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Journal articles on the topic 'Long-acting release kinetics'

Author: Grafiati

Published: 10 December 2022

Last updated: 31 July 2025

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1

Kim, Soyoung, Brian Cicali, Michelle Pressly, et al. "Model-Based Analysis of In Vivo Release Data of Levonorgestrel Implants: Projecting Long-Term Systemic Exposure." Pharmaceutics 15, no. 5 (2023): 1393. http://dx.doi.org/10.3390/pharmaceutics15051393.

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Levonorgestrel (LNG) is a progestin used in many contraceptive formulations, including subcutaneous implants. There is an unmet need for developing long-acting formulations for LNG. To develop long-acting formulations, release functions need to be investigated for LNG implant. Therefore, a release model was developed and integrated into an LNG physiologically-based pharmacokinetic (PBPK) model. Utilizing a previously developed LNG PBPK model, subcutaneous administration of 150 mg LNG was implemented into the modeling framework. To mimic LNG release, ten functions incorporating formulation-spec

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Verma, Malvika, Jacqueline N. Chu, John A. F. Salama, et al. "Development of a long-acting direct-acting antiviral system for hepatitis C virus treatment in swine." Proceedings of the National Academy of Sciences 117, no. 22 (2020): 11987–94. http://dx.doi.org/10.1073/pnas.2004746117.

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Chronic hepatitis C virus (HCV) infection is a leading cause of cirrhosis worldwide and kills more Americans than 59 other infections, including HIV and tuberculosis, combined. While direct-acting antiviral (DAA) treatments are effective, limited uptake of therapy, particularly in high-risk groups, remains a substantial barrier to eliminating HCV. We developed a long-acting DAA system (LA-DAAS) capable of prolonged dosing and explored its cost-effectiveness. We designed a retrievable coil-shaped LA-DAAS compatible with nasogastric tube administration and the capacity to encapsulate and release

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Cortez, John M., Rafaela Quintero, John A. Moss, Martin Beliveau, Thomas J. Smith, and Marc M. Baum. "Pharmacokinetics of Injectable, Long-Acting Nevirapine for HIV Prophylaxis in Breastfeeding Infants." Antimicrobial Agents and Chemotherapy 59, no. 1 (2014): 59–66. http://dx.doi.org/10.1128/aac.03906-14.

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ABSTRACTMother-to-child transmission (MTCT) of HIV-1 remains a global health problem. The World Health Organization (WHO) recommendations advise the administration of a once-daily, oral, prophylactic regimen of the nonnucleoside reverse transcriptase inhibitor nevirapine (NVP) from birth until 4 to 6 weeks of age for infants born to HIV-infected mothers in regions without access to safe and nutritionally adequate alternatives to breast milk. A critical factor driving the successful implementation of the WHO guidelines involves sustaining high adherence to the frequent dosing. With these challe

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Son, Young Jin, Tae Han Yun, Jeong Gyun Lee, Kyu Ho Bang, and Kyeong Soo Kim. "Development and Characterization of Long-Acting Injectable Risperidone Microspheres Using Biodegradable Polymers: Formulation Optimization and Release Kinetics." Processes 12, no. 12 (2024): 2858. https://doi.org/10.3390/pr12122858.

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The aim of this study was to develop a long-acting injectable formulation of risperidone using polylactic acid (PLA) or poly (lactic-co-glycolic acid) (PLGA), a biodegradable and biocompatible polymer. Risperidone microspheres (RMs) were prepared by creating an O/W emulsion using dichloromethane (DCM) as a solvent and then employing the solvent evaporation method. The RMs were prepared with four different risperidone-to-PLGA ratios (1:1, 1:1.3, 1:2, and 1:3 (w/w)), and each ratio was subjected to the same manufacturing process. The physicochemical properties of the prepared RMs, such as their

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Yan, Xieguo, Shiqiang Wang, and Kaoxiang Sun. "Long-Acting Risperidone Dual Control System: Preparation, Characterization and Evaluation In Vitro and In Vivo." Pharmaceutics 13, no. 8 (2021): 1210. http://dx.doi.org/10.3390/pharmaceutics13081210.

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Schizophrenia, a psychiatric disorder, requires long-term treatment; however, large fluctuations in blood drug concentration increase the risk of adverse reactions. We prepared a long-term risperidone (RIS) implantation system that can stabilize RIS release and established in-vitro and in-vivo evaluation systems. Cumulative release, drug loading, and entrapment efficiency were used as evaluation indicators to evaluate the effects of different pore formers, polymer ratios, porogen concentrations, and oil–water ratios on a RIS implant (RIS-IM). We also built a mathematical model to identify the

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Gohn, Anne M., Amy Nolte, Ethan Ravotti, et al. "Dissolution from Ethylene Vinyl Acetate Copolymer Long-Acting Implants: Effect of Model Active Ingredient Size and Shape." Pharmaceutics 14, no. 6 (2022): 1139. http://dx.doi.org/10.3390/pharmaceutics14061139.

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In recent pharmaceutical applications, an active pharmaceutical ingredient (API) can be mixed with a polymer material to yield a composite long-acting drug-delivery device. These devices boast higher patient compliance, localized drug delivery, and lower dosage concentrations, which can increase patient safety. As a laboratory-safe option, calcium carbonate (CaCO3) was used as a drug surrogate to mimic the release kinetics of a low-solubility API. The release of CaCO3 from a poly(ethylene vinyl acetate) (EVA) polymer matrix was studied in ultra-high-purity water. The geometry of CaCO3, along w

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Wojcik-Pastuszka, Dorota, Justyna Krzak, Bartosz Macikowski, Ryszard Berkowski, Bogdan Osiński, and Witold Musiał. "Evaluation of the Release Kinetics of a Pharmacologically Active Substance from Model Intra-Articular Implants Replacing the Cruciate Ligaments of the Knee." Materials 12, no. 8 (2019): 1202. http://dx.doi.org/10.3390/ma12081202.

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Implants are readily applied as a convenient method of therapy. There is great interest in the prolonged release of active substances from implants. The objective of this work was to evaluate the dissolution kinetics of steroidal anti-inflammatory preparation (SAP) released from novel implants, and to test the influence of the technology on SAP release kinetics. The proposed long-acting preparations may overcome difficulties resulting from repeated injections and often visits to ambulatory clinic, as the stabilizing function of the artificial ligament would be enriched with pharmacological act

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Comets, Emmanuelle, France Mentré, Ryosei Kawai, Fritz Nimmerfall, Peter Marbach, and Jacky Vonderscher. "Modeling the Kinetics of Release of Octreotide from Long‐Acting Formulations Injected Intramuscularly in Rabbits." Journal of Pharmaceutical Sciences 89, no. 9 (2000): 1123–33. http://dx.doi.org/10.1002/1520-6017(200009)89:9<1123::aid-jps4>3.0.co;2-k.

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9

Ishkaeva, Rezeda A., Nail N. Khaertdinov, Aleksey V. Yakovlev, et al. "Characterization of Glutathione Dithiophosphates as Long-Acting H2S Donors." International Journal of Molecular Sciences 24, no. 13 (2023): 11063. http://dx.doi.org/10.3390/ijms241311063.

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Considering the important cytoprotective and signaling roles but relatively narrow therapeutic index of hydrogen sulfide (H2S), advanced H2S donors are required to achieve a therapeutic effect. In this study, we proposed glutathione dithiophosphates as new combination donors of H2S and glutathione. The kinetics of H2S formation in dithiophosphate solutions suggested a continuous H2S release by the donors, which was higher for the dithiophosphate of reduced glutathione than oxidized glutathione. The compounds, unlike NaHS, inhibited the proliferation of C2C12 myoblasts at submillimolar concentr

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Yue, Zhaoyan. "The Release Kinetics of Long-Lasting Tracer Particles in Horizontal Wells." Scientific Journal of Technology 7, no. 2 (2025): 101–11. https://doi.org/10.54691/hwvb0g03.

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In the context of China's ongoing development of unconventional oil and gas reservoirs, horizontal well segmental fracturing technology currently holds a dominant position. Accurate and effective monitoring of fracture parameters and production profiles is imperative for the efficient development of oil and gas resources. Tracer monitoring technology has emerged as a pivotal method for monitoring horizontal wells fractured in tight oil segments. This technology involves the injection of slow-release tracer particles into the fractured fracture, followed by the continuous monitoring of the trac

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Gao, Ge Fiona, Mukul Ashtikar, Ryo Kojima, et al. "Predicting drug release and degradation kinetics of long-acting microsphere formulations of tacrolimus for subcutaneous injection." Journal of Controlled Release 329 (January 2021): 372–84. http://dx.doi.org/10.1016/j.jconrel.2020.11.055.

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Chrysafi, Iouliana, Stavroula Nanaki, Alexandra Zamboulis, Margaritis Kostoglou, Eleni Pavlidou, and Dimitrios N. Bikiaris. "Poly(Lactic Acid) Block Copolymers with Poly(Hexylene Succinate) as Microparticles for Long-Acting Injectables of Risperidone Drug." Polymers 14, no. 19 (2022): 4111. http://dx.doi.org/10.3390/polym14194111.

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In the present work, Risperidone microparticles from poly(lactic acid)/poly(hexylene succinate) (PLA-b-PHSu) block copolymers in different ratios, 95/05, 90/10 and 80/20 w/w, were examined as long-acting injectable formulations. Nuclear magnetic resonance (NMR) was used to verify the successful synthesis of copolymers. Enzymatic hydrolysis showed an increase in weight loss as the content of PHSu increased, while the cytotoxicity studies confirmed the biocompatibility of the copolymers. The polyesters were further used to encapsulate Risperidone by spray drying. The drug-loaded microparticles w

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Nanaki, Stavroula, Panagiotis Barmpalexis, Alexandros Iatrou, Evi Christodoulou, Margaritis Kostoglou, and Dimitrios Bikiaris. "Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations." Pharmaceutics 10, no. 3 (2018): 130. http://dx.doi.org/10.3390/pharmaceutics10030130.

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The present study evaluates the preparation of risperidone controlled release microspheres as appropriate long-acting injectable formulations based on a series of novel biodegradable and biocompatible poly(lactic acid)–poly(propylene adipate) (PLA/PPAd) polymer blends. Initially, PPAd was synthesized using a two-stage melt polycondensation method (esterification and polycondensation) and characterized by 1H-NMR, differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) analyses. DSC and XRD results for PLA/PPAd blends (prepared by the solvent evaporation method) showed that t

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Sonam, ,., Nilesh Jain, and Jitendra Banveer. "Formulation, Development and Evaluation of Gastroretentive Sustained Release Tablets of Lansoprazole Using Natural Polymer." Journal of Drug Delivery and Therapeutics 11, no. 5-S (2021): 108–12. http://dx.doi.org/10.22270/jddt.v11i5-s.5087.

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The goal of this study is to develop a long-acting Lansoprazole delivery system. Lansoprazole belongs to a class of antisecretory drugs known as substituted benzimidazoles, which decrease gastric acid secretion by inhibiting the (H+,K+)-ATPase enzyme system at the secretory membrane of the stomach parietal cell. Due to its mechanism of action, despite its short half-life of 1-5 hours, it can effectively block acid secretion for 24 hours. However, as his plasma concentration falls, the effect will diminish. Lansoprazole will be given as a sustained release tablet to avoid multiple dosing or to

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15

Ahn, Jun-hyun. "Preparation and Evaluation of Long-Acting Injectable Levocetirizine Prodrug Formulation." Pharmaceutics 17, no. 7 (2025): 806. https://doi.org/10.3390/pharmaceutics17070806.

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Background/Objectives: Levocetirizine (LCZ) is a second-generation antihistamine with minimal central nervous system effects. However, its short half-life necessitates daily dosing, potentially reducing adherence in pediatric populations. This study aimed to develop a long-acting injectable LCZ formulation by synthesizing lipophilic prodrugs and evaluating their physicochemical stability, enzymatic hydrolysis, and pharmacokinetics in vivo. Methods: Two prodrugs of LCZ, LCZ decanoate (LCZ-D) and LCZ laurate (LCZ-L), were synthesized via esterification with alkyl alcohols. The compounds were cha

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Yonet-Tanyeri, Nihan, Robert S. Parker, Louis D. Falo, and Steven R. Little. "Investigation of the Impact of Manufacturing Methods on Protein-Based Long-Acting Injectable Formulations: A Comparative Assessment for Microfluidics vs. Conventional Methods." Pharmaceutics 16, no. 10 (2024): 1264. http://dx.doi.org/10.3390/pharmaceutics16101264.

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Background/Objectives: Microparticle-based drug delivery systems offer several advantages for protein-based drug formulations, enhancing patient compliance and therapeutic efficiency through the sustained delivery of the active pharmaceutical ingredient. Over the past few decades, the microfluidics method has emerged as a continuous manufacturing process for preparing drug-encapsulating microparticles, mainly for small molecule drugs. However, comparative assessments for the conventional batch method vs. the microfluidics method for protein-based drug formulations have been lacking. The main o

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Mertz, Nina, Susan Weng Larsen, Jesper Kristensen, Jesper Østergaard, and Claus Larsen. "Long-Acting Diclofenac Ester Prodrugs for Joint Injection: Kinetics, Mechanism of Degradation, and In Vitro Release From Prodrug Suspension." Journal of Pharmaceutical Sciences 105, no. 10 (2016): 3079–87. http://dx.doi.org/10.1016/j.xphs.2016.06.013.

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18

Cagnon, Marie-Emérentienne, Silvio Curia, Juliette Serindoux, Jean-Manuel Cros, Feifei Ng, and Adolfo Lopez-Noriega. "Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables." Pharmaceutics 13, no. 5 (2021): 605. http://dx.doi.org/10.3390/pharmaceutics13050605.

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This article describes the utilization of (methoxy)poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) ((m)PEG–PTMC) diblock and triblock copolymers for the formulation of in situ forming depot long-acting injectables by solvent exchange. The results shown in this manuscript demonstrate that it is possible to achieve long-term drug deliveries from suspension formulations prepared with these copolymers, with release durations up to several months in vitro. The utilization of copolymers with different PEG and PTMC molecular weights affords to modulate the release profile and duration. A pha

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Joiner, Jordan B., Alka Prasher, Isabella C. Young, et al. "Effects of Drug Physicochemical Properties on In-Situ Forming Implant Polymer Degradation and Drug Release Kinetics." Pharmaceutics 14, no. 6 (2022): 1188. http://dx.doi.org/10.3390/pharmaceutics14061188.

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In-situ forming implants (ISFIs) represent a simple, tunable, and biodegradable polymer-based platform for long-acting drug delivery. However, drugs with different physicochemical properties and physical states in the polymer-solvent system exhibit different drug release kinetics. Although a few limited studies have been performed attempting to elucidate these effects, a large, systematic study has not been performed until now. The purpose of this study was to characterize the in vitro drug release of 12 different small molecule drugs with differing logP and pKa values from ISFIs. Drug release

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20

Li, Linying, Christine Areson, Ariane van der Straten, and Leah M. Johnson. "Effects of Polymer Blending on the Performance of a Subcutaneous Biodegradable Implant for HIV Pre-Exposure Prophylaxis (PrEP)." International Journal of Molecular Sciences 22, no. 12 (2021): 6529. http://dx.doi.org/10.3390/ijms22126529.

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Long-acting (LA) HIV pre-exposure prophylaxis (PrEP) can mitigate challenges of adhering to daily or on-demand regimens of antiretrovirals (ARVs). We are developing a subcutaneous implant comprising polycaprolactone (PCL) for sustained delivery of ARVs for PrEP. Here we use tenofovir alafenamide (TAF) as a model drug. Previously, we demonstrated that the release rates of drugs are controlled by the implant surface area and wall thickness, and the molecular weight (MW) of PCL. Here, we further advance the implant design and tailor the release rates of TAF and the mechanical integrity of the imp

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Kapralos, Iasonas, and Aristides Dokoumetzidis. "Population Pharmacokinetic Modelling of the Complex Release Kinetics of Octreotide LAR: Defining Sub-Populations by Cluster Analysis." Pharmaceutics 13, no. 10 (2021): 1578. http://dx.doi.org/10.3390/pharmaceutics13101578.

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The aim of the study is to develop a population pharmacokinetic (PPK) model, of Octreotide long acting repeatable (LAR) formulation in healthy volunteers, which describes the highly variable, multiple peak absorption pattern of the pharmacokinetics of the drug, in individual and population levels. An empirical absorption model, coupled with a one-compartment distribution model with linear elimination was found to describe the data well. Absorption was modelled as a weighted sum of a first order and three transit compartment absorption processes, with delays and appropriately constrained model

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Georgieva, Dilyana, Mariela Alexandrova, Sijka Ivanova, Darinka Christova, and Bistra Kostova. "Conceptualization and Investigation of Multicomponent Polymer Networks as Prospective Corticosteroid Carriers." Gels 9, no. 6 (2023): 470. http://dx.doi.org/10.3390/gels9060470.

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Dexamethasone (DXM) is a highly potent and long-acting synthetic glucocorticoid with anti-inflammatory, anti-allergic, and immunosuppressive effects. However, the systemic application of DXM can cause undesirable side effects: sleep disorders, nervousness, heart rhythm disorders, heart attack, and others. In the present study, multicomponent polymer networks were developed as potential new platforms for the dermal application of dexamethasone sodium phosphate (DSP). First, a copolymer network (CPN) comprising hydrophilic segments of different chemical structures was synthesized by applying red

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To, Minh D., Fahar Merchant, and Nina Merchant. "MDNA11 is a long-acting IL-2 superkine that potentiates durable immune response in mouse tumor models and non-human primates." Journal of Clinical Oncology 39, no. 15_suppl (2021): e14546-e14546. http://dx.doi.org/10.1200/jco.2021.39.15_suppl.e14546.

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e14546 Background: The efficacy and safety of recombinant human IL-2 (rhIL-2; Proleukin) to treat certain cancers is limited by a short half-life, marked toxicity and selective high affinity binding to IL2Ra over IL2Rb, resulting in preferential activation of suppressive Tregs. In contrast, MDNA11 has been engineered as a long-acting IL-2 superkine with high affinity IL2Rb receptor selectivity, resulting in preferential anti-cancer effector immune cell activation. Methods: MDNA11 was characterized in both in vitro and in vivo studies including assessment of receptor binding kinetics using BLI/

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Dominguez, Belisario, Ricardo Felix, and Eduardo Monjaraz. "Upregulation of voltage-gated Na+ channels by long-term activation of the ghrelin-growth hormone secretagogue receptor in clonal GC somatotropes." American Journal of Physiology-Endocrinology and Metabolism 296, no. 5 (2009): E1148—E1156. http://dx.doi.org/10.1152/ajpendo.90954.2008.

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A central question in adenohypophyseal cell physiology concerns the role of transmembrane ionic fluxes in the initiation of the hormone secretion process. In the current report, we investigated the effects of the growth hormone (GH) secretagogues ghrelin and GH-releasing peptide-6 (GHRP-6) on the regulation of the functional expression of voltage-gated Na+ channels using the tumoral somatotrope GC cell line as a model. Cells were cultured under control conditions or in presence of the GH secretagogues (GHS) for 96 h, and Na+ currents ( INa) were characterized in whole cell patch-clamp experime

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Huang, Lijie, Hanyu Zhao, Hao Xu, et al. "Kinetic model of a carboxymethylcellulose-agar hydrogel for long-acting and slow-release of chlorine dioxide with a modification of Fick’s diffusion law." BioResources 14, no. 4 (2019): 8821–34. http://dx.doi.org/10.15376/biores.14.4.8821-8834.

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A long-acting and slow-release material for chlorine dioxide, based on bagasse pulp (BP) was prepared with a superabsorbent resin as the slow-release substrate and agar as the cross-linking agent. The stable ClO2 solution and the acidic activator were locked into the network structure of the superabsorbent resin, which was prepared with a carboxymethyl cellulose made from bagasse pulp. Because of the network structure of the resin, the diffusion resistance was greatly increased, and the effective release time was up to 2 months. The mechanism for the release process of the ClO2 was explored, a

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Kinsale, Talisa S., Mackenzie L. Cottrell, Linying Li, et al. "Pharmacokinetic Modeling to Guide Preclinical Development of an Islatravir-Eluting Reservoir-Style Biodegradable Implant for Long-Acting HIV PrEP." Pharmaceutics 16, no. 2 (2024): 201. http://dx.doi.org/10.3390/pharmaceutics16020201.

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Long-acting injectable cabotegravir is more effective than daily oral PrEP at preventing HIV transmission due to improved adherence, but requires bi-monthly large-volume intramuscular injections. Subcutaneous (SC) contraceptive implants can be formulated with antiretrovirals for extended-duration HIV PrEP. Islatravir (ISL) is a first-in-class, investigational antiretroviral with pharmacologic properties well-suited for implant delivery. We performed preclinical studies for the development of a reservoir-style, poly(ε-caprolactone) ISL-eluting implant by conducting a single-dose SC ISL dose-ran

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Zashikhina, Natalia, Vladimir Sharoyko, Mariia Antipchik, et al. "Novel Formulations of C-Peptide with Long-Acting Therapeutic Potential for Treatment of Diabetic Complications." Pharmaceutics 11, no. 1 (2019): 27. http://dx.doi.org/10.3390/pharmaceutics11010027.

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The development and application of novel nanospheres based on cationic and anionic random amphiphilic polypeptides with prolonged stability were proposed. The random copolymers, e.g., poly(l-lysine-co-d-phenylalanine) (P(Lys-co-dPhe)) and poly(l-glutamic acid-co-d-phenylalanine) (P(Glu-co-dPhe)), with different amount of hydrophilic and hydrophobic monomers were synthesized. The polypeptides obtained were able to self-assemble into nanospheres. Such characteristics as size, PDI and ζ-potential of the nanospheres were determined, as well as their dependence on pH was also studied. Additionally,

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Rimpelä, Anna-Kaisa, Iiro Kiiski, Feng Deng, Heidi Kidron, and Arto Urtti. "Pharmacokinetic Simulations of Intravitreal Biologicals: Aspects of Drug Delivery to the Posterior and Anterior Segments." Pharmaceutics 11, no. 1 (2018): 9. http://dx.doi.org/10.3390/pharmaceutics11010009.

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Biologicals are important ocular drugs that are be delivered using monthly and bimonthly intravitreal injections to treat retinal diseases, such as age-related macular degeneration. Long acting delivery systems are needed for prolongation of their dosing interval. Intravitreal biologicals are eliminated from the eye via the aqueous humor outflow. Thus, the anterior and posterior segments are exposed to the drug. We utilized a kinetic simulation model to estimate protein drug concentrations in the vitreous and aqueous humor after bolus injection and controlled release administration to the vitr

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Jiang, Lei, Fan Fan, Xuemei Wang, Shaukat Ali, Feng Zhou, and Jiantao Zhang. "Multi-Level Drug Delivery System Integrated with Injectable Hydrogels and ZIF-8 for Sustained Release of Lidocaine." Journal of Pharmaceutical and BioTech Industry 2, no. 1 (2025): 3. https://doi.org/10.3390/jpbi2010003.

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Lidocaine plays a significant role in postoperative analgesia by effectively reducing pain. However, due to its short half-life, it is challenging for lidocaine to achieve the desired duration of analgesia in clinical settings. Drug delivery systems can regulate the release rate over time, making them one of the most effective strategies for achieving sustained release. In this work, a multi-level drug delivery system was designed using hyaluronic acid-modified zeolitic imidazolate framework-8 (HA/ZIF-8) nanoparticles and injectable hydrogels composed of modified natural polymers. Lidocaine wa

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Nayak, Bhabani Shankar, P. Ellaiah, Suprava Sethy, Monalisha Nayak, and Subham Sourajit. "Formulation design and characterization of osmotically controlled tablet of Ramipril." Pharmaceutical and Biological Evaluations 4, no. 1 (2017): 1. http://dx.doi.org/10.26510/2394-0859.pbe.2017.01.

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Objective: Ramipril is a long-acting angiotensin-converting enzyme inhibitor. The study aimed to design, formulate and evaluate the oral osmotic drug delivery dosage form of an anti-hypertensive drug, ramipril.Methods: The tablet was formulated using ramipril and different polymers like PVP- K30 and Ethyl cellulose. The microcrystalline cellulose (MCC - diluent), Potassium chloride, Mannitol (osmogen) and Magnesium stearate (lubricant) were used in all the formulations. All the tablets were manufactured by wet granulation method followed by film coating. Compatibility of the drug with excipien

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de M. Barbosa, Raquel, Ligia Ribeiro, Bruna Casadei, et al. "Solid Lipid Nanoparticles for Dibucaine Sustained Release." Pharmaceutics 10, no. 4 (2018): 231. http://dx.doi.org/10.3390/pharmaceutics10040231.

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Dibucaine (DBC) is among the more potent long-acting local anesthetics (LA), and it is also one of the most toxic. Over the last decades, solid lipid nanoparticles (SLN) have been developed as promising carriers for drug delivery. In this study, SLN formulations were prepared with the aim of prolonging DBC release and reducing its toxicity. To this end, SLN composed of two different lipid matrices and prepared by two different hot-emulsion techniques (high-pressure procedure and sonication) were compared. The colloidal stability of the SLN formulations was tracked in terms of particle size (nm

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Camargo, Luan Pereira, Augusto Batagin-Neto, Marcelo Rodrigues da Silva Pelissari, Paulo Rogério Catarini da Silva, Odair Pastor Ferreira, and Luiz Henrique Dall'Antonia. "Unveiling Tungsten Trioxide and Iron Vanadate Heterojunction: Enhanced Photoelectrochemical Response via Improved Visible-Light Absorption and Charge Carrier Separation." ECS Meeting Abstracts MA2025-01, no. 56 (2025): 2711. https://doi.org/10.1149/ma2025-01562711mtgabs.

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Sustainable development prioritizes environmental sustainability, including renewable energy, sustainable agriculture, efficient waste management, and long-term resilience and harmony. However, renewable energy production faces challenges due to its intermittent and unpredictable nature. Energy storage is essential for use during reduced or absent power generation periods. An attractive approach to overcome this is converting molecules into potential fuels (e.g. H2 and CxHyOz) that can release energy on demand. For instance, water can be split into hydrogen and oxygen gases (H2O → O2 + H2), or

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Rimando, Joseph, Michael P. Rettig, Matt Christopher, et al. "Flotetuzumab and Other Cellular Immunotherapies Upregulate MHC Class II Expression on Acute Myeloid Leukemia Cells in Vitro and In Vivo." Blood 136, Supplement 1 (2020): 22–23. http://dx.doi.org/10.1182/blood-2020-133891.

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Background: Allogeneic hematopoietic cell transplantation (allo-HCT) is the only curative therapy for patients with high-risk and refractory acute myeloid leukemia (AML). Unfortunately, up to 50 percent of patients relapse after allo-HCT.Recent research has shown that 30-50 percent of AML samples from patients relapsing after allo-HCT have downregulation of MHC class II (MHC-II) expression, which may promote immune effector evasion and disease relapse. These studies also report that interferon gamma (IFNγ) can restore MHC-II expression. IFNγ has never been systemically administered after allo-

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Saito, Yoriko, Eyal Attar, Samyukta Jana, et al. "Nucleotide Receptor P2Y14 Modulates Hematopoietic Stem Cell Response to Tissue Injury Altering Stem Cell Preservation and Tissue Recovery." Blood 108, no. 11 (2006): 679. http://dx.doi.org/10.1182/blood.v108.11.679.679.

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Abstract P2 receptors are functionally diverse cell surface receptors that bind nucleotides adenine (ADP, ATP) and uridine (UDP, UTP). P2Y receptors are metabotropic G protein-coupled receptors that mediate vascular and immune responses to injury. We previously reported the differential expression cloning of the UTP-glycoconjugate receptor, P2Y14 from quiescent primary human bone marrow (BM) hematopoietic stem cells (HSCs). Using P2Y14−/− mice, we now report that the presence of P2Y14 protects HSCs from apoptosis in the face of cytotoxic chemical injury. P2Y14 null mice develop normally and sh

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Weiden, Peter J., Gregory A. Watkins, Brian Liu, Garrett L. Healy, Lana T. Ho, and Francis J. Martin. "Feasibility of a Risperidone Implant for the Maintenance Treatment of Schizophrenia for up to 12 Months After a Single Administration." CNS Spectrums 29, no. 5 (2024): 524. https://doi.org/10.1017/s1092852924002050.

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IntroductionDisruptions of antipsychotic therapy lead to greater symptoms and increased likelihood of relapse. One way to improve medication adherence has been with long-acting formulations, usually administered by injection. Implantable technology has been used to support medication continuity in a few therapeutic areas, e.g., contraception. Despite the potential benefits from implants, this modality is not yet available for maintenance treatment of schizophrenia. Delpor, Inc. is developing an investigational risperidone implant (DLP-114) that releases therapeutic drug levels for up to 12-mon

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Chobisa, Dhawal, Anbukkarasi Muniyandi, Kamakshi Sishtla, Timothy W. Corson, and Yoon Yeo. "Long‐Acting Microparticle Formulation of Griseofulvin for Ocular Neovascularization Therapy." Small, November 8, 2023. http://dx.doi.org/10.1002/smll.202306479.

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AbstractNeovascular age‐related macular degeneration (nAMD) is a leading cause of vision loss in older adults. nAMD is treated with biologics targeting vascular endothelial growth factor; however, many patients do not respond to the current therapy. Here, a small molecule drug, griseofulvin (GRF), is used due to its inhibitory effect on ferrochelatase, an enzyme important for choroidal neovascularization (CNV). For local and sustained delivery to the eyes, GRF is encapsulated in microparticles based on poly(lactide‐co‐glycolide) (PLGA), a biodegradable polymer with a track record in long‐actin

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Lu, Leihao, Jianchang Xu, Xuehui Huang, et al. "Mussel Foot Protein Membrane‐Enclosed Crystalline Drug with Zero‐Order Release Kinetics for Long‐Acting Therapy." Angewandte Chemie International Edition, March 11, 2025. https://doi.org/10.1002/anie.202502205.

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AbstractInjectable formulations with sustained and steady release capabilities are critically required to treat diseases requiring temporary or lifelong continuous therapy, especially for drugs with a short half‐life. Additionally, achieving a sufficiently high drug loading in a single dose remains a persistent challenge. Herein, by mimicking the formation principles of mussel adhesive plaques, we have developed membrane‐enclosed crystalline systems of insulin and progesterone as model macro‐ and small‐molecular crystalline drugs. The system exhibits a substantial drug loading capacity (>90

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Lu, Leihao, Jianchang Xu, Xuehui Huang, et al. "Mussel Foot Protein Membrane‐Enclosed Crystalline Drug with Zero‐Order Release Kinetics for Long‐Acting Therapy." Angewandte Chemie, March 11, 2025. https://doi.org/10.1002/ange.202502205.

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AbstractInjectable formulations with sustained and steady release capabilities are critically required to treat diseases requiring temporary or lifelong continuous therapy, especially for drugs with a short half‐life. Additionally, achieving a sufficiently high drug loading in a single dose remains a persistent challenge. Herein, by mimicking the formation principles of mussel adhesive plaques, we have developed membrane‐enclosed crystalline systems of insulin and progesterone as model macro‐ and small‐molecular crystalline drugs. The system exhibits a substantial drug loading capacity (>90

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Molavi, Fatima, Mohammad Barzegar-Jalali, and Hamed Hamishehkar. "Changing the daily injection of glatiramer acetate to a monthly long acting product through designing polyester-based polymeric microspheres." BioImpacts, August 13, 2022. http://dx.doi.org/10.34172/bi.2022.23733.

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Introduction: Glatiramer acetate (GA) is a newly emerged therapeutic peptide to reduce the frequency of relapses in multiple sclerosis (MS). Despite its good performance in controlling MS, it is not widely used due to daily or biweekly subcutaneous injections due to rapid degradation and body clearance. Therefore, implant design with sustained release leads to prolonged biological effects by gradually increasing drug exposure and protecting GA from rapid local degradation. Methods: Different emulsion methods, PLGA type, surfactant concentration, drug/polymer ratio, drying processes, stirring m

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Bannigan, Pauric, Zeqing Bao, Riley John Hickman, et al. "Machine Learning Models to Accelerate the Design of Polymeric Long-Acting Injectables." November 9, 2022. https://doi.org/10.5281/zenodo.7309021.

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Long-acting injectables are considered one of the most promising therapeutic strategies for the treatment of chronic diseases as they can afford improved therapeutic efficacy, safety, and patient compliance. The use of polymer materials in such a drug formulation strategy can offer unparalleled diversity owing to the ability to synthesize materials with a wide range of properties. However, the interplay between multiple parameters, including the physicochemical properties of the drug and polymer, make it very difficult to intuitively predict the performance of these systems. This necessitates

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Rudd, Nathan D., Roy Helmy, Peter G. Dormer, et al. "Probing in Vitro Release Kinetics of Long-Acting Injectable Nanosuspensions via Flow-NMR Spectroscopy." Molecular Pharmaceutics, January 14, 2020. http://dx.doi.org/10.1021/acs.molpharmaceut.9b00958.

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Daniels, Juma N., and Andrew Otte. "Development of Long-Acting Injectable Ketamine Loaded PLGA Microparticles as a Non-opioid Analgesic." Proceedings of IMPRS 4, no. 1 (2021). http://dx.doi.org/10.18060/25777.

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Background/Objective: Ketamine, a psychedelic, is a noncompetitive N-methyl-D-aspartate receptor antagonist that may also bind to mu opioid receptors. Historically, it has been used as an anesthetic (KetalarÒ), although now has found uses as a novel, quick acting, antidepressant for treatment-resistant depression (SpravatorÒ) and could be used as an adjuvant to opioid analgesia providing opioid-sparing effects. One major advantage over opioids is Ketamine does not suffer from respiratory depression and maintains patent airways during anesthesia. Ketamine is only available as a short-acting inj

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Singh, Akanksha, Rajkiran Narkhede, and Rajani Athawale. "A Quality By Design (QbD) Prospect in Fabrication of PLGA-based Antipsychotic Long-acting Microspheres: An Alternative to Combination Therapy." Current Applied Polymer Science 07 (May 30, 2024). http://dx.doi.org/10.2174/0124522716306759240522112102.

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Background: Discontinuation and poor compliance with long-term oral medicine are major therapeutic issues in psychosis treatment. Poorer long-term outcomes may result from non-compliance as well as a higher chance of relapse. In order to sustain therapeutic drug plasma levels, co-administration of oral antipsychotics is necessary for commercially available longacting injections of second-generation antipsychotics, as they have a lag period of approximately three weeks during the drug release process. Methods: Poly(lactic-co-glycolic acid) (PLGA) encapsulated microspheres loaded with risperidon

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Gunawardana, Manjula, Mariana Remedios-Chan, Debbie Sanchez, et al. "Preclinical Considerations for Long-acting Delivery of Tenofovir Alafenamide from Subdermal Implants for HIV Pre-exposure Prophylaxis." Pharmaceutical Research, November 23, 2022. http://dx.doi.org/10.1007/s11095-022-03440-6.

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Abstract Purpose Long-acting formulations of the potent antiretroviral prodrug tenofovir alafenamide (TAF) hold potential as biomedical HIV prevention modalities. Here, we present a rigorous comparison of three animal models, C57BL/6 J mice, beagle dogs, and merino sheep for evaluating TAF implant pharmacokinetics (PKs). Methods Implants delivering TAF over a wide range of controlled release rates were tested in vitro and in mice and dogs. Our existing PK model, supported by an intravenous (IV) dosing dog study, was adapted to analyze mechanistic aspects underlying implant TAF delivery. Result

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MALI, SANDIP, and NISHANT OZA. "CENTRAL COMPOSITE DESIGN FOR FORMULATION AND OPTIMIZATION OF LONG-ACTING INJECTABLE (LAI) MICROSPHERES OF PALIPERIDONE PALMITATE." International Journal of Applied Pharmaceutics, September 7, 2021, 87–98. http://dx.doi.org/10.22159/ijap.2021v13i5.42297.

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Objective: The aim of the present study was to optimize long-acting injectable (LAI) microspheres of Paliperidone palmitate (PP) for treatment of schizophrenia using face-centered central composite design (FC-CCD). Methods: In this study, poly lactic-co-glycolic acid (PLGA) based LAI microspheres of paliperidone palmitate (PP) were formulated by using FC-CCD. LAI microspheres were developed by using oil in water (O/W) emulsion solvent evaporation technique. On the basis of preliminary trials, FC-CCD was employed to check effect of independent variables such as drug polymer ratio (X1), homogeni

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Tanushree, Aman Sharma, Monika, Rahul Pratap Singh, and Vikas Jhawat. "Human immunodeficiency virus infection challenges: Current therapeutic limitations and strategies for improved management through long‐acting injectable formulation." Reviews in Medical Virology 34, no. 4 (2024). http://dx.doi.org/10.1002/rmv.2563.

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AbstractHIV infection has been a severe global health burden, with millions living with the virus and continuing new infections each year. Antiretroviral therapy can effectively suppress HIV replication but requires strict lifelong adherence to daily oral medication regimens, which presents a significant challenge. Long‐acting formulations of antiretroviral drugs administered infrequently have emerged as a promising strategy to improve treatment outcomes and adherence to HIV therapy and prevention. Long‐acting injectable (LAI) formulations are designed to gradually release drugs over extended

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Chu, Bo, Dagui Chen, Senlin Ma, et al. "Novel poly(lactic-co-glycolic acid) nanoliposome-encapsulated diclofenac sodium and celecoxib enable long-lasting synergistic treatment of osteoarthritis." Journal of Biomaterials Applications, May 31, 2024. http://dx.doi.org/10.1177/08853282241258311.

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Background: Diclofenac sodium (DS) and celecoxib (CEL) are primary anti-inflammatory agents used in the treatment of osteoarthritis (OA). Formulating these drugs into extended-release versions can effectively address the issue of multiple daily doses. In this study, we designed and synthesized a novel poly(lactic-co-glycolic acid) (PLGA) nanoliposome as a dual-drug delivery sustained-release formulation (PPLs-DS-CEL) to achieve long-lasting synergistic treatment of OA with both DS and CEL. Methods: PPLs-DS-CEL was synthesized by the reverse evaporation method and evaluated for its physicochemi

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MAJEE, SUTAPA BISWAS, TRISHA MISHRA, and SOUVIK GUPTI. "GASTRORETENTIVE EFFERVESCENT FLOATING TABLETS (GREFT) OF DRUGS ACTING ON CARDIOVASCULAR DISEASES." International Journal of Pharmacy and Pharmaceutical Sciences, July 1, 2024, 21–27. http://dx.doi.org/10.22159/ijpps.2024v16i7.51296.

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Incidences of Cardio Vascular Diseases (CVDs) are increasing in an alarming proportion in India. Conventional oral dosage forms cannot be retained in the stomach for long owing to gastric emptying. Moreover, drugs which are commonly employed in management of chronic CVDs either have reduced solubility at alkaline pH, undergo colonic degradation, exhibit site-specific absorption or varying bioavailability with combination therapy. Gastro-retentive drug delivery systems (GRDDS) are designed to overcome these challenges. Since 2006, Food and Drug Administration has approved only few GRDDS for tre

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Bowden, Anna Catherine, Rachel A. Allbaugh, Joe S. Smith, Jonathan P. Mochel, and Lionel Sebbag. "Kinetics and minimal inhibitory concentrations of ceftiofur in tear film following extended-release parenteral administration (Excede®) in dogs." Frontiers in Veterinary Science 9 (September 20, 2022). http://dx.doi.org/10.3389/fvets.2022.975113.

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PurposeDescribe the pharmacokinetics of extended-release parenteral ceftiofur (Excede®) in canine tear film and compare these concentrations to minimal inhibitory concentrations (MICs) of ceftiofur against common ocular pathogens in dogs.MethodSix dogs of various breeds were enrolled. Disruption of blood-tear barrier was achieved with histamine-induced conjunctivitis to ensure clinical relevance of the results. Each dog received a single subcutaneous injection of 5 mg/kg Excede®, followed by tear collection with Schirmer strips at times 0, 0.25, 0.5, 1, 2, 4, 8, 12, 24, 36, 48, 72, 96, 120, 14

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Kiefer, Nadine, Judith Klein, Mirko Rohr, et al. "Simulation of the biocide distribution in soil using PELMO coupled with COMLEAM." Environmental Science and Pollution Research, January 9, 2025. https://doi.org/10.1007/s11356-024-35760-y.

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AbstractBiocides, applied in building materials as antimicrobial protectants, can be leached out by rain, presenting substantial environmental risks as confirmed by studies on aquatic environments. However, these biocides are consistently released throughout the year in a diluted form, posing unique challenges for the prediction of transport, transformation, and ecotoxicity assessment in soil. To address this challenge, we combined COMLEAM, which predicts leaching from facades into the soil, with the FOCUS PELMO pesticide model to predict biocide distribution in soil. The study predicted the c

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