Raymond R Tjandrawinata, Antonius H Cahyana, Ajeng O Nugroho, Indra K Adi, Joseph S R Talpaneni
{"title":"Structure Identification and Risk Assurance of Unknown Impurities in Pramipexole Oral Drug Formulation.","authors":"Raymond R Tjandrawinata, Antonius H Cahyana, Ajeng O Nugroho, Indra K Adi, Joseph S R Talpaneni","doi":"10.1155/2024/5583526","DOIUrl":"10.1155/2024/5583526","url":null,"abstract":"<p><p>Impurities compounds in any pharmaceutical product or drug substance are inevitable from a chemistry point of view. The quality and safety of a pharmaceutical product are also significantly affected by these impurities content; therefore, impurities need to be identified and characterized through the use of appropriate analytical methods. Pramipexole is a nonergot dopamine agonist used to treat various Parkinson's disease symptoms. Two unknown impurities were detected from a pramipexole dihydrochloride solid dosage form. These impurities were identified and characterized using ultra-performance liquid chromatography coupled with high-resolution mass spectroscopy (UPLC-HRMS). These impurities were found to be enriched when mannitol existed in the formulation. The structure and mechanism involved in the existence of the impurities were proposed. Furthermore, observation of the binding affinity potential risk of these impurities to the pramipexole receptor has also been demonstrated through molecular docking and molecular dynamics simulation study. The binding energy result showed that pramipexole interaction with dopamine receptors D2 and D3 was higher than pramipexole mannose adduct and pramipexole ribose adduct.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2024 ","pages":"5583526"},"PeriodicalIF":2.8,"publicationDate":"2024-02-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10878758/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139911801","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Simon Nyarko, Kwabena Ofori-Kwakye, Raphael Johnson, Noble Kuntworbe, Desmond Asamoah Bruce Otu, Denis Dekugmen Yar, Yaa Asantewaa Osei
{"title":"Development of the RP-HPLC Method for Simultaneous Determination and Quantification of Artemether and Lumefantrine in Fixed-Dose Combination Pharmaceutical Dosage Forms.","authors":"Simon Nyarko, Kwabena Ofori-Kwakye, Raphael Johnson, Noble Kuntworbe, Desmond Asamoah Bruce Otu, Denis Dekugmen Yar, Yaa Asantewaa Osei","doi":"10.1155/2024/3212298","DOIUrl":"10.1155/2024/3212298","url":null,"abstract":"<p><p>Developing countries face enormous challenges with substandard and falsified antimalarial drugs. One specific issue is the lack of a simple, cost-effective, and robust HPLC method to simultaneously determine and quantify the active pharmaceutical ingredients (APIs) in fixed-dose artemether-lumefantrine pharmaceutical dosage forms. The current study developed a novel, simple, sensitive, precise, accurate, and cost-effective RP-HPLC method for the simultaneous determination and quantification of artemether and lumefantrine in pharmaceutical dosage forms. The HPLC analysis was carried out on an Agilent 1260 Infinity Series HPLC system equipped with an ODS Intersil-C8 (150 × 4.6 mm) 5.0 <i>µ</i>m column, by isocratic elution. The mobile phase composition consisted of acetonitrile and 0.05% orthophosphoric acid buffer of pH 3.5 in the ratio of 70 : 30 v/v. The analysis was performed at a 1 mL/min flow rate and a column temperature of 25°C. The total run time was 6 minutes. The detection was done with a variable wavelength detector (VWD) at an isosbestic point wavelength (<i>λ</i>) of 210 nm. The developed method was validated according to the ICH guidelines concerning system suitability, specificity, linearity, accuracy, precision, and robustness. The system suitability of the developed method revealed satisfactory theoretical plates and symmetry factors. The method proved to be specific, with no interference of mobile phase or excipients. The calibration plot exhibited linearity over the concentration range of 275-1925 <i>μ</i>g/mL with <i>R</i><sup>2</sup> = 0.9992 for artemether and a range of 150-1050 <i>μ</i>g/mL with <i>R</i><sup>2</sup> = 0.9985 for lumefantrine. The accuracy of the method, determined by the recovery study, was 99.79-100.16% for artemether and 99.04-99.50% for lumefantrine. The % RSD values for intraday precision were 0.175 and 0.203, while interday precision values were 0.340 and 0.554 for artemether and lumefantrine, respectively. The method demonstrated robustness when subjected to slight modifications in the flow rate, column temperature, and mobile phase composition. The developed analytical method proved satisfactory as per ICH guidelines and hence can be used for the determination and quantification of artemether and lumefantrine in bulk drug and pharmaceutical dosage forms.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2024 ","pages":"3212298"},"PeriodicalIF":2.8,"publicationDate":"2024-02-07","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10866635/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139734200","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
M. Ahmed, E. Ameyaw, F. A. Armah, P. Fynn, I. Asiamah, G. Ghartey-Kwansah, F. Zoiku, E. OFORI-ATTAH, C. K. Adokoh
{"title":"Alkaloidal Extracts from Avicennia africana P. Beauv. (Avicenniaceae) Leaf: An Antiplasmodial, Antioxidant, and Erythrocyte Viable","authors":"M. Ahmed, E. Ameyaw, F. A. Armah, P. Fynn, I. Asiamah, G. Ghartey-Kwansah, F. Zoiku, E. OFORI-ATTAH, C. K. Adokoh","doi":"10.1155/2024/4541581","DOIUrl":"https://doi.org/10.1155/2024/4541581","url":null,"abstract":"Background. The emergence of drug-resistant parasites impedes disease management and eradication efforts. Hence, a reinvigorated attempt to search for potent lead compounds in the mangroves is imperative. Aim. This study evaluates in vitro antiplasmodial activity, antioxidant properties, and cytotoxicity of A. africana leaf alkaloidal extracts. Methods. The A. africana leaves were macerated with 70% ethanol to obtain a total crude extract. Dichloromethane and chloroform-isopropanol (3 : 1, v/v) were used to extract the crude alkaloids and quaternary alkaloids from the total crude. The antiplasmodial activities of the alkaloidal extracts were performed against 3D7 P. falciparum chloroquine-sensitive clone via the SYBR Green I fluorescence assay with artesunate serving as the reference drug. The alkaloidal extracts were further evaluated for antioxidant properties via the total antioxidant capacity (TAC), the total glutathione concentration (GSH), the DPPH (2,2-diphenyl-1-picrylhydrazyl) assay, and the ferric-reducing antioxidant power (FRAP) methods. The cytotoxic activity of the alkaloidal extracts was tested on erythrocytes using a 3-(4,5-dimethylthiazol-2-yl)-5-diphenyltetrazolium bromide-MTT assay with little modification. The phytocompounds in the alkaloidal extracts were identified via gas chromatography-mass spectrometry (GC-MS) techniques. Results. The total crude extract showed good antiplasmodial activity (IC50 = 11.890 µg/mL). The crude and quaternary alkaloidal extracts demonstrated promising antiplasmodial effects with IC50 values of 6.217 and 6.285 µg/mL, respectively. The total crude and alkaloidal extracts showed good antioxidant properties with negligible cytotoxicity on erythrocytes with good selectivity indices. The GC-MS spectral analysis of crude alkaloidal extracts gave indole and isoquinoline alkaloids and several other compounds. Dexrazoxane was found to be the main compound predicted, with an 86% peak area in the quaternary alkaloidal extract. Conclusion. The crude and quaternary alkaloidal extracts exhibited antiplasmodial activities and ability to inhibit oxidative stress with negligible toxicity on erythrocytes. This may be good characteristics to avoid oxidative stress related to Plasmodium infection in the treatment of malaria.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"14 10","pages":""},"PeriodicalIF":2.8,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139441610","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Rita Ayuk Ndip, Joelle Ngo Hanna, James Ajeck Mbah, Stephen Mbigha Ghogomu, Moses Njutain Ngemenya
{"title":"<i>In Vitro</i> Synergistic Activity of Combinations of Tetrahydroisoquinolines and Treatment Antibiotics against Multidrug-Resistant <i>Salmonella</i>.","authors":"Rita Ayuk Ndip, Joelle Ngo Hanna, James Ajeck Mbah, Stephen Mbigha Ghogomu, Moses Njutain Ngemenya","doi":"10.1155/2023/6142810","DOIUrl":"10.1155/2023/6142810","url":null,"abstract":"<p><p>The global burden of <i>Salmonella</i> infections remains high due to the emergence of multidrug resistance to all recommended treatment antibiotics. Tetrahydroisoquinolines (THIQs) have demonstrated promising activity against multidrug-resistant (MDR) <i>Salmonella</i> Typhi. Hence, their interaction with treatment antibiotics was investigated for possible synergy. Twenty combinations of five THIQs (<b>1</b>, <b>2</b>, <b>3</b>, <b>4,</b> and <b>5</b>) and four antibiotics were tested against each of 7 <i>Salmonella</i> isolates by the checkerboard method giving a total of 140 assays performed. Fractional inhibitory concentration indices (FICIs) were calculated, and isobolograms were plotted. In terms of FICI, synergism ranged from 0.078 to 0.5 and the highest magnitude (0.078) was recorded for chloramphenicol-THIQ <b>1</b> combination. In a total of 140 antibiotics-THIQs combination assays, 27 were synergistic (17%), 42 were additive (30%), 11 were antagonistic (7.8%), and 60 were indifferent (42%). The synergistic activity recorded for each antibiotic class in combination based on the total of 7 bacterial isolates tested ranged from 14.29% to 71.43%; the highest percentage was recorded for two combinations (chloramphenicol or sulphamethoxazole with THIQ <b>1</b>). Ciprofloxacin-THIQ <b>1</b> combination showed additivity on all bacteria isolates tested (100%). Overall, THIQ <b>1</b> was the most synergistic and most additive in combination with three antibiotics (ampicillin, chloramphenicol, or sulphamethoxazole-trimethoprim). Some combinations of the THIQs and treatment antibiotics have shown high synergism which could potentially be efficacious against multidrug-resistant <i>S.</i> Typhi, hence this interaction should be further studied <i>in vivo</i>.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"6142810"},"PeriodicalIF":2.8,"publicationDate":"2023-12-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10733592/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138827595","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
S. Chemmalar, A. R. I. Shameha, Che Azurahanim, Che Abdullah, Nor Asma, Ab Razak, L. M. Yusof, M. Ajat, Kim Wei Chan, Md Zuki, Abu Bakar Zakaria
{"title":"Busting the Breast Cancer with AstraZeneca's Gefitinib","authors":"S. Chemmalar, A. R. I. Shameha, Che Azurahanim, Che Abdullah, Nor Asma, Ab Razak, L. M. Yusof, M. Ajat, Kim Wei Chan, Md Zuki, Abu Bakar Zakaria","doi":"10.1155/2023/8127695","DOIUrl":"https://doi.org/10.1155/2023/8127695","url":null,"abstract":"Breast cancer is the most common cancer diagnosed in women, and in 2020, there were 684, 996 deaths due to this disease. Epidermal growth factor receptors (EGFRs) and their respective ligands have been blamed for the pathogenesis and resistance to treatment in specific breast cancer cases. With EGFR having four homologues: EGFR1, EGFR2, EGFR3, and EGFR4, in-depth understanding of EGFR biology led to the discovery of small-molecule inhibitors and antibodies against this receptor. Gefitinib (GEF), a tyrosine kinase inhibitor of EGFR1, possesses a vast potential for treatment against breast cancer and is supported by a multiplicity of experiments. Unfortunately, in clinical trials, GEF did not show the outcomes expected with complete response and disease progress. This is due to incomplete understanding of the molecular mechanisms involved in EGFR signaling and endocrine sensitivity. Hence, additional in-depth experiments are needed regarding various molecular pathways and crosstalk pathways to comprehend GEF's action mechanism thoroughly in breast cancer patients. In this review, the role of EGFR in the development and pathogenesis of breast cancer and the pharmacokinetics and pharmacotherapy of GEF for the treatment of breast cancer have been elaborated. Nanomedicines synthesized with GEF have shown positive experimental response, paving a promising path for GEF against breast cancer.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"17 9","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138602810","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Laila M. Najia, Eric Pyles, Arnaldo Lopez-Ruiz, Bibidh Subedi
{"title":"Antistaphylococcal Efficacy of Cefepime, Meropenem, and Piperacillin-Tazobactam in Patients with Polymicrobial Infection with MSSA Bacteremia or Pneumonia","authors":"Laila M. Najia, Eric Pyles, Arnaldo Lopez-Ruiz, Bibidh Subedi","doi":"10.1155/2023/7684613","DOIUrl":"https://doi.org/10.1155/2023/7684613","url":null,"abstract":"There is a paucity of literature describing de-escalation techniques in patients with polymicrobial infections with one offending organism being methicillin-susceptible Staphylococcus aureus (MSSA) being treated with β-lactam therapy. The purpose of this study is to determine treatment outcomes for patients with polymicrobial infections with MSSA bacteremia or pneumonia who are treated with cefepime (FEP), meropenem (MEM), or piperacillin-tazobactam (TZP). This trial design represents a retrospective observational three-group comparison study of patients at a community teaching hospital system. Patients reviewed included those who had a MSSA bacteremia or pneumonia in addition to a confirmed polymicrobial infection or presence of a coinfection and received definitive therapy with FEP, MEM, or TZP. The primary outcome is defined as the resolution of fever of ≥100.4°F, hypothermia (≤95°F), leukocytosis (WBC °>° 12,000 cells/mm3), and leukopenia with WBC °<° 4,000 cells/mm3. Secondary outcomes included duration of definite therapy, in-hospital mortality, hospital and ICU length of stay (LOS), 30-day readmission rates for a presumed infection, and hospital-acquired Clostridioides difficile infection (HCDI). From August 1, 2016, to August 30, 2019, 45 patients met eligibility criteria. There were no observed differences in primary endpoint (p = 0.65) or secondary endpoints, i.e., in-hospital mortality (p = 0.10), hospital LOS (p = 0.75), ICU LOS (p = 0.53), 30-day readmission rates for presumed infection (p = 0.07), or HCDI (p = 0.34). There was no difference in treatment success with FEP, MEM, or TZP for polymicrobial infections with one offending organism being MSSA. Due to the lack of evidence in this unique patient population and observed results of our study, randomized studies are warranted to determine appropriate therapy in this complex patient population.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"115 18","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138607597","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Yan-Ding Su, Xinyi Wei, Q. Cheng, He Qi, Jianghui Chen, Xiang-jun Qiu
{"title":"Exploring the Effect of Compound Glycyrrhizin and Silybinin on the Metabolism of Pexidartinib in Rats Based on CYP3A4 and CYP2C9","authors":"Yan-Ding Su, Xinyi Wei, Q. Cheng, He Qi, Jianghui Chen, Xiang-jun Qiu","doi":"10.1155/2023/6737062","DOIUrl":"https://doi.org/10.1155/2023/6737062","url":null,"abstract":"Pexidartinib offered a new therapeutic option for adult patients with symptomatic tenosynovial giant cell tumor (TGCT) who were refractory to surgical treatment and had severe morbidity or functional limitations. Meanwhile, the metabolism of pexidartinib was mainly mediated through the oxidation of cytochrome P450 (CYP) 3A and glucuronidation by uridine glucuronosyltransferase (UGT) 1A4 and attention shall be paid to CYP450-based drug-drug interactions during therapeutic dosing. This study aimed to examine the changes in the pharmacokinetics of pexidartinib by silymarin and compound glycyrrhizin on pexidartinib in vivo in rats by high-performance liquid chromatography (HPLC)-UV approach and to detect its expression in CYP3A4 and CYP2C9 using the western blot. The findings of chromatography experiments revealed that silybinin as well as compound glycyrrhizin increased the exposure of pexidartinib in rats and had a significant inhibitory effect on the metabolism of pexidartinib. The results of immunoblotting assays suggested that silybinin as well as compound glycyrrhizin inhibited the protein expression of CYP3A4 and CYP2C9 in rats. Therefore, the combination of pexidartinib with silybinin and compound glycyrrhizin should be monitored to avoid clinical adverse effects.","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"110 3","pages":""},"PeriodicalIF":2.8,"publicationDate":"2023-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138608482","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Janinne Ortega-Montiel, Alejandra Montoya, René Soria-Saucedo, Katia Gallegos-Carrillo, Paula Ramírez-Palacios, Jorge Salmerón, Eduardo Salazar-Martínez
{"title":"Trends of Antihypertensive, Antidiabetic, and Nonsteroidal Anti-Inflammatory Drugs Use among the Health Workers Cohort Study, Mexico 2004 to 2018.","authors":"Janinne Ortega-Montiel, Alejandra Montoya, René Soria-Saucedo, Katia Gallegos-Carrillo, Paula Ramírez-Palacios, Jorge Salmerón, Eduardo Salazar-Martínez","doi":"10.1155/2023/5555274","DOIUrl":"10.1155/2023/5555274","url":null,"abstract":"<p><strong>Background: </strong>Hypertension and type 2 diabetes (T2D) are the most prevalent noncommunicable diseases in Mexico and worldwide. According to international practice management guidelines, the principal chronic management therapy is daily oral medication.</p><p><strong>Aim: </strong>We aim to describe the trends of antihypertensive, antidiabetic, and nonsteroidal anti-inflammatory (NSAID) drugs use among the Mexican adult population from 2004-2018.</p><p><strong>Methods: </strong>We analyzed data from the Health Workers Cohort Study (HWCS) for males and females aged >18 years. We calculated the prevalence of chronic diseases and utilization for every kind of antihypertensive, antidiabetic, and NSAIDs (measured by self-reported utilization) at baseline and two follow-ups (2004, 2010, and 2017). Trends were analyzed using Fisher's exact test.</p><p><strong>Results: </strong>Hypertension prevalence increased from 19.8 to 30.3%, higher than T2D prevalence from 7.0 to 12.8% through fourteen years of follow-up. Like the self-reported dual therapy, the proportion of patients using beta-blockers and angiotensin II receptor blockers increased. Regarding T2D, the prevalence of metformin utilization increased to 83.9%. The utilization of common NSAIDs, mainly for muscular pain, remained around 13 to 16%.</p><p><strong>Conclusions: </strong>Our findings showed a changing prevalence of drug utilization for hypertension and T2D between 2004 and 2018 and consistent use of NSAIDs in the adult Mexican population.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"5555274"},"PeriodicalIF":2.1,"publicationDate":"2023-11-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10684324/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457176","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"Enhancement of Liver Targetability through Statistical Optimization and Surface Modification of Biodegradable Nanocapsules Loaded with Lamivudine.","authors":"Srikar Grandhi, Moawia Al-Tabakha, Prameela Rani Avula","doi":"10.1155/2023/8902963","DOIUrl":"https://doi.org/10.1155/2023/8902963","url":null,"abstract":"<p><p>The intention of the current work was to develop and optimize the formulation of biodegradable polymeric nanocapsules for lamivudine (LMV) in order to obtain desired physical characteristics so as to have improved liver targetability. Nanocapsules were prepared in this study as aqueous-core nanocapsules (ACNs) with poly(lactide-co-glycolide) using a modified multiple emulsion technique. LMV was taken as a model drug to investigate the potential of ACNs developed in this work in achieving the liver targetability. Three formulations factors were chosen and 3<sup>3</sup> factorial design was adopted. The selected formulation factors were optimized statistically so as to have the anticipated characteristics of the ACNs viz. maximum entrapment efficiency, minimum particle size, and less drug release rate constant. The optimized LMV-ACNs were found to have 71.54 ± 1.93% of entrapment efficiency and 288.36 ± 2.53 nm of particle size with zeta potential of -24.7 ± 1.2 mV and 0.095 ± 0.006 h<sup>-1</sup> of release rate constant. This optimized formulation was subjected to surface modification by treating with sodium lauryl sulphate (SLS), which increased the zeta potential to a maximum of -41.6 ± 1.3 mV at a 6 mM concentration of SLS. The results of <i>in vivo</i> pharmacokinetics from blood and liver tissues indicated that hepatic bioavailability of LMV was increased from 13.78 ± 3.48 <i>μ</i>g/mL <i>∗</i> h for LMV solution to 32.94 ± 5.12 <i>μ</i>g/mL <i>∗</i> h for the optimized LMV-ACNs and to 54.91 ± 6.68 <i>μ</i>g/mL <i>∗</i> h for the surface-modified LMV-ACNs.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"8902963"},"PeriodicalIF":2.8,"publicationDate":"2023-11-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10676277/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457175","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Leonardo da Rocha Sousa, Nildomar Ribeiro Viana, Angélica Gomes Coêlho, Celma de Oliveira Barbosa, Débora Santos Lula Barros, Maria do Carmo de Carvalho E Martins, Ricardo Martins Ramos, Daniel Dias Rufino Arcanjo
{"title":"Use of Monoterpenes as Potential Therapeutics in Diabetes Mellitus: A Prospective Review.","authors":"Leonardo da Rocha Sousa, Nildomar Ribeiro Viana, Angélica Gomes Coêlho, Celma de Oliveira Barbosa, Débora Santos Lula Barros, Maria do Carmo de Carvalho E Martins, Ricardo Martins Ramos, Daniel Dias Rufino Arcanjo","doi":"10.1155/2023/1512974","DOIUrl":"https://doi.org/10.1155/2023/1512974","url":null,"abstract":"<p><p>Monoterpenes are secondary metabolites of plants belonging to the terpenoid class of natural products. They are the most abundant components of essential oils that are generally considered to have various pharmacological properties. These compounds are reported to have antidiabetic effects in recent years. Due to nature's complex biosynthetic machinery, they also exhibit a reasonable degree of structural complexity/diversity for further analysis in structure-activity studies. Therefore, monoterpenes as antidiabetic agents have been investigated by recent in vitro and in vivo studies extensively reported in the scientific literature and claimed by patent documents. The purpose of this survey is to provide a comprehensive and prospective review concerning the potential applications of monoterpenes in the treatment of diabetes. The data for this research were collected through the specialized databases PubMed, Scopus, Web of Science, and ScienceDirect between the years 2014 and 2022, as well as the patent databases EPO, WIPO, and USPTO. The research used 76 articles published in the leading journals in the field. The main effect observed was the antidiabetic activity of monoterpenes. This review showed that monoterpenes can be considered promising agents for prevention and/or treatment of diabetes as well as have a marked pharmaceutical potential for the development of bioproducts for therapeutics applications.</p>","PeriodicalId":7369,"journal":{"name":"Advances in Pharmacological and Pharmaceutical Sciences","volume":"2023 ","pages":"1512974"},"PeriodicalIF":2.8,"publicationDate":"2023-11-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10665111/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"138457177","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}