Challenges and Advances in Pharmaceutical Research Vol. 5

The administration of Tenofovir (TDF) based (Tenofovir/Lamivudine/Efavirenz) antiretroviral regimen for the management of HIV has been associated with dyslipidaemia, which are associated cardiovascular-related complications, and reduced life expectancy. Through a randomised comparative trial, the study evaluated the effect of Moringa oleifera supplementation on metabolic abnormalities associated with HIV patients on TDF-based regimen. The RCT was a time dependent study that comprised of two arms (intervention TDF-M and control TDF-NM). Of the 140 recruited participants 56 were in the TDF-M group (administered Moringa Supplement) and 84 in the TDF-NM (control). At baseline, more than half of the patients showed aberrant atherogenic lipoprotein indices (Log [TC/HDL-C] = 85.7%; TC/HDL-C = 58.5% and LDL-C/HDL-C = 51.4%); albeit at lower levels. The prevalence of TDF-M participants at risk of CVD had reduced to 20% after 12 weeks of Moringa supplement administration, showing a remarkable (40.4 percent) decline, while the prevalence of TDF-NM subject at risk of CVD rose to 53.6% (x²=26.67, P<0.001). HIV patients on a TDF-based regimen who were at risk of CVD exhibited higher TGL and LDL levels, which had an inverse effect on HDL levels and a negative effect on atherogenic indices. The changes in proportion of TDF-M group were not significantly different from TDF-NM group after 4 weeks (visit 1); however, after 12 weeks (visit 2) of moringa administration, the subjects on Moringa had 4.67 [2.39 – 9.13] higher odds of normal API (x2[Yates]=24.688; P<0.001), 2.39 [1.58 – 3.60] higher odds of normal TC/HDL-c (x2[Yates]=16.879; P<0.001), and 2.09 [1.56 – 2.80] higher odds of normal LDL/HDL-c (x2[Yates]=23.388; P<0.001). The study observed marked changes in the atherogenic lipoprotein indices of both groups, with better indices for the TDF-NM group. This, therefore strengthens the advocacy for the inclusion of Moringa as dietary supplement for management of ART induced dyslipidaemia.

The objective of the present study is to formulate and evaluate omeprazole magnesium delayed release pellets by using drug layering technique with fluid bed processor for the treatment of acidity and ulcers.

Solubility studies were carried out by preparing saturated solutions of omeprazole magnesium in various non volatile solvents like methanol, ethanol, acetone, isopropanol and water and also to determine the solubility of drug in the solvents of purified water, pH 6.8 and pH 7.4 phosphate buffers. By adjusting the compositions of drug loading, barrier coating, and enteric coating by employing fluid bed processor, the formulation of delayed release pellets of omeprazole magnesium was developed. The effective release of the medicine takes place in 30 minutes due to the dissolving profile of formulation (F8), which contains an effective amount of hydroxypropyl cellulose-L and eudragit-L30 D55. To demonstrate that the improved formula was not incompatible with the drug and excipients, FTIR and DSC experiments were carried out. To understand the surface morphology of the pellets, SEM investigations were carried out. The enteric polymer eudragit, due to presence of an ester structure, were liable to hydrolysis in humid conditions, affecting the enteric protection in acid medium.

One of the most important pharmacokinetic processes is drug metabolism, which is crucial to medication development. The examination of the metabolite profile is essential because the metabolites produced may be helpful for therapy or cause major harm. The objective of this systematic review is to summarize the research articles relating to the metabolite profile investigation of conventional drugs and herb-derived compounds for cancer chemotherapy, to examine factors influencing metabolite profiling of these drugs/compounds and determine the relationship between therapeutic efficacy and toxicity of their metabolites. The literature search was performed through PubMed, and ScienceDirect searches up to January 2019. It was discovered that the creation of metabolites was influenced by four primary variables, including species, gender, drug administration route, and dose. There are certain metabolites that have been classified as hazardous or active.  This information is important for cancer chemotherapy and the development of anticancer drugs.  

Solanum torvum is a commonly used herb in traditional medicine. The aim of this study was to evaluate the effect of ethanol extract of Solanum torvum leaf on the liver of treated Wistar rats.  Freshly harvested leaves of S.torvum were shade dried and ground to fine powder. 500 g of powdered plant sample was macerated in ethanol for 72 hrs. Adult male Wistar rats weighing 150-200 g were admistered with extract. Animals were slaughtered, and then blood and tissue samples were taken, extracted, and analysed according to standard protocols. The findings of this study demonstrate that administration of an aqueous extract of S. torvum boosted liver enzyme activity as well as levels of total and conjugated bilirubin in a dose-dependent way. However, there was no difference between the 100 mg/kg of S. torvum extract and the control in terms of enzyme activity and the levels of conjugated and total bilirubin (P>0.05). It can be concluded that Solanum torvum which is conventionally considered safe for human consumption could be hepatotoxic at high doses.

This study aims to evaluate pregabalin's impact on post-operative pain control and osteoarthritis (OA) patients' quality of life (QOL) following total knee arthroplasty.

This prospective observational study was carried out at the orthopaedics department. Two groups of 96 patients each were created. Nonsteroidal anti-inflammatory drugs (NSAIDs) are used to treat 50 patients in Group A, while pregabalin is used to treat 46 patients in Group B. The visual analogue scale (VAS) and knee injury and OA outcome score (KOOS) questionnaires were administered to the study participants once every 60 days over the course of six months. By comparing the follow-up score to the baseline score, the treatment's impact was evaluated. Nonsteroidal anti-inflammatory drugs (NSAIDs) are often considered to be the preferred first-line treatment for OA.

The study's findings revealed that the pain score of Group Bin VAS at the end of the study was2.56±0.34 and the KOOS pain score was 92.73±3.45 (p<0.01). The QOL score was improved significantly to 81.56±5.29 (p<0.01) as compared to Group A. The research found that pregabalin with NSAIDs group patients showed a better improvement in pain, symptoms, and QOL within a short duration as compared to NSAIDs alone used group

The purpose of the study is to design and assess topical gel-loaded fluconazole niosomes. A macrolide antibiotic, fluconazole is used to treat a variety of sensitive bacteria. Niosomes can improve the penetration of drugs into the skin, and further increase the residence time of drug in the stratum corneum and epidermis, while reducing the systemic uptake of the drug. Niosomes play an important function in medication delivery because they can lower toxicity and alter pharmacokinetics and bioavailability.

The investigation was conducted to confirm that the sample is a pure drug. Fourier transform infrared (FTIR 8400s, Shimadzu Japan) spectra obtained for Fluconazole (pure drug) was checked. Potassium bromide disc method was used. 

Optimized formulations FNS5 and FNT4 prepared with Span-60 and Tween-60 exhibited vesicle sizes of 845.6 nm and 164.2 nm, zeta potential -10.2 mV and -46.4 mV indicating the formulation has good stability. The optimized niosomes were integrated into carbopol 934 and guar gum gels and then extensively characterized for zeta potential and vesicle size.

The study concluded that drug entrapment in niosomes resulted in increased drug release time, penetration, and retention.

Epilepsy is a global public health issue requiring a global response. Epilepsy is present everywhere and affects people of various ages, genders, ethnicities, and social backgrounds, regardless of geographical locations. The epileptic state is typically caused by excessive cortical neuron discharge in the cortical region of the brain. The first step toward a proper epilepsy diagnosis, course of treatment, and prognosis is understanding the classification of epileptic episodes. Specific drugs or surgical techniques frequently work better on particular seizure types or disorders. Multidrug resistant syndrome and refractory epilepsy are the biggest challenge in treatment of epilepsy, they lead to defect access of Anti-Epileptic Drugs AEDs to their target in CNS. Moreover, the marketed drugs carry severe side effects such as drowsiness, hepatotoxicity, anemia, and teratogenicity. There is a pivotal need to discover more safe and effective drugs. Quinazolinones analogues represent molecules which are capable of binding at multiple sites with high affinity and facilitate more rapid discovery of useful medicinally active compounds. Numerous scientists from all around the world have created a number of novel quinazolinone derivatives that have been virtually screened and tested for their ability to treat various forms of seizures. They will play a crucial role in the future treatment of epilepsy.