Article
Materials Science, Composites
Tingting Zhang, Xuhui Chen, Zhenyou Guo, Youbo Zhao, Hao Xiu, Hongwei Bai, Qin Zhang, Qiang Fu
Summary: This study demonstrates a novel route to control the distribution of hydrophilic silica in polymer blends by tailoring the silanol number of the silica, resulting in improved impact toughness and maintained strength and modulus of the blends.
COMPOSITES COMMUNICATIONS
(2021)
Article
Medicine, Research & Experimental
Saed Abbasi, Haruki Higashino, Yusuke Sato, Keiko Minami, Makoto Kataoka, Shinji Yamashita, Hideyoshi Harashima
Summary: The study investigated the use of a novel cinnamic acid-derived oil-like material (CAOM) in a SMEDDS for the oral delivery of fenofibrate. The results showed that the CAOM SMEDDS significantly improved fenofibrate bioavailability compared to traditional oils or enhancers. This suggests a strong potential for CAOM formulations in enhancing oral delivery of drugs with limited water solubility.
MOLECULAR PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Margherita Falavigna, Sunniva Brurok, Mette Klitgaard, Goril Eide Flaten
Summary: The study combined high-throughput in vitro intestinal lipolysis model with mucus-PVPA in vitro permeation model to investigate the solubilization capacity and drug permeation of SNEDDSs for fenofibrate. Results showed a significant impact of in vitro lipolysis on drug solubilization and permeation profiles. The correlation between in vitro permeation data and in vivo plasma concentration in rats was excellent, indicating the predictive ability of the developed combined in vitro model for in vivo drug absorption.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Review
Biochemistry & Molecular Biology
Phuong H. L. Tran, Thao T. D. Tran
Summary: Clays have been extensively used in health care products, including drug delivery systems. Their properties make them an ideal carrier for delivering poorly water-soluble drugs. There is limited information on the classification and discussion of clay-based formulations for poorly water-soluble drugs at present.
CURRENT DRUG METABOLISM
(2021)
Review
Chemistry, Multidisciplinary
Alejandro J. Paredes, Peter E. McKenna, Inken K. Ramoller, Yara A. Naser, Fabiana Volpe-Zanutto, Mingshan Li, M. T. A. Abbate, Li Zhao, Chunyang Zhang, Juhaina M. Abu-Ershaid, Xianbing Dai, Ryan F. Donnelly
Summary: Poorly soluble drugs make up a significant portion of the pharmaceutical market, with microarray patches (MAPs) showing potential as a strategy for delivering such drugs through the skin. The future of MAPs looks promising in terms of providing a convenient and effective therapeutic alternative for patients.
ADVANCED FUNCTIONAL MATERIALS
(2021)
Article
Pharmacology & Pharmacy
Amalie Moller, Hayley B. Schultz, Tahlia R. Meola, Anette Muellertz, Clive A. Prestidge
Summary: This study investigated the influence of lipid formulation classification and physical state on the in vitro solubilisation of blonanserin, a poorly soluble drug. The results showed that liquid SNEDDS was identified as the optimal oral supersaturated lipid-based formulation strategy for BLON.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Physical
F. J. Rubio-Hernandez, E. Fernandez-Diaz, J. F. Velazquez-Navarro
Summary: This study investigates the influence of temperature and solid concentration on the stress-induced shear-thickening behavior of A200PPG400 suspension, and proposes a more detailed description of the shear-thickening mechanism based on the analysis of intrinsic viscosity and activation energy for the viscous flow.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
Article
Pharmacology & Pharmacy
Kalle Sigfridsson, Theresa Andreasson, Britt-Marie Fihn, Martin Kearns, Sara Lindblom
Summary: This study describes a way to overcome oral administration challenges in early preclinical projects. Two main approaches were used to formulate a weak acid, AZ'403, for oral administration, resulting in significantly higher oral absorption compared to references. The findings suggest that both solid dispersions and crystalline salts may be promising for late stage product development.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Review
Pharmacology & Pharmacy
Do-Hyun Kim, Young-Woo Kim, Yee-Yee Tin, Mya-Thet-Paing Soe, Byoung-Hyen Ko, Sun-Jae Park, Jaeh-Wi Lee
Summary: Amorphization technology is a focus in the pharmaceutical industry to enhance the solubility and bioavailability of drugs. Traditional carriers for amorphous drugs have limitations, leading to the investigation of novel carriers and preparation methods to improve drug loading and amorphization. Recent advancements in amorphization technologies, such as co-amorphous systems and mesoporous particle-based techniques, are discussed for their characteristics and commercial potential.
Article
Engineering, Biomedical
Kaijun Gou, Yumei Wang, Xianmou Guo, Yuxin Wang, Yan Bian, Haiqing Zhao, Yingyu Guo, Yue Pang, Linlin Xie, Sanming Li, Heran Li
Summary: This study aimed to investigate the delivery of poorly water-soluble non-steroidal antiinflammatory drugs (NSAIDs) by carboxyl-functionalized mesoporous silica nanoparticles (MSN-COOH) with high specific surface area. The results showed that MSN-COOH had high drug loading capacity and exhibited good in vitro drug release properties, leading to improved bioavailability and strong anti-inflammatory effects in vivo.
ACTA BIOMATERIALIA
(2021)
Article
Pharmacology & Pharmacy
Fan Xie, Pedro Fardim, Guy Van den Mooter
Summary: Cellulose beads with high drug loading capacity were developed in this study, showing differences in drug dissolution between amorphous and crystalline forms, as well as a supersaturation phenomenon. The choice of solvent system during preparation greatly impacted the bead structure, resulting in different drug release behaviors. This study highlights the potential of dialdehyde cellulose beads as a carrier for improving poorly soluble drug dissolution and maintaining supersaturation.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Medicine, Research & Experimental
Ridhdhi Dave, Gurpreet Randhawa, Daeun Kim, Madeline Simpson, Todd Hoare
Summary: This review focuses on the design of microgels for the delivery of hydrophobic drugs. Strategies discussed include creating core-shell structures, introducing hydrophobic domains, utilizing host-guest interactions, and applying environmentally responsive materials. The challenge of promoting drug loading without compromising the advantages of microgels as delivery vehicles is also highlighted.
MOLECULAR PHARMACEUTICS
(2022)
Article
Polymer Science
Yubo Liu, Xiaohong Chen, Yuyang Liu, Yuhang Gao, Ping Liu
Summary: In this study, different physicochemical properties of polymeric fibers were successfully prepared for drug delivery system. The results showed that the weaker hydrophilicity of F2 fibers has longer drug dissolution time compared to the better hydrophilic F1 fibers.
Article
Pharmacology & Pharmacy
Vladimir Katev, Sonya Tsibranska-Gyoreva, Zahari Vinarov, Slavka Tcholakova
Summary: Shorter-chain triglycerides are crucial for faster drug release, while solubilization of long-chain triglycerides governs the release of fenofibrate. Additionally, the drop size and surfactant concentration of the lipid carrier also influence the rate of drug release.
Article
Pharmacology & Pharmacy
Jie Zhang, Minzhuo Liu, Zhihong Zeng
Summary: In recent years, the poor solubility of drug candidates in the pharmaceutical industry has posed a challenge. To overcome this issue, various delivery systems, including nanocrystals, cocrystals, nanoparticles, and amorphous solid dispersions, have been developed. Among them, the antisolvent coprecipitation method stands out as a relatively simple and cost-effective approach. This review provides an overview of the recent developments in solubility enhancement using the antisolvent coprecipitation method, emphasizing the process, properties, and factors influencing the efficacy of this approach.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Instruments & Instrumentation
Sajedeh Maghrebi, Nicky Thomas, Clive A. Prestidge, Paul Joyce
Summary: In this study, rifampicin, a poorly soluble and poorly permeable antibiotic, was encapsulated within inulin-lipid hybrid (ILH) particles for the treatment of macrophages infected with small colony variants of Staphylococcus aureus. The pH-responsive properties of ILH microparticles allowed for lysosomal drug release and increased intracellular drug concentration compared to the pure drug. These findings suggest that ILH microparticles can serve as a safe and efficacious delivery system for antibiotics in the treatment of intracellular infections.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2023)
Article
Instruments & Instrumentation
Leah Wright, Anthony Wignall, Silver Joemetsa, Paul Joyce, Clive A. Prestidge
Summary: The gastrointestinal mucus barrier plays a crucial role in protecting the body against harmful pathogens and particles. This study developed a microfluidic device called mucus-on-a-chip (MOAC) to quantify the permeation kinetics of nanoparticles through a synthetic mucus layer. The MOAC revealed differences in permeation patterns and mucoadhesive behavior of different nanoparticle systems, providing insights into mucus binding interactions at a microscopic scale.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Muhammed Awad, Zlatko Kopecki, Timothy J. J. Barnes, Anthony Wignall, Paul Joyce, Nicky Thomas, Clive A. A. Prestidge
Summary: Cutaneous chronic wounds are a global problem affecting millions of people, often complicated by bacterial infections. Staphylococcus aureus is a common bacteria in infected wounds, capable of forming antibiotic-resistant biofilms. Gallium protoporphyrin lipid liquid crystalline nanoparticles (GaPP-LCNP) have shown potential as a photosensitizer against S. aureus biofilms. In this study, GaPP-LCNP demonstrated superior antibacterial activity, reducing biofilm viability and promoting wound healing in pre-clinical models. These findings open doors for further research and optimization of GaPP-LCNP for clinical applications.
Article
Pharmacology & Pharmacy
Amalie Moller, Hayley B. Schultz, Tahlia R. Meola, Paul Joyce, Anette Muellertz, Clive A. Prestidge
Summary: Reformulating poorly water-soluble drugs as supersaturated lipid-based formulations can increase drug loading and potentially improve solubilization and bioavailability. However, for the weak base blonanserin, solidified supersaturated lipid-based formulations with silica have shown reduced solubilization compared to their liquid counterparts. This study aimed to understand the influence of supersaturated drug load on blonanserin solubilization from liquid and solid silica-based supersaturated self-nanoemulsifying drug delivery systems (super-SNEDDS) during in vitro lipolysis.
Article
Chemistry, Physical
Ludivine C. Delon, Matthew Faria, Zhengyang Jia, Stuart Johnston, Rachel Gibson, Clive A. Prestidge, Benjamin Thierry
Summary: Understanding the intestinal transport of particles is crucial for optimizing drug delivery systems and assessing health risks associated with nano- and micro-sized particles in human environment. This study combines an intestine-on-chip model and in silico modeling to demonstrate that particle transcytosis across Caco-2 cell monolayers is significantly higher under fluid shear stress compared to static conditions. The findings reveal the importance of mechanical stimulation in altering cell phenotype and polarity, and highlight the energy-dependent transcytosis process involving clathrin and macropinocytosis.
Article
Biochemistry & Molecular Biology
Yuen Yi Lam, Angel Tan, Cameron J. Nowell, Kristian Kempe, Ben J. Boyd
Summary: Metabolic oligosaccharide engineering (MOE) allows the introduction of functionality to cell membranes through synthetic monosaccharides. MOE enables the expression of unnatural sugars (e.g., peracetylated mannose-azide) on cell surfaces, and the azide group can participate in a copper-free click reaction with an alkyne probe (e.g., dibenzocyclooctyne, DBCO), providing insights into monosaccharide metabolism in cells.
Article
Biochemistry & Molecular Biology
Patrick Tai, Andrew J. Clulow, Ben J. Boyd, Matt Golding, Harjinder Singh, David W. Everett
Summary: Sphingomyelin and cholesterol in the milk fat globule membrane form functional liquid-ordered domains. These domains resist digestion by bile and play a crucial role in gastrointestinal digestion. By using small-angle X-ray scattering, the structural changes in various model bilayer systems were investigated upon interaction with bovine bile. The results showed that the complexation of sphingomyelin with cholesterol can inhibit the disruption of vesicles by bile at lower cholesterol concentrations. The swelling of biliary mixed micelles was influenced by the cholesterol concentration, with less swelling observed at higher cholesterol concentrations. The importance of these findings is discussed.
CHEMISTRY AND PHYSICS OF LIPIDS
(2023)
Article
Pharmacology & Pharmacy
Xiaoyue Xu, Thomas Rades, Holger Grohganz
Summary: It has been observed that water, as a plasticizer, can increase molecular mobility and decrease the glass transition temperature (Tg) in amorphous systems. However, a recent study found an anti-plasticizing effect of water on prilocaine (PRL), which could be used to moderate the plasticizing effect of water in co-amorphous systems. Nicotinamide (NIC) can form co-amorphous systems with PRL. In this study, the Tgs and molecular mobility of hydrated co-amorphous NIC-PRL systems were compared with those of anhydrous systems to investigate the effect of water.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Katharina Holzapfel, Thomas Rades, Claudia S. Leopold
Summary: The influence of an enantiomeric co-former and the preparation method on the solid-state properties and physical stability of co-amorphous systems was investigated in this study. It was found that the chirality of the co-former and the preparation method had an impact on the solid-state properties and physical stability of the systems.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Editorial Material
Pharmacology & Pharmacy
Shyamal Das, Thomas Rades, Arlene McDowell
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Chemistry, Physical
Anas Aljabbari, Abhijeet Girish Lokras, Jacob Judas Kain Kirkensgaard, Thomas Rades, Henrik Franzyk, Aneesh Thakur, Yibang Zhang, Camilla Foged
Summary: We investigated the structural and material properties of siRNA-loaded LPNs using various analytical techniques. The results revealed the self-assembly of lipidoid into lamellar structures, the lateral organization of siRNA between lipidoid bilayers, and the core-shell structure of siRNA-loaded LPNs. The interactions between lipidoid and siRNA were observed, and the inclusion of siRNA affected the phase behavior of lipidoid. These findings contribute to the understanding of siRNA-loaded LPNs and their applications.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Nanoscience & Nanotechnology
Syaza Y. Binte Abu Y. Bakar, Malinda Salim, Andrew J. Clulow, Susanne Seibt, Cornelia B. Landersdorfer, Donna T. Geddes, Kevin R. Nicholas, Ben J. Boyd
Summary: Colostrum provides essential bioactive components for the infant gut microbiota colonization and preventing infectious diseases. However, substitutes are urgently needed for premature infants when colostrum is unavailable. This study aimed to design an appropriate lipid component for a colostrum substitute and evaluate its ability to reduce inflammation in intestinal cells. Analysis showed that the digestion of colostrum and the substitute mixtures had similar lipid profiles but exhibited subtle differences in self-assembly behavior. Bifidobacteria cultured on the substitute mixtures modulated the biological markers of necrotizing enterocolitis, suggesting the potential of these substitutes in reducing the characteristics associated with this disease.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Article
Chemistry, Multidisciplinary
Chiara Pasquarella, Serena Bertoni, Nadia Passerini, Ben J. Boyd, Karlis Berzins
Summary: This study evaluated the performance of different spectral ranges in the kinetic in situ analysis of lipid polymorphic transformations and found that the low-frequency Raman (LFR) domain showed superior characteristics and structural sensitivity.
CRYSTAL GROWTH & DESIGN
(2023)
Article
Pharmacology & Pharmacy
Mengwei Wang, Junbo Gong, Thomas Rades, Ines C. B. Martins
Summary: Ball milling can reduce the particle size of pharmaceutical powders and induce changes in their physical properties. In this study, we prepared three crystal forms of furosemide and used X-ray diffraction and modulated differential scanning calorimetry to characterize the samples. We found that forms I and III directly converted into an amorphous phase, while form II first underwent a polymorphic transition to form I and then gradually lost its crystallinity. The structural relaxation time of the amorphous fraction was longer for forms I and II, while it was shorter for form III, indicating an amorphous-to-amorphous transformation phenomenon.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Medicine, Research & Experimental
Anas Aljabbari, Shinji Kihara, Thomas Rades, Ben J. Boyd, Karlis Berzins
Summary: The adsorption of gut relevant biomolecules onto particles after oral administration of solid oral dosage forms is expected to form a gastrointestinal corona, which could influence solution-mediated solid-state transformations. This study used low-frequency Raman spectroscopy to investigate the in situ solid-state phase transformations under biorelevant conditions and the presence of biomolecules. The results showed a change in the solid-state transformation pathway from amorphous to crystalline drug and the role of biomolecules in influencing these transformations.
MOLECULAR PHARMACEUTICS
(2023)