NEUROPHARMACOLOGICAL EFFECTS OF THE ETHANOLIC EXTRACT OF DERIVATIVES OF LUPEOL IN RATS

Objective: The neuropharmacological activities of ethanolic extract derivatives of lupeol are being screened on rats. Prepared derivatives are evaluated for their locomotor, anxiolytic and stereotype activities. The present investigation was designed to evaluate the antipsychotic effect of semisynthetic derivatives of lupeol using rat models of elevated maze model and apomorphine-induced stereotype behavior.Methods: Lupeol was extracted from Crataeva nurvala bark using ethano. After chemical modification, we made different derivatives using aldol condensation. Different derivatives were obtained from a series of reaction previously published LAH-3, LAP-3, LAPEA-3, LAMP-3, LATS-3, and LAS-3. Neuropharmacological effects, including anxiolytic, central nervous inhibitory, and stereotype antipsychotic effects were evaluated in the different derivatives of lupeol at a dose of 250 mg/kg using standard methods.Results: The absolute derivatives of LAH3 and LAPEA3 showed a significant reduction in the activity score in actophotometer test. Reduction in the locomotor activity indicates central nervous system (CNS) depressant property of the drug. LAMP3 and LAS3 show a significant anxiolytic effect. From the result of elevated plus maze, it was evident that derivatives of lupeol treated animals exhibit an increased number of entries into open arm when compared to normal control, which shows the anxiolytic activity of the lupeol derivatives. Sniffing, rearing and licking activities for lupeol derivatives LAH3 and LAPEA3 were found to be 35%, 33%, and 40% and 40.33%, 38%, and 33.33% respectively when it compared with standard and control groups. This model is suggestive of the absence of negative symptoms alleviating property of all the treatment groups.Conclusions: The lupeol and its semisynthetic derivatives possess anxiolytic, CNS inhibitory, and antipsychotic effects to varying degree

VERSATILE RP-HPLC METHOD DEVELOPMENT FOR QUANTITATIVE ESTIMATION OF TELMISARTAN AND RAMIPRIL IN ANIMAL PLASMA

Objective: A fast, specific, and sensitive high-performance liquid chromatographic method has been developed and validated for the quantitative determination of unchanged Ramipril (RAM) and Telmisartan (TEL) in animal plasma.Methods: Analytes were extracted from animal plasma, 250 µl of animal plasma sample were mixed with internal working standard (25 ngmL-1) with the further addition of chloroform (HPLC Grade, Merck). The clear organic layer was separated and reconstituted to 1 ml in mobile phase and analysed by HPLC. The method was validated and evaluated in terms of linearity, accuracy, precision, specificity, limit of detection and limit of quantitation.Results: Absorption maxima of TEL and RAM was found to be 270 and 273 nm respectively. TEL and RAM with their respective internal standards (I. S.) were found to be well separated from the co-eluted components and there were no interferences from the endogenous material. The limit of detection (LOD) and limit of quantitation (LOQ) were found to be 2.01±.05; 4.88±0.10 and 0.11 and 0.25 for TEL and RAM respectively on the basis of a signal to noise ratio. The ruggedness of the method at various parameters was found to be±1.94% and±1.02% for TEL and RAM respectively. The low values of %RSD (<2.0) for each of the drug proposed that during all deliberate variations, middle-quality control (MQC) was not affected and it was in accordance with that of actual.Conclusion: Thus developed High-Performance Liquid Chromatography (HPLC) method was found to be more accurate, precise, sensitive, selective and reproducible

Titanium dioxide nanoparticles decreases activity of rat brain when administered prenatally

Background: Titanium dioxide nanoparticles are widely used in the sunscreens, toothpastes, and cosmetic products that the human use daily. Previous reports have proved that the impact of nanomaterials on brain activity is not negligible, especially for the people working in nanomaterials manufacturing factories. We are using titanium dioxide in our daily life in cosmetics, food industry and many other pharmaceutical products. So to keep a check on the threat what these chemicals may cause, we conducted a research to study effect of titanium dioxide nanoparticles on rat brain. This research gave us an insight of the possible threats it can cause to brain.Methods: The effects of titanium dioxide nanoparticles on brain activity were reported. Our studies showed that titanium dioxide nanoparticles have a differential tendency towards neurons. To insight the possible effect on titanium dioxide nanoparticles on neurobehaviour we conducted a conditioned avoidance response study using shuttle box analysis. In the study we administered the drug titanium dioxide nanoparticles prenatally and observed its effects by neurobehaviour studies in progenies of wistar rat.Results: In the results we observed that titanium dioxide nanoparticles have caused a decreased learning and memory behaviours as compared to control groups.Conclusions: We studied the neurobehaviour of progenies, when the drug was administered to rat brain prenatally. The results showed that the titanium dioxide nanoparticles particles have decreased the brain activity of the rat brain by showing decreased brain activity in progenies also

Primary and novel approaches for colon targeted drug delivery – A review

The colon is a site where both local and systemic delivery of drugs can take place. Local delivery could, for example, allow topical treatment of inflammatory bowel disease. Treatment could be made more effective if it were possible for drugs to be targeted directly on the colon. Systemic side effects could also be reduced. Colon specific systems might also allow oral administration of peptide and protein drugs, which are normally inactivated in the upper parts of the gastrointestinal tract. Primary approaches for CDDS (Colon Specific Drug Delivery), which includes prodrugs, pH and time dependent systems and microbially triggered drug delivery system achieved limited success and having limitations. Newly developed CDDS, which includes pressure controlled colonic delivery capsules (PCDCS), CODESTM and osmotic controlled drug delivery are unique in terms of achieving in vivo site specificity and feasibility of manufacturing process. This review also focuses on evaluations of CDDS in general.Keywords: Colon drug delivery systems; Primary approaches; Newly developed approaches; evaluation of colon targeted drug delivery system

Entrega liposomal de 5 fluorouracilo y tretinoína: un aspecto del tratamiento tópico de las verrugas cutáneas

Background: Tretinoin and 5-fluorouracil are indicated for treatment of various skin disorders and actinic keratosis respectively. Objective: Present study was focused to design liposomes containing 5- fluorouracil and tretinoin. Design was further optimized by 32 full factorial design. Methods: Liposomes were prepared by ethanol injection method and evaluated by Transmission Electron Microscopy, percentage entrapment efficiency, zeta potential and in vitro drug release. Optimized formulation was subjected to histopathological and stability studies at 4ºC, 25ºC and 60ºC temperatures. Results: No drug crystals were visible in transmission electron microscopy, regardless of the preparation technique or the loaded drug. Formulation F9 showed maximum drug entrapment of 72.86% and 69.70% for 5-fluorouraciland tretinoin respectively. When phospholipid concentration was increased from 40 to 60 mg/ml, encapsulation efficiencies of formulation increased. Zeta potential and particle size were maintained within range of -19.14 to -25.61 and 100 to 200 nm respectively which facilitated good stability and penetration of liposomes. Dissolution profiles of formulations F1 to F6 showed high amount of drug release (30.6 to 67.42%) at 2 h. Liposomes were not stable at high temperature but formulations were most stable when stored at lower temperature i.e. 4oC. Conclusion: So, in liposomes both 5-fluorouracil and tretinoin were successfully incorporated and it can be further used for formulation development. Objetivo: El presente estudio se centró en el diseño de liposomas que contenían 5-fluorouracilo y tretinoína. El diseño fue optimizado por 32 diseño factorial completo. Metodos: Los liposomas se prepararon mediante el método de inyección de etanol y se evaluaron mediante Microscopía Electrónica de Transmisión, % de eficiencia de encapsulación, potencial zeta y liberación de fármaco in vitro. La formulación optimizada se sometió a estudios histopatológicos y de estabilidad a temperaturas de 4ºC, 25ºC y 60ºC. Resultados: Ningún cristal de los fármacos era visibles en el Microscopía Electrónica de Transmisión, sin importar la técnica de la preparación o el fármaco cargado. La formulación F9 demostró el atrapamiento máximo del fármaco del 72,86% y del 69,70% para 5-fluorouracilo y tretinoína respectivamente. Cuando la concentración del fosfolípido fue aumentada a partir de 40 a 60 mg/ml, las eficiencias de encapsulación de la formulación aumentaron. El potencial de zeta y el tamaño de partícula fueron mantenidos dentro de la gama de-19,14 a -25,61 y 100 a 200 nanómetros respectivamente, que facilitó la buena estabilidad y la penetración de liposomas. Los perfiles de disolución de las formulaciones F1 a F6 mostraron una alta cantidad de liberación de fármaco (30,6 a 67,42%) a las 2h. Los liposomas no eran estables a alta temperatura, pero las formulaciones eran más estables cuando se almacenaban a una temperatura más baja, es decir, 4 ºC. Concusiones: Así, en los liposomas, tanto los fármacos 5-fluorouracilo como los tretinoína se incorporaron con éxito y se pueden utilizar para el desarrollo de la formulación

Role of Herbal Medicine, Acupressure and Acupuncture in the Treatment of Irritable Bowel Syndrome

Irritable bowel syndrome (IBS), is a chronic functional gastrointestinal disease that is characterized by a variety of symptoms that have a major negative impact on patients’ quality of life. It affects 9–23% of the total population of the world. At this time, no medication that is capable of addressing all symptoms associated with IBS in an effective manner (antispasmodics, antidiarrheals, sedatives). More than half of patients may seek treatment for their gastrointestinal problems via the use of complementary and alternative medicine (CAM), which includes treatments like herbal medicine, acupuncture, and acupuncture. The objective of this chapter is to evaluate the effectiveness and safety of a herbal preparation, acupuncture, and acupressure treatment in patients diagnosed with IBS. Several sources were used to acquire the material, including review articles published in various publications that had keywords such as herbal drugs, acupuncture, acupressure, IBS and so on. The information was also gathered from the Internet. Herbal therapy and plant products are widely utilized to treat IBS. Acupuncture and acupressure have long been used successfully by patients to treat functional gastrointestinal problems. Multiple clinical studies have shown that their effectiveness and safety are superior to those of placebo and conventional medications. Herbal medications, acupressure, or acupuncture show clinically and statistically significant alleviation of IBS symptoms

VITAL POTENTIAL OF MULTIPLE HERBS IN PROPHYLAXIS OF OBESITY

Objective: Allopathic medications are associated with several inconveniences such as drug dependency. More than 2000 herbal medicines have been proved to have a therapeutic effect in multiple disorders. The prominent aim of this review paper is to compute the therapeutic effect of herbal drug against obesity along with their different mechanisms. Methods: Data have been selected by evaluating merger of specific review and research papers through filtering through data bases such as PubMed, and Google Scholar of last 10 years 2009–2019. Results: On the basis of our interpretations, we have concluded that the herbal drugs constituting active constituents’ as tannins, alkaloids, resins, saponins, and flavonoids are effective in lowering the blood triglycerides level, lipid accumulation in liver, fat accumulation, adipocyte differentiation, and ultimately decrease body weight with almost negligible toxicity. Conclusion: Obesity is highly related to elevated morbidity rate as well as has become cause of various disorders. Herbal drugs have potential to treat obesity through different mechanisms including lipid peroxidation, free-radical scavenging activity, and inhibition of fat accumulation

A REVIEW ON ROLE OF BERRIES AND ITS BIOACTIVE COMPOUNDS IN TREATING HYPERTENSION

Objective: Hypertension or raised blood pressure leads to the occurrence of morbidity and mortality rate among peoples and it was considered as the primary factor for the occurrence of various cardiac and vascular disorders include ischemic cardiac disease, myocardial necrosis, cardiac failure, renal disorder, atherosclerosis, and cerebrovascular accident. Called “silent killer” because hypertension is an asymptomatic disease in the early stages with no indications on suffered patients and leads to act as a significant factor for the occurrence of severe other cardiovascular diseases (CVDs). As berries show considerable interest in improving cardiovascular diseases because they are rich in polyphenol contents and bioactive compounds. Besides their single usage, a polyherbal combination is much better for the treatment of hypertension. Methods: The data were collected by reviewing a combination of research and review papers from different databases such as PubMed, Medline, ScienceDirect, and Web of science using search keywords such as “hypertension,” “cardiovascular disease,” “berries,” “cranberry,” and “red raspberry” with all their synonyms and related terms. Result: Various studies shown better associations between higher berry flavonoids and other polyphenolic components and lower the risk of cardiovascular disorders. Based on various scientific evidence, the characteristic of various biochemical processes is treated by berries with its antioxidant, antihypertensive, and anti-sclerotic and other properties. Conclusion: This paper concludes that in the present day, there is a global increase in berry consumption, which is used in the ailment of various cardiovascular diseases. The studies which are held are needed to define their optimal dose, process, or method of preparation (formulation) and the duration of berry intervention so that these showed better treatment options for hypertension

Aliskiren: An orally active renin inhibitor

Renin inhibitors are antihypertensive drugs that block the first step in the renin-angiotensin system. Their mechanism of action differs from that of the angiotensin-converting enzyme inhibitors and angiotensin-receptor antagonists, but like these drugs, renin inhibitors interrupt the negative feedback effects of angiotensin II on renin secretion. The renin–angiotensin–aldosterone system (RAAS) has long been recognized to play a significant role in hypertension pathophysiology. Certain agents that modify the RAAS can control blood pressure and improve cardiovascular outcomes. Optimization of this compound by Novartis led to the development of aliskiren – the only direct renin inhibitor which is clinically used as an antihypertensive drug. Aliskiren is the first of a new class of antihypertensive agents. Aliskiren is a new renin inhibitor of a novel structural class that has recently been shown to be efficacious in hypertensive patients after once-daily oral dosing. In short-term studies, it was effective in lowering blood pressure either alone or in combination with valsartan and hydrochlorothiazide, and had a low incidence of serious adverse effects. It was approved by the Food and Drug Administration in 2007 for the use as a monotherapy or in combination with other antihypertensives. Greater reductions in blood pressure have been achieved when aliskiren was used in combination with hydrochlorothiazide or an angiotensin-receptor blocker. The most common adverse effects reported in clinical trials were headache, fatigue, dizziness, diarrhea, and nasopharyngitis. Aliskiren has not been studied in patients with moderate renal dysfunction; as an RAAS-acting drug, it should be prescribed for such patients only with caution