Formulation and Evaluation of Lipid Based Nanoparticles of Etravirine

Engineered nanoparticles have the potential to revolutionize the diagnosis and treatment of many diseases like HIV/AIDS. Etravirine is one of the key components of highly active antiretroviral therapy used for the treatment of HIV-1 infections. The aim of the present study was to formulate and evaluate nanostructured lipid carriers of etravirine, intended for targeted delivery to macrophages, using solvent emulsification - evaporation technique.  Estimates of drug solubility were employed for selection of solid lipids, liquid lipids and stabilizers for the preparation of NLCs. Design of experiments was used to optimize the formulation with respect to drug-lipid ratio and concentration of stabilizer in the external phase using 32 full factorial design. Particle size of the carriers and drug release characteristics were the responses which were set to suitable levels for optimization. The optimized formulation was prepared and characterized for size, poly dispersity index, zeta potential, entrapment efficiency and appearance. The nanostructured lipid carriers of etravirine were prepared using stearylamine and glyceryl monostearate as solid lipids, Capryol 90 as liquid lipid and polyvinyl pyrrolidone as stabilizer. All experimental batches showed high drug loading efficiencies nearing 99%, indicating that etravirine remained closely associated with the lipids. The nanostructured lipid carriers displayed a zeta potential of -10.1 mv and a particle size of 261.6 nm with a polydispersity index of 0.374. In vitro release of etravirine from the optimized formulation at 2 h was 9% indicative of a low burst; and 56% of the entrapped drug was released after 24 h, suggesting prolonged release characteristics. Thus, etravirine loaded lipidic nanoparticles with potential for targeting cellular reservoirs of the AIDS virus such as macrophages were successfully developed. Keywords: Etravirine, Nanostructured lipid carriers, full factorial desig

Unveiling the Mode of Action of Dravya Vikalpa

Shodhana-shamana is one of the treatment classifications in Ayurveda. Medicines for Shodhana can be administered in single drug or combination form. The explanation regarding formulations has been dealt in Ayurveda. Though single drugs have been indicated in various disorders, they may fail to target every stage of disease and may therefore fail in treatment. Thus, the permutation and combination of drugs can act efficiently and target every stage of disease. In the Charaka Samhita Chikitsasthana, shodhana yogas are briefly described for specific ailments, however in the Kalpasthana, dravyavikalpa are extensively explained for shodhana. It is difficult to understand choice of dravyavikalpa as there is no direct description on mode and site of action of yogas mentioned. Hence there is a need for proper understanding of the mode and site of action of various dravyavikalpa. Understanding a specific combination and its kalpana helps one understand how medicines are targeted at vitiated doshas and sthanasamshraya. To illustrate the same, Dravyavikalpa for panduroga mentioned in Charaka Samhita Kalpasthana has been taken as an example. In this study an effort will be made to analyze mode and site of action of Dravyavikalpa mentioned in Charaka Samhita Kalpasthana. Keywords: Dravyavikalpa, kalpana vishesha, pandu rog

Current practices in the veterinary use of antibiotics in poultry laying hens in Friguiagbé (Guinea)

The use of antibiotic molecules on poultry farms, while justified by their efficacy, must be carried out rationally, as their uncontrolled use modifies the ecology of bacteria and thus contributes to the selection of multi-resistant bacteria.  The aim of this study was to carry out a descriptive survey of antibiotic use on laying hen farms in the sub-prefecture of Friguiagbé (Kindia). To achieve this, surveys were carried out among veterinary service managers, poultry farmers and sales outlets. At the end of our work, we identified the existence of two (2) veterinary pharmaceutical supply establishments. Establishments selling veterinary medicines revealed that Tetracycline is the most widely marketed antibiotic family. The most widely used antibiotic molecules are Tetracolivit and Oxytetracycline (26%); Neoxyvital (13%); Alfaceryl and Panteryl (8%); Limoxin (5%); Enrofloxacin, TTS, Colisol and Amoxillin (3%), which are used either for preventive or curative purposes. Keywords : Antibiotic molecules, poultry farming, laying hens, Guine

Risk factors for Undiagnosed Kidney Disease among Stable First-Degree Relatives of Chronic Kidney Disease Patients at Nnamdi Azikiwe University Teaching Hospital, Nnewi, South Eastern Nigeria

Background: Chronic kidney disease (CKD) is a global public health problem and has a major impact on health and cost of health care. In Nigeria, renal replacement therapy (RRT) is funded out of pockets by patients and their relatives unlike in most developed countries. There is a high clustering of the risk factors for CKD in FDRs of CKD patients, making then an ideal population for the screening for and the reversal of the modifiable risk factors that predispose to CKD. Objective: This study determined the risk factors for CKD in the FDRs of patients Methodology: This study involving 300 subjects: 150 FDRs of CKD patients and 150 control subjects without personal or family history of CKD. The study and control subjects were screened for CKD using urine albumin creatinine ratio (uACR) and estimated glomerular filtration rate (eGFR). Prevalence rate of the risk factors for CKD such as hypertension, diabetes mellitus, obesity, dyslipidaemia, hyperuricaemia and life style practices like significant smoking and heavy alcohol consumption were determined for both the FDRs and the control subjects. Data was analyzed with SPSS version 21.0. Mann-Whitney U test was used for comparing the variables between the two study groups for continuous variables that were not normally distributed and Chi square tests for categorical variables. Results: The prevalence rate of dyslipidaemia and hyperuricaemia was significantly higher among the FDRs of CKD patients compared with the control subjects (26% versus 12%; P = 0.003) and (20.7% versus 7.3%; P = 0.001) respectively. The other risk factors for CKD that included hypertension, diabetes mellitus, obesity, significant cigarette smoking, heavy alcohol consumption and herbal medication use were equally more among the FDRs of CKD patients compared with the controls, although not statistically significant. Conclusion: The risk factors for CKD were common among FDRs of CKD patients. Screening for these risk factors at the earliest possible contact with the FDRs of CKD patients and taking appropriate actions to tackle the modifiable ones will prevent the development of CKD and retard the progression of the already existing disease, reduce the alarming global burden of CKD.&nbsp

Effects of Intravenous Lidocaine as an Analgesic Adjuvant in Oncological Pain

Objectives: To verify that intravenous lidocaine is effective as an adjuvant analgesic in pain for hospitalized cancer patients at the National Institute of Cancerology, Mexico. Methods: Clinical records of patients hospitalized at the National Institute of Cancerology who received intravenous lidocaine infusion as an adjuvant to pain during the 4-year period from November 1, 2019, to October 31, 2023, were reviewed. Patients who met inclusion and exclusion criteria were included. A statistically significant measure was defined as a decrease equal to or greater than 4 points in the NRS value after lidocaine administration. Results: A total of 179 patients were included; 46.4% were men, and 53.6% were women. The most common painful syndrome was somatic (54%). Patients with neuropathic pain received a higher lidocaine dose (mg/kg/hr) of 1.9 ± 0.79. Regarding adverse effects, 1.7% of patients experienced them. It was established that a reduction of 4 points with respect to the previous value on the numeric rating scale (NRS) would be considered statistically significant. A statistically significant association was found between patients under 38 years old and a higher risk of not achieving the objective (p 0.05, CI 0.95–1 OR 0.9). Patients who received lidocaine infusions for less than 4.63 days also had a risk of not reaching the goal (p 0.02, CI 0.7–0.9, OR 0.8). Conclusions: This study demonstrated that the analgesic adjuvant use of intravenous lidocaine infusion is an effective and well-tolerated analgesic intervention for oncology patients. Keywords: lidocaine, Neuropathic Pain, Somatic Pain, Visceral Pain, numeric rating scale

Phytochemicals properties and antimicrobial activities of Carica papaya and Balanites aegyptiaca’ seeds aqueous infusion and decoction extracts

Carica papaya and Balanites aegyptiaca seeds extract have several uses, from food to traditional medicine. This study aims to determine their phytochemicals compound and appreciate their antimicrobial properties against clinical strains. Polyphenolic content was determined with standard methods while DPPH radical scavenging activity is used to appreciate the antioxidant properties, using ascorbic acid as standard. Antimicrobial activities were performed according to the inhibition diameters, using agar diffusion method. Minimum inhibitory concentrations and Minimum fungicidal concentrations were established based on broth dilution methods. The extraction yield is ranged between 6.3 and 20.3%. The results shown polyphenolic content varying from 1256.13±21.09 to 2315.81±53.52 µg GAE/100 mL for Carica papaya and from 303.98±0.93 to 948.06±3.23 µg GAE/100 mL for Balanites aegyptiaca while the antioxidant activity is ranged between 31.76±2.35 and 58.47±4.24 µg AEAC/100 mL for Carica papaya and from 29.80±0.32 to 78.44±2.81 µg AEAC/100 mL for Balanites aegyptiaca. Infusion’s extracts always have the highest values of polyphenols content and antioxidant activity than decoction extracts, be it papaya or balanites seeds. Neitheir flavonoids content nor antibacterial activity was found. The inhibition diameter varies from 14.5±0.5 to 40.5±0.5 mm for papaya seeds extracts and from 16.5±0.5 to 21.0±0.5 mm for balanites seeds extracts without a significative effect of mixture for both extracts. MICs vary from 11.71±0.1 to 75.0±0.0 mg. mL-1 for Carica papaya seeds extracts with 11.72±0.2 to 37.30±0.2 mg. mL-1 and 18.74±0.1 to 100±0.0 mg.mL-1 for Balanites aegyptiaca. Mixture extracts presented intermediaire values. Decoction extracts have lowest MICs values and infusion reveals itself to be the sweetable aqueous extraction techniques but the appropriate infusion time need to be highlight. Keywords: Carica papaya, Balanites aegyptiaca, Seeds extracts, Phytochemical, antifunga

Adult Onset Still’s Disease in a Patient with Fever of Unknown Origin: A Rare Case

Adult onset Still’s disease (AOSD) is a rare clinical entity with unknown etiology, characterized by arthritis, fever, evanescent rash, and other systemic presentations. AOSD generally does not overlap with other rheumatic diseases. AOSD is a diagnosis by exclusion, and it is one of the common causes of pyrexia of unknown origin (PUO) which can be life-threatening if mistreated. Although steroids are the first line of therapy, about 20%-30% of patients are refractory, intolerant, and or relapse during tapering or upon discontinuation of steroids. There are no clinical guidelines in treating such patients, which is challenging. Keywords:  Still’s disease, arthritis, fever, auto-inflammator

A Case Report on Iatrogenic Cushing Syndrome with Diabetes Mellitus

Cushing syndrome (CS) is a condition caused due to high levels of cortisol in which weight gain and fat tissue build-up take place. Generally, patients with Cushing syndrome also suffer from diabetes. A 57-year-old female patient with aggravated cortisol levels. Laboratory investigations of the patient were performed and they showed decreased haemoglobin levels, but increased vitamin B12 levels, and TSH levels. The patient was prescribed a combination of medications to manage anemia, anemia, and diabetes. The patient's medical history included splenomegaly, cholelithiasis, panniculitis, and kidney enlargement. The patient's diabetes was responding well to the treatment and was better after 10 days. Keywords: Cushing syndrome, Diabetes mellitus, corticosteroid

Ethanolic Stem-Bark Extract of Blighia unijugata Possesses Anti-Hyperglycemic and Anti-Hyperlipidemic Activity in a Streptozotocin-Induced Diabetes Model

Introduction: The global rise in the incidence of diabetes mellitus, particularly type 2 diabetes mellitus (T2DM), and its associated complications have become a public health threat. Besides hyperglycemia, hyperlipidemia has been associated with diabetes due to the defect in insulin secretion and/or action. Medicinal plants are being investigated to discover drug alternatives with better efficacies, lesser adverse effects, and cost-effectiveness. This work investigated the anti-hyperglycemic and anti-hyperlipidemic activity of ethanolic stem bark extract of Blighia unijugata (EBU) in streptozotocin (STZ)-induced diabetic Sprague- Dawley (SD) rats. Method: T2DM was induced in male SD rats by a single intraperitoneal injection of STZ (50 mg/kg in 0.1 M citrate buffer, pH 4.5) and confirmed 72 hours later. EBU (100 and 200 mg/kg) and glibenclamide (5 mg/kg) were administered orally to the diabetic rats (n = 5) for 28 days. The effect of the treatments on fasting blood glucose (FBG), lipid profile, atherogenic predictor indices, and body weight were assessed. Results: EBU treatments significantly reduced (p≤0.001) elevated blood glucose, total cholesterol, triglycerides, and Very Low-Density Lipoprotein cholesterol (VLDL-c, p≤0.001) but increased High-Density Lipoprotein cholesterol (HDL, p≤0.05) compared to the diabetic control. Also, all the atherogenic risk predictor indices were significantly reduced (p≤0.001). In addition, EBU treatment mitigated the significant weight loss (p≤0.01) associated with the diabetic state when compared to the normal control. Conclusion: These findings first report the anti-hyperglycemic, anti-hyperlipidemic, and anti-atherogenic properties of the stem bark of ethanolic extract of Blighia unijugata, and can be further studied and used as an anti-diabetic and anti-hyperlipidemic agent. Keywords: Blighia unijugata; hyperglycemia; atherogenic index; hyperlipidemia; diabete

Experimental animal models for gastric ulcer / peptic ulcer: An overview

In the present study we have discussed around sixteen different animal models used worldwide for the scientific research and new drug discovery.  The main aim of the using experimental animal models in drug discovery is to establish and provide evidence for non-clinical 'proof-of-concept' for the safety, efficacy, and target of interest for specific drug molecules. Experimental preparations developed in one species for the purpose of studying phenomena occurring in another species. The use of experimental animal models serves to better understand the origins, pathology, and the overall nature of comparable diseases of humans being. Similarly, animal models perform duties for in the development of safe and effective treatments and cures of such diseases and/or associated symptoms. Experimental animal models for drug discovery and development have played a major role in the characterization of the pathophysiology of diseases and associated mechanisms of injury, drug target identification, and evaluation of novel therapeutic agents for toxicity, pharmacokinetics and pharmacodynamics activity. Through animal model researchers can perform experiments that would be impractical or ethically prohibited with humans. There are various animal models used for screening of uncountable therapeutic activities, in this review our main focus is animal models used for peptic ulcer. Peptic ulcer is one of the worldwide diseases where 10% of adults are affected by peptic ulcer once in their lifetime. The antiulcer models for drug development against gastric and duodenal ulcer studies are limited in number that has hindered the progress of targeted therapy in this field. Therefore, it is necessary to review the literature on experimental animal models that are used to screen agents with potential anti-gastric ulcer activity and describe their biochemical basis in order to facilitate their use in the development of new preventive and curative antiulcer drugs. There are many models used to induce ulcer such as pylorus ligation or it can be chemically induced by ethanol, NSAIDs (e.g. indomethacin) or many more. In this review paper, current in-vivo animal models of ulcers and the pathophysiological mechanisms underlying their induction, their drawbacks, as well as the challenges associated with their use have been discussed