Rubatosis Publications (E-Journals)
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Advancements in Nanostructure Applications for the Anticancer Delivery of Natural Compounds
In drug design, compounds and extracts sourced from natural origins continue to play a crucial role, offering versatile interactions with enzymes, receptors, and metabolic pathways. Nanomedicine emerges as a powerful strategy for delivering these natural products, ensuring enhanced bioavailability, precise targeting, controlled release, and protection against physical alterations. The escalating interest in nano-delivery of natural compounds is evident through the growing number of scientific publications in this field. This review goes beyond merely showcasing successful examples of nano-delivery systems containing natural products; it aims to underscore the untapped potential within pharmaceutical and nutraceutical markets. Commencing with an exploration of plant-derived natural products and the methodologies employed for obtaining nanoformulations, this work delves into nanoparticulate drug delivery systems designed for the skin, central nervous, skeletal, cardiovascular systems, and diabetes. Despite notable advancements in preparing nanomedicines featuring specific dietary polyphenols, research focused on crude extracts or standardized fractions remains limited. Many plants possessing well-documented therapeutic properties, as listed in pharmacopoeias, are yet to fully harness the benefits of nanotechnological advancements. This review emphasizes the significance of developing adequate nanoformulations, with the potential to elevate certain plants from dietary supplements to pharmaceutical status by improving their bioavailability and efficacy. The exploration of untapped opportunities within the nexus of natural compounds and nanomedicine is vital for advancing drug delivery systems and expanding the repertoire of therapeutic options
Formulation And Evaluation Of Mucoadhesive Buccal Films Of Enalapril Maleate
Nowadays, extensive research is being carried out on the design and development of innovative drug delivery systems to improve safety, efficacy, and patient compliance. One such delivery system is the buccal film technology. The buccal mucosa is the best-suited site for local, as well as systemic delivery of drugs due to its physiological features. The goal of designing oral mucoadhesive buccal film for the anti-hypertensive drug Enalapril maleate is to increase the bioavailability. The formulation and evaluation of oral mucoadhesive buccal films of Enalapril maleate by solvent casting method. The Enalapril maleate is an anti-hypertensive drug that has high first-pass metabolism and shows 40-60% of bioavailability. Due to this condition, we took this drug to convert into films, which increases its bioavailability by decreasing the first mass metabolism. The preparation contains different formulations by using different polymers like Hydroxypropyl methylcellulose E 5 (HPMC), Hydroxypropyl methylcellulose E 50 (HPMC), and different plasticizers like PEG 400 & PG. The films of physicochemical evaluations like thickness (0. 14±0.004 mm), tensile strength 120.23 (g/cm2), % Drug content uniformity (97.6± 1.040%), surface pH (6.74±0.051), the swelling index is in the optimum range, folding endurance ( 175±2), and diffusion studies showed the optimum release of drug in the predetermined time
Herbal remedies on post acne hyperpigmentation
One of the most prevalent skin problems is acne. Nearly all teenagers are affected, and up to 41% of adults may still have the condition. Regardless of skin tone, pigmentary consequences are significant cosmetic concerns for all patients, and they may cause the patient greater problems than the primary skin disorder did. Darker skinned people appear to have a higher likelihood of pigmentary disorders, which should be taken into account while examining these patients. Even mild to moderate acne might result in post-acne hyperpigmentation. Acne with hyperpigmentation manifests as dark patches or blotches on the skin. There are many cosmetic products available in the market that reduces hyperpigmentation, but it is best to look for herbal remedies that reduce dark spots. The aim of this study is to determine the importance of herbs for the treatment of post acne hyperpigmentation
Harnessing Medicinal Plant Phytochemicals: Unveiling Pharmacological Potential and Novel Drug Delivery Strategies
The significant progress in the field of anticancer research has spurred a growing interest in bioactive compounds with potential pharmacological properties. One well-established challenge in utilizing these natural bioactives is their inherent low solubility, leading to limited bioavailability and difficulties in formulating effective drug delivery strategies to specific target sites. In response to this challenge, this review provides a comprehensive overview of the latest advancements in the development of innovative drug delivery systems. Our analysis focuses on published data related to key plant secondary metabolites known for their potent anticancer potential, specifically the flavone, isoflavone, and stilbene groups, which have been successfully formulated using novel drug delivery systems. While the precise mechanisms of action for these selected natural compounds remain a subject of ongoing investigation, their anticancer effects are undeniable. Consequently, current research efforts are primarily dedicated to identifying these bioactive compounds' most effective delivery systems. Recent studies aim to elucidate the exact mechanisms of action and therapeutic benefits of these compounds and address the crucial issue of designing suitable natural compound delivery systems capable of efficiently transporting therapeutic doses to the intended target sites. This multifaceted approach underscores the ongoing commitment to advancing the field of anticancer research and improving the delivery of bioactive compounds with promising anticancer potential
The analgesic activity of novel synthesized tetrapeptides: overview
The tetrapeptide class of biased analgesics from an Australian fungus targets the -opioid receptor. The current study sought to investigate the analgesic and anti-inflammatory effects of Tyr-MIF-1 mimetics in rats suffering from acute pain. We report the synthesis of two new compounds which are hybrid molecules between the substituted pyrrole (Pyr) and analogues of Tyr MIF-1 peptide. The in vitro opioid activity of the analogs was tested in the guinea pig ileum (GPI) and naloxone-induced pain model. The study examined the effect of an analog to an N-terminal nociceptin fragment on the behavior of albino rats. We have also elucidated a novel G protein-biased agonist, Phe-Phe-Asp]NH2, for the management of moderate to severe acute pain following abdominoplasty. The pharmacophore based on Phe, NH2, was synthesised and characterized by solid phase chemistry and high performance liquid chromatography/mass spectrometry (HPLC/MS). The results show that a series of hybrid molecules with a unique stereochemical arrangement of hydrophobic amino acids, bilaids A-C, were synthesized. The effects of a new molecule, an analog of N-Terminal Nociceptinal Fragment (PK20M), on motor and exploratory activity of mature rats and in 42-day pups and 21-day rat pups were evaluated. The antinociceptive and antipyretic activities of the original molecule were evaluated in a model of post-incisional pain in rats at doses lower than 1g/kg. The present study reporting the overview of analgesic activity of some novel synthesized tetrapeptides fragments shows satisfaction effects comparing with morphine, aspirin, naloxone, etc
Antimicrobial activity of microwave assisted synthesized chalcones and conventional synthesized chalcones: an overview
A chalcone is a type of acetophenone in which one of the methyl hydrogens has been swapped out for a benzylidene group, making it a member of the class of chalcones. Kamboj*, et al has synthesized A fast and very rapid procedure is reported for the synthesis of chalcones from the ketones and aldehydes under microwave irradiation. All the synthesized compounds 1-28 were screened for their in vitro antibacterial and antifungal activities. All the compounds were tested for their antibacterial and antifungal activities by cup plate method. The structures of the compounds were confirmed by spectral data (infrared spectroscopy [IR] and 1H nuclear magnetic resonance [NMR]). All compounds showed excellent results against all fungi and are comparable to that of the standard antibiotic, Nystatin
Exploring the Drug delivery systems of Natural products on inflammation-mediated Disorders: a short Note
Advancements in diagnostic tools and clinical procedures have unveiled much about the causes and workings of these conditions. In vitro and in vivo experimental models have paved the way for numerous biomedical breakthroughs, notably in discovering potential drugs to tackle metabolic disorders. Natural compounds have garnered attention as promising candidates due to their antioxidant and anti-inflammatory properties, offering hope for managing conditions like diabetes, obesity, heart diseases, and cancer. Efforts are ongoing to enhance the effectiveness and availability of these compounds through specialized drug delivery methods. Our focus delves into the recent strides made in understanding how inflammatory responses kickstart metabolic disorders, especially in diabetes, obesity, heart diseases, and cancer. We explore the potential of natural products in combating these conditions and provide a roster of biological targets for efficient screening in drug development. Furthermore, we discuss insights gained from both preclinical and clinical studies, aiming to pinpoint optimal approaches for using phytochemical drug delivery systems in treating metabolic disorders. This comprehensive review aims to shed light on the latest developments and potential avenues in addressing the complexities of metabolic disorders through innovative drug strategies
Medication Errors - An Understated Healthcare Menace: A Journey Through A South-Indian Tertiary Care Facility
This research work targets to analyze and ascertain the epidemiological profile of medication errors occurred at a tertiary care hospital in South India. A retrospective cross-sectional investigation of medication errors by chart review method. The process involved assessment and interpretation of medication errors reported to and by the Department of Clinical Pharmacology from April 2016 to March 2020. Data was later analyzed employing descriptive statistics. A total of 11,314 medication errors [8,835 prescription errors and 2,479 non-prescription errors] were reported among 1,01,981 hospitalized patients, with an average incidence of 26.56 per 1000 patient days. More than a quarter of prescription errors were within the drug dosage modification subclass, whereas transcription errors were the most common non-prescription errors, around 70%. An appreciable portion of the total medication errors constituted by potential errors were prevented before reaching patients [9681, 85.56%] with timely interventions by health care professionals, remarkably by clinical pharmacists, over 96%. The study benchmarks how a well-designed voluntary reporting system provides a good way for identifying the emerging medication errors before they result in harm to the patients. Ward-based clinical pharmacists in close liaison with health care professionals are effective in reporting and implementing interventions to prevent such unfortunate events, ensuring patient safety
To study the organization of LDL-C/HDL-C ratio and inflammatory marker CRP in acute myocardial infarction
There is an increasing incidence of coronary artery disease in India. We therefore need a tool to evaluate the severity and prognosis of this acute myocardial infarction. In acute myocardial infarction, the function of plaque rupture and inflammation has already been identified. Aim: To study the organization of LDL-C/HDL-C ratio and inflammatory marker CRP in acute myocardial infarction. Methods and Material: Patients who have been diagnosed as acute myocardial infarction (ST Elevation Acute myocardial Infarction or Unstable angina/Non ST Elevation Myocardial Infarction) and admitted to ICCU of Rajiv Gandhi institute of Medical Sciences, Kadapa, AP. are the subjects. Sample consists of 100 cases of acute myocardial infarction. Case history was taken from the patients, and studied according to proforma. Conclusion: Elevated levels of CRP are independent indicators of adverse effects. When contrast with the LDL / HDL ratio, CRP is used for risk stratification and as a prognostic predictor. These findings suggest that in patients with acute myocardial infarction, raised CRP Levels is significant as compared to LDL/HDL ratio
SCREENING OF NOVEL AMINOPYRIMIDINE DERIVATIVES AGAINST HUMAN CDK-8 ENZYME: AN INSILICO APPROACH
The Human CDK8-CYCC in complex with compound 4: N-methyl-4-(4-pyridyl)-1H-pyrrole-2-carboxamide (PDB ID: 5XQX) was obtained from Protein Data Bank . These aminopyrimidine compounds are designed insilico with help of Chemsketch. The molecular docking study was performed using AutoDock vina software. The active binding site of the compounds were screened in the Biovia-2019.ds2019client. The pharmacokinetics and physiochemical properties were calculated in SwissADME. The toxicity of the compound is studied by using PreADME and PreTox-Ⅱ Prediction software.The designed compounds shows a better binding affinity than the standard drug 5-fluro uracil and based on the toxicity studies performed , the compounds are non-toxic in nature. This study leads to the development of novel aminopyrimidine derivatives as anticancer agent against Human cyclic dependent kinase (CDK-8) enzyme