Indonesian Journal of Pharmacy
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Effectiveness of Dry Grinding and Wet Grinding Methods on Physicochemical Properties, Solubility, and Dissolution Rate of Nimodipine-HPMC Nanoparticles
Get PDFNimodipine is a dihydropyridine calcium channel blocker that shares the general properties of nifedipine, but acts mainly on cerebral blood vessels. Nimodipine belongs to the Class II Biopharmaceutical Classification System (BCS) drug group, which has low solubility and high permeability. The purpose of this study was to look at the differences in the yield of nanoparticles between the dry grinding and wet grinding methods on the physicochemical properties, solubility, and dissolution rate of nimodipine nanoparticles. The nanoparticles were prepared a nimodipine: HPMC ratio of 1:0.6 using two different methods. Sample characterization was carried out using Particle Size Analyzer (PSA), Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), and Fourier Transform Infrared (FT-IR). The Solubility test was carried out in CO2-free distilled water and the dissolution rate was carried out in phosphate buffer pH 7.2. The solubility of pure nimodipine in CO2-free distilled water was 0.339 µg/mL, the physical mixture was 1.948 µg/mL, the dry grinding nanoparticles were 3.367 µg/mL, and the wet grinding nanoparticles were 19.952 µg/mL. The dissolution test results obtained with the percentage of pure nimodipine dissolution at 60th minutes was 33.947%, the physical mixture was 39.482%, the dry grinding nanoparticles were 49.798%, and the wet grinding nanoparticles were 56.484%. Based on the results of the study, it can be said that the nimodipine-HPMC nanoparticles significantly increased the solubility and dissolution rate of nimodipine
Impact of Gene Polymorphism on Pharmacokinetics and Pharmaco-dynamics of Calcium Channel Blockers: A Narrative Review
Get PDFA class of drugs known as calcium channel blockers (CCBs) is used to treat hypertension, angina, and arrhythmias. There are two subcategories of this medication class: dihydropyridines and non-dihydropyridines. Studies on CYP3A5*3, AGTR1 rs275653, ABCB1 (MDR1) rs1045642, and POR*28 A503V have all investigated the effects of SNPs on CCBs. This study will carry out more research to ascertain which SNPs have the most influence on the effectiveness of CCBs. The narrative reviews in this article come from a variety of sources. We performed searches in Pubmed, ScienceDirect, and Google Scholar using the terms "calcium channel blocker," "efficacy," "blood pressure response," "pharmacokinetic," and "polymorphism" OR "genetic" OR "genomic" to find pertinent articles. When prescription antihypertensive medications, particularly calcium channel blockers, it is important to take into account certain gene variants for example CYP3A5*3/*3, CYP3A4 *1G/*1G, MDR1 C3435T , RyR3 gene rs877087 because of their considerable effects
Bioactivity Profiles of Actinobacterium Strain BTA 1-131 (InaCC A1205) Isolated from Indonesian Sponge Melophlus sarassinorum
Get PDFThe phylum Actinobacteria recognized as the most promising producers of many bioactive compounds. Among actinobacteria, the genus Streptomyces are widely known as prolific producers of many antibiotics, for example Streptomycin. The present study investigates potential bioactivity of actinobacteria BTA 1-131 isolated from an Indonesian marine sponge Melophlus sarassinorum. Molecular identification using the 16S rRNA gene sequencing showed that the isolate is similar to Streptomyces kunmingensis (98.4%). The isolate was cultivated on to three different fermentation media (ISP2, YS, and SYP) to select the best media for bioactive compounds production. The compounds were extracted from both solid and liquid cultures using methanol as a solvent. The crude methanol extracts were tested for antibacterial and anticancer activity. The bioactivity screening indicates active potential of the extracts against bacterial pathogen Staphylococcus aureus ATCC 13420, invasive breast cancer MDA-MB-231 and human colorectal adenocarcinoma cells CaCo-2. The extracts profiling using LC-MS/MS method indicates probable influence among different fermentation media to selectively induce production of target bioactive compounds. Although further compounds dereplication and fractionation are important for specific identification, the present study demonstrates the potential of Streptomyces BTA 1-131 as producer of tetracycline and/or staurosporine. In addition to that, further genome-mining approach and analysis using a whole genome sequencing data also important to comprehensively explore the bioactive potential of the actinobacteria BTA 1-131.
 
The The Enzalutamide and EPI-001 Modulate Cell Proliferation and Metastasis Markers in T47D by Targeting AR/ARV7
No full textAndrogen receptor (AR) and its splicing variant 7 (ARv7) play vital roles in the pathobiology of breast cancer (BC) but their role in the estrogen receptor-positive (ER+) type is controversial. Hence, we studied the influence of the blockers of AR (Enzalutamide) and ARv7 (EPI-001) on tumorigenesis processes using T47D, an ER+ BC cell line. Several techniques were employed: Sulphorhodamine assay (SRB), Flow cytometry, Immunostaining, Scratch wound healing assay, Enzyme Linked Immunosorbent assay (ELISA), and Western blot. Mechanistically, the drugs successfully arrested the cell cycle at S-phase and downregulated the protein expression of cyclins A, E, & C. Additionally, they inhibited the cell proliferation stimulator nuclear factor kappa B (NF-ĸB), whereas only EPI-001 reduced the cell regulatory marker c-Myc. They also opposed the endothelial-to-mesenchymal transition (EMT) process, by boosting the epithelial marker E-cadherin and reducing the protein expression of the mesenchymal marker fibronectin. Their anti-metastatic potential was evidenced by the hindrance of cell migration using the wound healing assay and further confirmed by the downregulation of metalloproteinase (MMP) 2 and 9 protein expression, and protein content of Rho kinase (ROCK)1 and 2. Besides, by downregulating the protein expression of vascular endothelial growth factor (VEGF) the drugs point to their anti-angiogenic aptitude. In conclusion, this in-vitro study highlights the importance of targeting AR/ARv7 using Enzalutamide and EPI-001 in decreasing proliferation cell markers, EMT, and metastasis in ER+ BC cells, findings that may have great impact in the treatment of ER+ BC
Five flavonoids from Lucerne (Medicago sativa L.) varieties
No full textAlfalfa (Medicago sativa L., Fabaceae) is knowed as perennial herbaceous leguminous plant species that originated in southwestern Asia and used as folk medicine for the treatment of various ailments. The upperground part of Lucerne contain phenolic compound such as flavonoids etc., that contributes to its biological activities. The aim of this study was to determine five widely knowing flavonoids in extracts 20 alfalfa varieties herb at the Ukrainian steppe growing. We selected 50 seeds of the same size from twenty alfalfa cultivars from different countries, were cultivated under controlled areas of southern part of the Ukrainian left-bank at border of forest-steppe and steppe zones (Zaporizhzhya, Ukraine) from April to June, with 15 °C/ 07 °C (day/night), 14 h/10 h (light/dark) and 60–65% relative humidity. The content of flavonoids were found unequable in ethanol extracts. The chemical compositions and their content were assessed by ultrahigh-performance liquid chromatography. The content of five flavonoids were different in the 20 alfalfa varieties raw materials. Umbelliferone were found high in ethanol extract of Mongolian colorful hybrid (Mongolia, 0,23 mg|g). Four sorts have not contained umbelliferone: Кisvardai (Hungary), Nizona (Cuba), Тanhuato (Mexico) and Mesopotamian (Iraq). The leader from cinaroside content was sort Commercial 2-52-75 of UK origin. Routine has been found in the highest quantities in WL 50 from USA. Ferganska 700 from Uzbekistan was leader in luteolin content and Кisvardai, Hungary was leader in average of kaempferol content (0,030 mg|g). The present article comprises the hierarchical cluster analyses from the data flavonoid assay
Impact of Educational Interventions in Therapy Programs for People with Schizophrenia (PwS): A Systematic Review
Get PDFNot only antipsychotics but additional interventions such as education for people with schizophrenia are also needed to support optimal therapy. Studies with educational interventions have been conducted and show varied outcomes. The systematic review aimed to summarize and evaluate the effectiveness of studies regarding educational interventions for people with schizophrenia. Two electronic databases (PubMed and Science Direct) were used to find studies with criteria that were educational interventions for people with schizophrenia and focused on outcome measures related to improving knowledge, medication adherence, and other outcomes as an effect of educational interventions, randomized or randomized controlled trial studies, published between 2012 and 2022. The manual search of referenced articles was also applied. A literature search was conducted using the terms ("people with schizophrenia" OR "patients with schizophrenia") AND ("education" OR "knowledge") AND ("medication adherence" OR "medication compliance" OR "medication persistence"). Of the 666 studies, seven were eligible. Some educational interventions are part of a therapy program, while others are full psychoeducational programs that target not only the patient but also the patient's family. There was only one study that used counseling supported by leaflets delivered by a pharmacist. Another intervention used face-to-face interviews and discussions supplemented by modules or booklets, or giving booklets to patients and then following up by phone. Only one of the seven studies was effective in increasing patient knowledge. The rest did not measure knowledge but assessed other parameters, i.e., stigma and insight, symptoms, social functioning, relapse rate, or quality of life as the effect of educational intervention. Three studies showed a significant difference in improvement in medication adherence between the intervention and control groups; two studies were not significant, and the rest were unmeasured. It can be concluded that educational intervention had a positive effect on PwS and their families’ knowledge, improved medication adherence, and other outcomes as an effect of the educational intervention
Alginate-ZnO-Poly(ethylene glycol) Dimethacrylate (PEGDMA) via Interpenetrating Polymer Network as a Functional Material for Wound Dressing
Get PDFAlginate is a biopolymer that has been widely applied as a wound dressing material. To increase the mechanical and antibacterial properties of a wound dressing material, nanoparticles and synthetic polymers are used to modify alginate. One of the materials synthesized into nanoparticles is ZnO, which has potential applications in the medical field because of its good antibacterial properties. On the other hand, PEGDMA has not been widely used in the medical field, opening opportunities to develop research, especially regarding wound dressing materials. However, there has never been a detailed report on the modification of alginate using ZnO and PEGDMA. In this paper, alginate was modified using ZnO and poly(ethylene glycol) dimethacrylate (PEGDMA; alginate–ZnO–PEGDMA, AZP), which was synthesized using the Interpenetrating Polymer Network (IPN) method. AZP can increase a wound dressing material’s mechanical properties by 78% and the antibacterial properties by 94%, which indicates that alginate modification with ZnO and PEGDMA produces high-performance wound dressing materials
Screening Herbal Compound Candidates for Use as Anti-Inflammatory Drugs for COVID-19 Treatment Using Deep Semisupervised Learning
Get PDFCOVID-19 is a disease caused by the SARS-CoV-2 virus. Its symptoms include cough, fever, shortness of breath, and acute inflammation (hyperinflammation), and severe cases can lead to death. These symptoms tend to worsen if inflammation is not controlled. This research aims to build a stacked autoencoder deep neural network (SAE-DNN) model for identifying herbal compound candidates that can be used as anti-inflammatory drugs for COVID-19 treatment. The model’s performance is evaluated on the basis of different data representations. The research process involves data collection, data preprocessing, modeling, and testing the model on the herbal data to obtain herbal compound candidates. Results indicate that the developed SAE-DNN model with compound representation that combines fingerprints and dipeptide composition produces the best performance with an accuracy of 0.96722, a recall of 0.96419, area under the receiver operating characteristic of 0.99596, and an F1 score of 0.96567. A total of 33 herbal compounds are found as candidate anti-inflammatory drugs by using the SAE-DNN model
Assessing Quality of Self-Medication Services in Pharmacies in Bandung, West Java, Indonesia using a Mystery Customer Approach
Get PDFSelf-medication practice is currently increasing in global population. Apart from the benefits, it is undeniable that self-medication can also have several negative impacts. The outcome of self-medication is affected by pharmacist’s clinical ability to provide self-medication services to the patient. This study was aimed to assess the quality of self-medication services in Indonesia using mystery customer approach. A pilot project had been conducted in Bandung, West Java, Indonesia. Mystery customers act as patients who come to the pharmacy seeking self-medication medications for cough/common cold, diarrhea/constipation, pain/fever, and gastritis cases. A total 232 pharmacies were involved in this study and selected through stratified random sampling. The quality of self-medication services was measured by four subdomains: patient assessment, the accuracy of drug selection, the drug information provided to mystery customer, and lifestyle modification counselling. Result showed that patient assessment regarding signs and symptoms only performed by 42,82% pharmacies in Bandung, 14,44% assessed pharmacological and nonpharmacological therapy prior to visit, and only 10,56% assessed patients’ specific medical condition. Although the percentage of patient assessment performed by pharmacies in Bandung were low, interestingly the accuracy of drug selection is relatively high (85,34%). The most prevalent information provided to patient was instruction to consume the medication (59,09%), meanwhile the least delivered information was about side effect (5,17%). Information about lifestyle modification only delivered by 10,34% pharmacies. The quality of self-medication services in Bandung varies depending on the type of pharmacy and service provider. State-owned pharmacy has a higher overall score of self-medication service than private retail pharmacy and private standalone pharmacy (p<0,05). Based on the service provider, pharmacist have a higher score of self-medication service compared to pharmacy technicians and other personnel in pharmacies (p<0,05). This study emphasizes the importance of the pharmacist’s role in self-medication services to ensure rational and safe treatment for patients
Persistence to Antihypertensive and Clinical Outcomes in Acute Coronary Syndrome Patients after Percutaneous Coronary Intervention
Get PDFAcute coronary syndrome (ACS) is a life-threatening condition that carries a high risk of recurrent cardiovascular events and death. Persistence to treatment is known to reduce disease morbidity and mortality in patients with ACS. In this study, we focus on ACS patients undergoing their first percutaneous coronary intervention (PCI) to investigate the association between persistence to antihypertensive therapy and clinical outcomes. A retrospective cohort study with two years of follow-up was conducted with 367 patients recruited. Patients were deemed as having the persistence to antihypertensive therapy (C02, C03, C07, C08, C09) if the gap between prescriptions was ≤ 30 days. The clinical outcomes are defined as a composite of major adverse cardiac event (MACE), major adverse cardiovascular and cerebrovascular events (MACCE), myocardial infarction, recurrent PCI, stroke, all-cause death, cardiovascular death, and hospitalization. Cumulative persistence to antihypertensive showed 72.3% of ACS patients still taking antihypertensive one year after PCI. Persistence to treatment with antihypertensive therapy can be used as a predictor of MACE or MACCE because it was associated with recurrent PCI (RR 1.94, 95% CI = 1.02-3.71). Our study indicates that among ACS patients undergoing their first PCI, non-persistence to antihypertensive therapy may lead to worse clinical outcomes. This data will be useful to promote secondary prevention in ACS patients after PCI