keyword
https://read.qxmd.com/read/38543294/liposome-based-drug-delivery-systems-in-cancer-research-an-analysis-of-global-landscape-efforts-and-achievements
#21
JOURNAL ARTICLE
Islam Hamad, Amani A Harb, Yasser Bustanji
Lipid-bilayer-based liposomes are gaining attention in scientific research for their versatile role in drug delivery. With their amphiphilic design, liposomes efficiently encapsulate and deliver drugs to targeted sites, offering controlled release. These artificial structures hold great promise in advancing cancer therapy methodologies. Bibliometric research analyzes systematic literary data statistically. This study used bibliometric indicators to examine, map, and evaluate the applications of liposomes in cancer therapy...
March 14, 2024: Pharmaceutics
https://read.qxmd.com/read/38543286/amide-to-triazole-switch-in-somatostatin-14-based-radioligands-impact-on-receptor-affinity-and-in-vivo-stability
#22
JOURNAL ARTICLE
Xabier Guarrochena, Panagiotis Kanellopoulos, Anna Stingeder, Lisa-Maria Rečnik, Irene V J Feiner, Marie Brandt, Wolfgang Kandioller, Theodosia Maina, Berthold A Nock, Thomas L Mindt
The use of metabolically stabilized, radiolabeled somatostatin (SST) analogs ([68 Ga]Ga/[177 Lu]Lu-DOTA-TATE/TOC/NOC) is well established in nuclear medicine. Despite the pivotal role of these radioligands in the diagnosis and therapy of neuroendocrine tumors (NETs), their inability to interact with all five somatostatin receptors (SST1-5 R) limits their clinical potential. [111 In]In-AT2S is a radiolabeled DOTA-conjugate derived from the parent peptide SST-14 that exhibits high binding affinity to all SSTR subtypes, but its poor metabolic stability represents a serious disadvantage for clinical use...
March 13, 2024: Pharmaceutics
https://read.qxmd.com/read/38543282/exploring-variability-in-rifampicin-plasma-exposure-and-development-of-anti-tuberculosis-drug-induced-liver-injury-among-patients-with-pulmonary-tuberculosis-from-the-pharmacogenetic-perspective
#23
JOURNAL ARTICLE
Agnija Kivrane, Viktorija Ulanova, Solveiga Grinberga, Eduards Sevostjanovs, Anda Viksna, Iveta Ozere, Ineta Bogdanova, Maksims Zolovs, Renate Ranka
Genetic polymorphisms can exert a considerable impact on drug pharmacokinetics (PK) and the development of adverse drug reactions (ADR). However, the effect of genetic polymorphisms on the anti-tuberculosis (anti-TB) drug, and particularly rifampicin (RIF), exposure or anti-TB drug-induced liver injury (DILI) remains uncertain. Here, we evaluated the relationship between single nucleotide polymorphisms (SNPs) detected in the RIF pharmacogenes ( AADAC , SLCO1B1 , SLCO1B3 , ABCB1 , and NR1I2 ) and RIF PK parameters, as well as anti-TB treatment-associated DILI...
March 12, 2024: Pharmaceutics
https://read.qxmd.com/read/38543281/validated-lc-ms-ms-assay-for-the-quantitative-determination-of-fenretinide-in-plasma-and-tumor-and-its-application-in-a-pharmacokinetic-study-in-mice-of-a-novel-oral-nanoformulation-of-fenretinide
#24
JOURNAL ARTICLE
Cristina Matteo, Isabella Orienti, Adriana Eramo, Ann Zeuner, Mariella Ferrari, Alice Passoni, Renzo Bagnati, Marianna Ponzo, Ezia Bello, Massimo Zucchetti, Roberta Frapolli
We describe the development and validation of a HPLC-MS/MS method to assess the pharmacokinetics and tumor distribution of fenretinide, a synthetic retinoid chemically related to all-trans-retinoic acid, after administration of a novel oral nanoformulation of fenretinide, called bionanofenretinide (BNF). BNF was developed to overcome the major limitation of fenretinide: its poor aqueous solubility and bioavailability due to its hydrophobic nature. The method proved to be reproducible, precise and highly accurate for the measurement of the drug and the main metabolites...
March 12, 2024: Pharmaceutics
https://read.qxmd.com/read/38543278/weekly-oral-tenofovir-alafenamide-protects-macaques-from-vaginal-and-rectal-simian-hiv-infection
#25
JOURNAL ARTICLE
Ivana Massud, Kenji Nishiura, Susan Ruone, Angela Holder, Chuong Dinh, Jonathan Lipscomb, James Mitchell, George M Khalil, Walid Heneine, J Gerardo Garcίa-Lerma, Charles W Dobard
Pre-exposure prophylaxis (PrEP) with a weekly oral regimen of antiretroviral drugs could be a suitable preventative option for individuals who struggle with daily PrEP or prefer not to use long-acting injectables. We assessed in macaques the efficacy of weekly oral tenofovir alafenamide (TAF) at doses of 13.7 or 27.4 mg/kg. Macaques received weekly oral TAF for six weeks and were exposed twice-weekly to SHIV vaginally or rectally on day 3 and 6 after each dose. Median TFV-DP levels in PBMCs following the 13...
March 11, 2024: Pharmaceutics
https://read.qxmd.com/read/38543277/metformin-mediated-improvement-in-solubility-stability-and-permeability-of-nonsteroidal-anti-inflammatory-drugs
#26
JOURNAL ARTICLE
Qi An, Cheng Xing, Zhipeng Wang, Shuang Li, Wenwen Wang, Shiying Yang, Linglei Kong, Dezhi Yang, Li Zhang, Guanhua Du, Yang Lu
Nonsteroidal anti-inflammatory drugs (NSAIDs) are class II biopharmaceutics classification system drugs. The poor aqueous solubility of NSAIDs can lead to limited bioavailability after oral administration. Metformin (MET), a small-molecule compound, can be used in crystal engineering to modulate the physicochemical properties of drugs and to improve the bioavailability of orally administered drugs, according to the literature research and preliminary studies. We synthesized two drug-drug molecular salts (ketoprofen-metformin and phenylbutazone-metformin) with NSAIDs and thoroughly characterized them using SCXRD, PXRD, DSC, and IR analysis to improve the poor solubility of NSAIDs...
March 11, 2024: Pharmaceutics
https://read.qxmd.com/read/38543269/forecasting-fetal-buprenorphine-exposure-through-maternal-fetal-physiologically-based-pharmacokinetic-modeling
#27
JOURNAL ARTICLE
Matthijs W van Hoogdalem, Ryota Tanaka, Khaled Abduljalil, Trevor N Johnson, Scott L Wexelblatt, Henry T Akinbi, Alexander A Vinks, Tomoyuki Mizuno
Buprenorphine readily crosses the placenta, and with greater prenatal exposure, neonatal opioid withdrawal syndrome (NOWS) likely grows more severe. Current dosing strategies can be further improved by tailoring doses to expected NOWS severity. To allow the conceptualization of fetal buprenorphine exposure, a maternal-fetal physiologically based pharmacokinetic (PBPK) model for sublingual buprenorphine was developed using Simcyp (v21.0). Buprenorphine transplacental passage was predicted from its physicochemical properties...
March 8, 2024: Pharmaceutics
https://read.qxmd.com/read/38543252/modeling-pharmacokinetics-in-individual-patients-using-therapeutic-drug-monitoring-and-artificial-population-quasi-models-a-study-with-piperacillin
#28
JOURNAL ARTICLE
Gellért Balázs Karvaly, István Vincze, Michael Noel Neely, István Zátroch, Zsuzsanna Nagy, Ibolya Kocsis, Csaba Kopitkó
Population pharmacokinetic (pop-PK) models constructed for model-informed precision dosing often have limited utility due to the low number of patients recruited. To augment such models, an approach is presented for generating fully artificial quasi-models which can be employed to make individual estimates of pharmacokinetic parameters. Based on 72 concentrations obtained in 12 patients, one- and two-compartment pop-PK models with or without creatinine clearance as a covariate were generated for piperacillin using the nonparametric adaptive grid algorithm...
March 4, 2024: Pharmaceutics
https://read.qxmd.com/read/38543242/preclinical-and-early-clinical-development-of-tenofovir-alafenamide-elvitegravir-topical-inserts-for-effective-on-demand-vaginal-and-rectal-hiv-prevention
#29
JOURNAL ARTICLE
M Melissa Peet, Vivek Agrahari, Meredith R Clark, Gustavo F Doncel
HIV/AIDS remains a global public health issue, and products available for the prevention of HIV infections are limited, especially those for short-acting, on-demand, user-controlled applications. Topical inserts are products that can be applied vaginally or rectally and have been explored as drug delivery systems. To fill the gap in the HIV prevention product pipeline, CONRAD has developed a topical insert containing tenofovir alafenamide fumarate (TAF) and elvitegravir (EVG), two potent and synergistic antiretrovirals, as a simple, low-cost, and discreet option that can be self-administered vaginally and/or rectally, before and after coitus...
March 1, 2024: Pharmaceutics
https://read.qxmd.com/read/38543236/conjugated-linoleic-acid-carboxymethyl-chitosan-polymeric-micelles-to-improve-the-solubility-and-oral-bioavailability-of-paclitaxel
#30
JOURNAL ARTICLE
Iqra Mubeen, Ghulam Abbas, Shahid Shah, Abdullah A Assiri
Oral delivery, the most common method of therapeutic administration, has two significant obstacles: drug solubility and permeability. The challenges of current oral medicine delivery are being tackled through an emerging method that uses structures called polymeric micelles. In the present study, polymeric micelles were developed using conjugates of linoleic acid-carboxymethyl chitosan (LA-CMCS) for the oral delivery of paclitaxel (PCL). The developed micelles were evaluated by particle size, zeta potential, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA)...
February 28, 2024: Pharmaceutics
https://read.qxmd.com/read/38543234/interaction-of-klaklak-nh-2-and-analogs-with-biomimetic-membrane-models
#31
JOURNAL ARTICLE
Victoria Vitkova, Krassimira Antonova, Ognyan Petkov, Angelina Stoyanova-Ivanova, Sirine Jaber, Vladislava Ivanova, Emilia Naydenova, Dancho Danalev
BACKGROUND: Specifically designed peptide mimetics offer higher selectivity regarding their toxicity to mammalian cells. In addition to the α-helix conformation, the specific activity is related to the peptide's ability to penetrate the cell membrane. The alterations in lipid membrane properties were addressed in the presence of the peptide KLAKLAK-NH2 and analogs containing β-alanine, strengthening the antibacterial activity and/or naphtalimide with proven anticancer properties...
February 28, 2024: Pharmaceutics
https://read.qxmd.com/read/38543228/pharmacokinetic-modeling-of-bepotastine-for-determination-of-optimal-dosage-regimen-in-pediatric-patients-with-allergic-rhinitis-or-urticaria
#32
JOURNAL ARTICLE
Sukyong Yoon, Byung Hak Jin, Choon Ok Kim, Kyungsoo Park, Min Soo Park, Dongwoo Chae
Bepotastine, a second-generation antihistamine for allergic rhinitis and urticaria, is widely used in all age groups but lacks appropriate dosing guidelines for pediatric patients, leading to off-label prescriptions. We conducted this study to propose an optimal dosing regimen for pediatric patients based on population pharmacokinetic (popPK) and physiologically based pharmacokinetic (PBPK) models using data from two previous trials. A popPK model was built using NONMEM software. A one-compartment model with first-order absorption and absorption lag time described our data well, with body weight incorporated as the only covariate...
February 27, 2024: Pharmaceutics
https://read.qxmd.com/read/38543226/advancing-precision-medicine-a-review-of-innovative-in-silico-approaches-for-drug-development-clinical-pharmacology-and-personalized-healthcare
#33
REVIEW
Lara Marques, Bárbara Costa, Mariana Pereira, Abigail Silva, Joana Santos, Leonor Saldanha, Isabel Silva, Paulo Magalhães, Stephan Schmidt, Nuno Vale
The landscape of medical treatments is undergoing a transformative shift. Precision medicine has ushered in a revolutionary era in healthcare by individualizing diagnostics and treatments according to each patient's uniquely evolving health status. This groundbreaking method of tailoring disease prevention and treatment considers individual variations in genes, environments, and lifestyles. The goal of precision medicine is to target the "five rights": the right patient, the right drug, the right time, the right dose, and the right route...
February 27, 2024: Pharmaceutics
https://read.qxmd.com/read/38543213/pharmacokinetic-interaction-of-kratom-and-cannabidiol-in-male-rats
#34
JOURNAL ARTICLE
Erin C Berthold, Shyam H Kamble, Siva Rama Raju Kanumuri, Michelle A Kuntz, Alexandria S Senetra, Yi-Hua Chiang, Sushobhan Mukhopadhyay, Christopher R McCurdy, Abhisheak Sharma
Kratom and cannabidiol products are used to self-treat a variety of conditions, including anxiety and pain, and to elevate mood. Research into the individual pharmacokinetic properties of commercially available kratom and cannabidiol products has been performed, but there are no studies on coadministration of these products. Surveys of individuals with kratom use history indicate that cannabidiol use is one of the strongest predictors of both lifetime and past month kratom use. The purpose of this study was to determine if there are changes in pharmacokinetic properties when commercially available kratom and cannabidiol products are administered concomitantly...
February 24, 2024: Pharmaceutics
https://read.qxmd.com/read/38543208/ranibizumab-port-delivery-system-in-neovascular-age-related-macular-degeneration-where-do-we-stand-overview-of-pharmacokinetics-clinical-results-and-future-directions
#35
REVIEW
Matteo Mario Carlà, Maria Cristina Savastano, Francesco Boselli, Federico Giannuzzi, Stanislao Rizzo
The ranibizumab (RBZ) port delivery system (PDS) is a device designed to continuously deliver RBZ in the vitreous chamber for the treatment of neovascular age-related macular degeneration (nAMD). It is implanted during a surgical procedure and can provide sustained release of the medication for several months. This review, updated to January 2024, focuses on past clinical studies as well as current and forthcoming trials looking into a PDS with RBZ. In the phase 2 LADDER trial, the mean time to first refill of a PDS with RBZ 100 mg/mL was 15...
February 23, 2024: Pharmaceutics
https://read.qxmd.com/read/38543198/limits-of-detection-of-topically-applied-products-in-the-skin-using-in-vivo-raman-spectroscopy
#36
JOURNAL ARTICLE
Cláudio Nico, Tom C Bakker Schut, Peter J Caspers, Gerwin J Puppels
We have developed a method to determine the limit of detection (LoD) for quantitative measurement of exogenous analytes in the outer layer of the human skin by in vivo confocal Raman spectroscopy. The method is in accordance with the guidelines of the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use that have been adopted by regulatory authorities such as the American Food and Drug Administration and the European Medicines Agency. The method can be applied in silico so that the limit of detection can be assessed before starting a skin penetration study, for example, in areas of pharmaceutical formulation, pharmacokinetics, or toxicokinetics...
February 22, 2024: Pharmaceutics
https://read.qxmd.com/read/38543175/cytotoxic-and-antiproliferative-activity-of-lassbio-2208-and-the-attempts-to-determine-its-drug-metabolism-and-pharmacokinetics-in-vitro-profile
#37
JOURNAL ARTICLE
Raysa Magali Pillpe-Meza, Wesley Leandro Gouveia, Gisele Barbosa, Carlos A M Fraga, Eliezer J Barreiro, Lidia Moreira Lima
Inappropriate expression of histone deacetylase (HDAC-6) and deregulation of the phosphatidylinositol 3-kinase (PI3K) signalling pathway are common aberrations observed in cancers. LASSBio-2208, has been previously described as a dual inhibitor in the nanomolar range of HDAC-6 and PI3Kα and is three times more potent in inhibiting HDAC-6. In this paper we described the cytotoxic and antiproliferative potency of LASSBio-2208 on different tumour cell lines, its possible synergism effect in association with PI3K and HDAC-6 inhibitors, and its drug metabolism and pharmacokinetics (DMPK) in vitro profile...
March 18, 2024: Pharmaceuticals
https://read.qxmd.com/read/38543162/new-pyrazolyl-thioureas-active-against-the-staphylococcus-genus
#38
JOURNAL ARTICLE
Anna Maria Schito, Debora Caviglia, Susanna Penco, Andrea Spallarossa, Elena Cichero, Bruno Tasso, Chiara Brullo
To meet the urgent need for new antibacterial molecules, a small library of pyrazolyl thioureas (PTUs) was designed, synthesized and tested against difficult-to-treat human pathogens. The prepared derivatives are characterized by a carboxyethyl functionality on C4 and different hydroxyalkyl chains on N1. Compounds 1a - o were first evaluated against a large panel of Gram-positive and Gram-negative pathogens. In particular, the majority of PTUs proved to be active against different species of the Staphylococcus genus, with MIC values ranging from 32 to 128 µg/mL on methicillin-resistant Staphylococcus strains, often responsible for severe pulmonary disease in cystic fibrosis patients...
March 15, 2024: Pharmaceuticals
https://read.qxmd.com/read/38543155/dose-prediction-and-pharmacokinetic-simulation-of-xzp-5610-a-small-molecule-for-nash-therapy-using-allometric-scaling-and-physiologically-based-pharmacokinetic-models
#39
JOURNAL ARTICLE
Lei Zhang, Feifei Feng, Xiaohan Wang, Hao Liang, Xueting Yao, Dongyang Liu
The objectives of this study were to support dose selection of a novel FXR agonist XZP-5610 in first-in-human (FIH) trials and to predict its liver concentrations in Chinese healthy adults. Key parameters for extrapolation were measured using in vitro and in vivo models. Allometric scaling methods were employed to predict human pharmacokinetics (PK) parameters and doses for FIH clinical trials. To simulate the PK profiles, a physiologically based pharmacokinetic (PBPK) model was developed using animal data and subsequently validated with clinical data...
March 13, 2024: Pharmaceuticals
https://read.qxmd.com/read/38543129/in-vivo-pharmacokinetic-study-of-polygonatum-cyrtonema-polysaccharide-dpc1-after-oral-and-intraperitoneal-administration
#40
JOURNAL ARTICLE
Jin Yong, Chaozheng Zhang, Yuening Cao, Shuang Tang, Fei Long, Zhixing Cao, Jun Lu, Teng Peng
(1) Background: Polygonatum cyrtonema is a medicinal plant, and its polysaccharides are used for immunomodulation and the treatment of hyperglycemia. Investigation of the tissue distribution and pharmacokinetics of P. cyrtonema polysaccharide can further elucidate its pharmacological mechanisms. (2) Methods: A fluorescence-labeling approach using rhodamine B (RhB) as a fluorescent molecular probe was used for the quantitative assessment of the polysaccharide from dried P. cyrtonema (DPC1) samples, and the pharmacokinetics and tissue distribution of DPC1 were evaluated in mice after intraperitoneal or oral administration...
March 6, 2024: Pharmaceuticals
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