activities, including the treatment of allergies, ocular diseases, metabolic ailments, inflammatory illnesses, cardiovascular ailments and arthritis. Quercetin has attracted interest as an emerging pharmacophore with the potential to significantly advance research and the development of novel therapeutic medicines for a variety of diseases. Despite having a huge therapeutic potential, these flavonoids have unfavourable pharmacokinetic characteristics, low bioavailability, and poor solubility, limiting their application in therapeutics. The objective of the current study is to present a new update on the major therapeutic uses of quercetin and other types of nanocarriers that contain quercetin to treat various ailments.

Exploring the Therapeutic Potential of Phytoconstituents for Addressing Neurodegenerative Disorders.

Neurodegenerative disorder is a serious condition that is caused by abnormal or no neurological function. Neurodegenerative disease is a major growing cause of mortality and morbidity worldwide, especially in the elderly. After World War Ⅱ, eugenics term was exterminated from medicines. Neurodegenerative disease is a genetically inherited disease. Lifestyle changes, environmental factors, and genetic modification, together or alone, are involved in the occurrence of this disorder. The major examples of neurodegenerative disorders are Alzheimer's and Parkinson's disease, in which apoptosis and necrosis are the two major death pathways for neurons. It has been determined from various studies that the etiology of the neurodegenerative disease involves the role of oxidative stress and anti-oxidant defence system, which are prime factors associated with the activation of signal transduction pathway that is responsible for the formation of synuclein in the brain and manifestation of toxic reactions in the form of functional abnormality, which ultimately leads to the dysfunction of neuronal pathway or cell. There has not been much success in the discovery of effective therapy to treat neurodegenerative diseases because the main cause of abnormal functioning or death of neurons is not well known. However, the use of natural products that are derived from plants has effective therapeutic potential against neurodegenerative disease. The natural compounds with medicinal properties to prevent neurological dysfunction are curcumin, wolfberry, ginseng, and Withania somnifera. The selection and use of natural compounds are based on their strong anti-inflammatory and anti-oxidant properties against neurodegenerative disease. Herbal products have active constituents that play an important role in the prevention of communication errors between neurons and neurotransmitters and their respective receptors in the brain, which influence their function. Considering this, natural products have great potential against neurodegenerative diseases. This article reviews the natural compounds used to treat neurodegenerative diseases and their mechanisms of action.

Therapeutic Potential and Clinical Effectiveness of Quercetin: A Dietary Supplement.

Fruits and vegetables (like apples, citrus, grapes, onions, parsley, etc.) are the primary dietary sources of quercetin. In addition, isolated quercetin is also available on the market as a dietary supplement with a daily dose of up to 1000 mg/d. The objective of the present study is to explore the therapeutic potential and clinical efficacy of quercetin as a dietary supplement. The present paper highlights the safety parameters and clinical trial studies with several targets reviewed from the data available on PubMed, Science Direct, ClinicalTrails. gov, and from many reputed foundations. The results of the studies prove the unique position of quercetin in the treatment of various disorders and the possibility of using phytochemicals such as quercetin for an efficient cure. As evidenced by the numerous published reports on human interventions, it has been concluded that quercetin intake significantly improves disease conditions with minimal adverse effects.

Chebulinic Acid: An Incipient Anticancer Agent.

BACKGROUND: Terminalia chebula (T. chebula) comprising chebulinic acid as its principle active constituent is used to cure various diseases. T. chebula and chebulinic acid are used as antimicrobial, antioxidant, antidiabetic, anti-inflammatory, hepatoprotective, antimutagenic, radioprotective, cardioprotective, antiproliferative, antiarthritic, anticaries, and so on. OBJECTIVE: The objective of this current study is to give an overview of the recent literature and patents of T. chebula and chebulinic acid including methods of its isolation/extraction and their application in the prevention of various cancers and other diseases. METHODS: Present research and patents highlighting the anti-cancer potential of T. chebula and chebulinic acid have been studied and discussed keeping in view the scientific novelty and impact. RESULTS: Both T. chebula and chebulinic acid are currently being explored for their anticancer potential in vitro and in vivo. They are either incorporated alone or in combination with other plants or drugs to show their activity and many clinical trials are also going on various potentials of the plant and chebulinic acid. Novel extraction techniques are also explored and patented. Efforts are being made to improve the bioavailability by developing Novel herbal drug delivery systems of the plant extract or chebulinic acid itself. CONCLUSION: Anti-cancer potential of T. chebula and chebulinic acid may be well established by promising clinical trials and may open new interventions in various tumors. Clinical trials in conjunction with standard therapies are required to explore and validate the actual potential of T. chebula and chebulinic acid respectively.

Therapeutic Potential and Clinical Evidence of Hesperidin as Neuroprotective Agent.

BACKGROUND: Neuroprotection is preserving neural function in various neurodegenerative diseases like Alzheimer's, Huntington's, Parkinson's, and multiple sclerosis. Hesperidin, a flavanone glycoside in citrus fruits such as sweet oranges and lemons, possesses many biological effects, including neuroprotection. OBJECTIVE: The study aims to explore the neuropharmacological mechanisms and therapeutic potential of hesperidin in the management of neurodegenerative disorders. METHODS: It emphasizes comparative and clinical trial studies with a number of targets reviewed from the data available on PubMed, Science Direct, Clinicaltrails.gov, and from many reputed foundations. RESULTS: Escalating clinical evidence has established the inhibitory effect of hesperidin in the management of neurodegenerative disorders. Neuroprotective potential of hesperidin is characterized by endogenous antioxidant defence functions, improvement of neural growth factors, antineuroinflammatory activity, and apoptotic pathways. CONCLUSION: The present study highlights the beneficial neuropharmacological potential of hesperidin, including anticonvulsant, antidepressant, antioxidant, anti-inflammatory, memory, and locomotor enhancing activities.

Transdermal Drug Delivery: A Step towards Treatment of Cancer.

BACKGROUND: Transdermal drug delivery is an emerging and appealing alternative to oral and hypodermic drug delivery systems. With the new developments in skin penetration techniques, anticancer drugs ranging from hydrophilic macromolecules to lipophilic drugs can be administered via a transdermal route to treat cancer. OBJECTIVE: In the present review, various approaches to enhance the transdermal delivery of drugs are discussed, including micro and nanotechnology-based transdermal formulations like chemotherapy, gene therapy, immunotherapy, phototherapy, vaccines, and medical devices. Limitations and advantages of various transdermal technologies are also elaborated. METHODS: In this review, patent applications and recent literature of transdermal drug delivery systems employed to cure mainly cancer are covered. RESULTS: Transdermal drug delivery systems have proved their potential to cure cancer. They increase the bioavailability of the drug by site-specific drug delivery and can reduce the side effects/- toxicity associated with anticancer drugs. CONCLUSION: The potential of transdermal drug delivery systems to carry the drug may unclutter novel ways for therapeutic intercessions in various tumors.

Formulation optimization and characterization of transdermal film of curcumin by response surface methodology.

Objective: India is referred as goldmine of herbal drugs but still lack of optimization of herbal drugs, which has kept us on the back foot. The rationale of the study is to prepare optimized transdermal drug delivery system of curcumin employing response surface methodology to study the collective effect of independent variables like concentration of ethyl cellulose, hydroxyl propyl methyl cellulose and dibutyl phthalate which significantly influenced characteristics like percentage elongation and in vitro drug release. Method: Twenty formulations containing varying concentrations of polymers and permeation enhancer were prepared using solvent casting technique. Result: The study revealed that the effect of dibutyl phthalate (DBP) concentration was the highest on percentage elongation (P < 0.0001), while hydroxy propyl methyl cellulose (HPMC) concentration exhibited pronounced effect on drug release (P < 0.0001) through dialysis membrane. Linear model fitted the best for curcumin release and elongation for all formulations. According to Derringer's desirability prediction tool, the composition of optimized film was found to be 242.14% of HPMC, 109.59% of ethyl cellulose (EC), and 1.03% of DBP. Under these conditions, the optimized patch exhibited a predicted value of %elongation and in vitro drug release of 94.35% and 80.0306%, respectively, which was comparable to the actual values of percent elongation and in vitro drug release i.e. 95.02% and 81.03% respectively. FTIR and thermal studies were also performed which revealed no interaction or complexation between drug and excipients. The ex vivo study performed using rat skin showed that the cumulative drug release from the optimized patch showed flux of (30.68 ± 18) µg/cm2/h. Conclusion: It can be concluded that in future if proper optimization of herbal formulations is carried out, they can become the first choice for patients as compare to synthetic drugs.

Recent Patents on Anti-Cancer Potential of Helenalin.

BACKGROUND: Arnica montana, containing helenalin as its principal active constituent, is the most widely used plant to treat various ailments. Recent studies indicate that Arnica and helenalin provide significant health benefits, including anti-inflammatory, neuroprotective, antioxidant, cholesterol-lowering, immunomodulatory, and most important, anti-cancer properties. OBJECTIVE: The objective of the present study is to overview the recent patents of Arnica and its principal constituent helenalin, including new methods of isolation, and their use in the prevention of cancer and other ailments. METHODS: Current prose and patents emphasizing the anti-cancer potential of helenalin and Arnica, incorporated as anti-inflammary agents in anti-cancer preparations, have been identified and reviewed with particular emphasis on their scientific impact and novelty. RESULTS: Helenalin has shown its anti-cancer potential to treat multiple types of tumors, both in vitro and in vivo. It has also portrayed synergistic effects when given in combination with other anti- cancer drugs or natural compounds. New purification/isolation techniques are also developing with novel helenalin formulations and its synthetic derivatives have been developed to increase its solubility and bioavailability. CONCLUSION: The promising anti-cancer potential of helenalin in various preclinical studies may open new avenues for therapeutic interventions in different tumors. Thus clinical trials validating its tumor suppressing and chemopreventive activities, particularly in conjunction with standard therapies, are immediately required.

Novel Herbal Topical Patch Containing Curcumin and Arnica montana for the Treatment of Osteoarthritis.

BACKGROUND: Osteoarthritis (OA) ranks fifth among all forms of disability affecting 10% of the world population. Current treatments available are associated with multiple side effects and do not slow down the progression of the disease. Moreover, no such effective treatment is available to date in various systems of medicine to treat osteoarthritis. Curcumin and Arnica have shown evident clinical advances in the treatment of osteoarthritis. OBJECTIVE: The aim of the present study was to design, optimize and characterize novel herbal transdermal patches of curcumin and Arnica montana using factorial design. METHODS: A multiple factorial design was employed to investigate the effect of hydroxypropyl methyl cellulose, ethyl cellulose and jojoba oil on elongation and drug release. Transdermal patches were evaluated by FTIR, DSC, FESEM, ex vivo drug permeation, anti osteoarthritic activity and analgesic activity. RESULTS: Independent variables exhibited a significant effect on the physicochemical properties of the prepared formulations. The higher values of drug release and elongation were observed with the higher concentration of hydroxypropyl methylcellulose and jojoba oil. Anti osteoarthritic activity was assessed by complete Freund's adjuvant arthritis model; using rats and analgesic activity by Eddy's hot plate method, using mice. Combination patch exhibited good anti osteoarthritic and analgesic activity as compare to individual drug patches. CONCLUSION: The design results revealed that the combination patch exhibited good physicochemical, anti osteoarthritic and analgesic activity for the treatment of osteoarthritis in animals. More plants and their combinations should be explored to get reliable, safe and effective formulations that can compete with synthetic drugs.

Arnica montana L. - a plant of healing: review.

OBJECTIVES: Arnica montana is a widely used therapeutic plant used traditionally to treat various ailments. The objective of this study was to evaluate the botany, phytochemistry and ethnopharmacology along with special emphasis given on pharmacological activity of plant A. montana. KEY FINDINGS: The plant extracts have been reported to possess antibacterial, antitumor, antioxidant, anti-inflammatory, antifungal and immunomodulatory activity. A wide range of chemical compounds including sesquiterpene lactones and their short-chain carbonic acid esters, flavonoids, carotenoids, essential oils, diterpenes, arnidiol, pyrrolizidine alkaloids, coumarins, phenolic acids, lignans and oligosaccharides, etc., are found in different parts of the plant. SUMMARY: It has been scrutinized that extensive research has been carried out to explore the therapeutic potential of flowers of the plant. Therefore, investigations should be carried out to explore the therapeutic potential of other parts of the plant for better therapeutic utilization.