Article
Pharmacology & Pharmacy
Thitiphorn Rongthong, Thaned Pongjanyakul
Summary: The study aimed to investigate the long-term stability of QPM-MAS nanocomposite film-coated tablets compared to QPM-coated tablets. The results showed that QPM-coated tablets had darker and shinier films after storage, while QPM-MAS-coated tablets showed minor changes in color and appearance. Both types of tablets experienced a decrease in wet mass and drug release rate, and an extension in lag time during storage.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Article
Pharmacology & Pharmacy
Napaphak Jaipakdee, Thitiphorn Rongthong, Watchara Kanjanakawinkul, Thaned Pongjanyakul
Summary: Complexation of nicotine with magnesium aluminum silicate was achieved through physical blending. The formed complexes demonstrated potential as drug carriers in buccal matrix formulations due to their sustained release capabilities.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Chaipat Siriwachirachai, Thaned Pongjanyakul
Summary: The objective of this study was to prepare gelatinized tapioca starch-magnesium aluminum silicate (GTS-MAS) composites for modified-release tablets. GTS and MAS dispersions were prepared and dried to obtain the composites. The GTS-MAS composites showed improved particle flowability and tablet compressibility compared to GTS particles. Increasing MAS ratios resulted in shorter disintegration time and faster drug release due to higher swelling capacity of the composites. These findings suggest that GTS-MAS nanocomposites can be used as matrix formers for modifying drug release in tablets.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Polymer Science
Gustavo Cabrera-Barjas, Liliam Becheran, Oscar Valdes, Ady Giordano, Rodrigo Segura-del Rio, Gaston Bravo-Arrepol, Esteban F. Duran-Lara, Juan Cea, Alex Berg, Johana Castanos, Saddys Rodriguez-Llamazares, Gast on Fuentes, Plamen Katsarov, Paolina Lukova, Cedric Delattre
Summary: The overuse of antibiotics can lead to the development of resistance to targeted bacteria. A controlled release system, such as the nanocomposite films prepared in this study, can provide a solution for achieving higher drug efficiency without overdosing and drug resistance. The films, made from chitosan reinforced with cellulose nanofibrils, showed promising properties for antibiotic release. The content of nanofibers in the film formulation affected the swelling capacity, stiffness, and tensile strength of the films, as well as the release rate of vancomycin, suggesting the potential application of these films for pharmaceutical purposes.
EUROPEAN POLYMER JOURNAL
(2023)
Article
Pharmacology & Pharmacy
Yuki Shirosaki, Yasuyo Tsukatani, Kohei Okamoto, Satoshi Hayakawa, Akiyoshi Osaka
Summary: In this study, the mechanical stability of chitosan-based drug delivery capsules was improved by crosslinking the chitosan and coating them with hydroxyapatite to control the release rate. The injection method was found to result in the highest drug loading.
Article
Chemistry, Physical
Zahra Shariatinia, Mahdieh Ziba
Summary: Chitosan was functionalized and utilized as smart pH-responsive drug delivery systems for the anticancer drug cyclophosphamide. Different synthesized materials showed varied drug release rates under different pH conditions, with CS-AC-U-CP being identified as the most desirable DDS.
SURFACES AND INTERFACES
(2022)
Article
Chemistry, Physical
Bahar Kanci Bozoglan, Osman Duman, Sibel Tunc
Summary: New OXI-loaded hydrogels with high antifungal activity were developed for onychomycosis treatment. The release of OXI from the hydrogels can be controlled by adjusting the amount of MMT in the hydrogel matrix.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2021)
Article
Biochemistry & Molecular Biology
Iryna Kozina, Halina Krawiec, Maria Starowicz, Magdalena Kawalec
Summary: Spin coating technique was used to deposit chitosan coatings on the surface of Mg20Zn magnesium alloy, resulting in increased corrosion resistance by forming CaSiO3 and Ca-3(PO4)(2) compounds on its surface. Corrosion rate was reduced from 3.2 mm/year to 1.2 mm/year for uncoated and coated substrates, respectively.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Engineering, Biomedical
Hongyan Tang, Shuangshuang Li, Yuan Zhao, Cunli Liu, Xuenan Gu, Yubo Fan
Summary: This study investigates the use of poly(trimethylene carbonate) (PTMC) drug-eluting coatings on magnesium alloys for vascular stent application. The PTMC35 coating provides excellent corrosion resistance and drug release ability, effectively inhibiting cell proliferation.
BIOACTIVE MATERIALS
(2022)
Article
Chemistry, Applied
Fumihiko Ohashi, Kenji Arai, Atsushi Shibahara
Summary: A non-crystalline aluminum silicate was synthesized and used as a nanofiller with clear or multicolored aqueous emulsion paint, showing improved wettability and antifouling ability. The exposed Si-OH and Al-OH active sites on the nanofiller surface significantly affect the surface properties of the films.
JOURNAL OF COATINGS TECHNOLOGY AND RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Hossein Ghasemzadeh, Shiravan Afraz, Mohadeseh Moradi, Samira Hassanpour
Summary: The study focuses on the production and characterization of antibacterial and biocompatible films made from chitosan and agarose, as well as the structural analysis of activated agarose. The research demonstrates the potential of these films for applications in food packaging and wound healing due to their strong antibacterial properties against gram-negative and gram-positive bacteria.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Materials Science, Multidisciplinary
Chenchun Chiu, Shaochen Tseng, Chingkong Chao, Xueling Fan, Weihung Cheng
Summary: Film cooling holes and CMAS infiltration have significant effects on temperature and residual stress in thermal barrier coatings. Film cooling holes can alleviate interfacial residual stress, while CMAS infiltration intensifies it. The increase in residual stress is mainly due to the larger penetration depths and expansion rates of phase transformation.
Article
Biochemistry & Molecular Biology
Pegah Sanjarnia, Jhamak Nourmohammadi, Saeed Hesaraki
Summary: This research introduces a new wound dressing made from chitosan and copper-containing Janus nanoparticles (JNPs) that have antibacterial and anti-inflammatory properties. The JNPs were synthesized by attaching copper to PDA nanospheres and were embedded in chitosan at different concentrations. The resulting JNPs showed successful adhesion of Cu2+ ions and increased pore size and porosity with higher JNPs concentration.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Chemistry, Physical
Shao-Wei Bian, Ya-Li Huang, Yuan Yue, Wen Zhang
Summary: In this study, a cotton/magnesium silicate composite film with a hierarchically porous structure was successfully synthesized, showing excellent adsorption properties to methylene blue. The composite film has a high specific surface area and abundant adsorption sites, making it effective in removing pollutants from wastewater.
COLLOIDS AND SURFACES A-PHYSICOCHEMICAL AND ENGINEERING ASPECTS
(2021)
Article
Polymer Science
Fahimeh Farshi Azhar, Mehrnoush Rezaei, Ali Olad, Hanieh Mousazadeh
Summary: The study demonstrated a significant synergistic effect of GO and MMT on the controlled release of GEM, with the nanocomposite containing 17wt% MMT showing optimal drug release rate and content, with a T-50% of about 2 hours. Non-Fickian diffusion mechanism and Korsmeyer-Peppas kinetic model were used to confirm drug release behavior. Additionally, in vitro cytotoxicity assay confirmed the potential of the nanocomposite as a breast cancer therapy system for controlled delivery of GEM.
Article
Pharmacology & Pharmacy
Mahdieh Dagina Pedersen, Andrew Megarry, Kaisa Naelapaa, Thomas Rades, Jenni Pessi
Summary: The compression behavior of oral formulations of proteins and peptides can be challenging due to the addition of poorly compactable permeation enhancers. This study demonstrates that tailoring the properties of peptide or protein particles can overcome the poor compression behavior, particularly in high-dose tablet formulations. Small and non-hollow spray-dried insulin particles showed the most significant enhancement in tabletability, especially in poorly tabletable formulations. The particle properties of the active pharmaceutical ingredient (API) play a crucial role in the manufacturability evaluation of poorly tabletable formulations.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Jacob Rune Jorgensen, Wolfgang Mohr, Matthias Rischer, Andreas Sauer, Shilpa Mistry, Anette Mullertz, Thomas Rades
Summary: In this study, the stability and intrinsic dissolution of vacuum compression molded (VCM) amorphous solid dispersions (ASDs) of efavirenz (EFV) were investigated. The solubility limits of EFV in seven polymers were determined using the melting point depression (MPD) method. The study found that combining preformulation miscibility determination and dissolution studies is important for rational decision-making regarding the stability and viability of ASD formulations.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Yixuan Wang, Thomas Rades, Holger Grohganz
Summary: In this study, the composition evolution of the ternary co-amorphous system CAR-TRP-HPMC was investigated by adding HPMC to previously formed binary systems (CAR - TRP + HPMC, CAR - HPMC + TRP and TRP - HPMC + CAR) prepared by ball milling. The miscibility of CAR with TRP was reduced by the addition of HPMC, as hydrogen bonds formed between CAR and polymer. Phase separation and crystallization of CAR and TRP were observed when their solubility limit in HPMC was exceeded. All ternary co-amorphous systems eventually reached the same composition, but followed different paths depending on the initially used binary system.
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
Instruments & Instrumentation
Mette Klitgaard, Maja Norgaard Kristensen, Ramakrishnan Venkatasubramanian, Priscila Guerra, Jette Jacobsen, Ragna Berthelsen, Thomas Rades, Anette Mullertz
Summary: This study aimed to improve the preclinical evaluation of new oral drug formulations by investigating the DSS-induced colitis model. Various parameters were evaluated, and the disease activity index, colon length, and histological evaluation of the colon were identified as effective indicators of colitis in rats. The study also found that the DSS-induced colitis affected luminal pH, lipase activity, and concentrations of bile salts, polar lipids, and neutral lipids.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2023)
Article
Pharmacology & Pharmacy
Afnan Bany Odeh, Boushra El-Sayed, Matthias Manne Knopp, Thomas Rades, Lasse Ingerslev Blaabjerg
Summary: This study investigates the influence of PVP concentration and molecular weight on the precipitation inhibition of poorly soluble drugs, albendazole, ketoconazole, and tadalafil. The results showed that increasing the PVP concentration leads to a higher onset of nucleation and a lower precipitation rate, while the medium viscosity has no significant effect on the nucleation and precipitation rate.
Article
Pharmacology & Pharmacy
Peter I. I. I. J. G. Remoto, Karlis Berzins, Sara J. Fraser-Miller, Timothy M. Korter, Thomas Rades, Jukka Rantanen, Keith C. Gordon
Summary: The solid-state landscape of carbamazepine during dehydration was investigated using both low- (-300 to -15, 15 to 300 cm(-1)) and mid- (300 to 1800 cm(-1)) frequency Raman spectroscopy. Density functional theory with periodic boundary conditions was employed to characterize the carbamazepine dihydrate and different forms, which showed good agreement with experimental Raman spectra. The dehydration process of carbamazepine dihydrate at various temperatures (40, 45, 50, 55, and 60 ?) was explored using principal component analysis and multivariate curve resolution, revealing different transformation pathways of solid-state forms. Low-frequency Raman spectroscopy was found to effectively detect the rapid growth and subsequent decline of carbamazepine form IV, which was not as well observed by mid-frequency Raman spectroscopy. These findings highlight the potential benefits of low-frequency Raman spectroscopy in pharmaceutical process monitoring and control.
Article
Pharmacology & Pharmacy
Jacob Rune Jorgensen, Wolfgang Mohr, Matthias Rischer, Andreas Sauer, Shilpa Mistry, Thomas Rades, Anette Muellertz
Summary: The use of amorphous solid dispersions (ASDs) is a commonly applied formulation strategy to improve the oral bioavailability of poorly water-soluble drugs. However, establishing a predictive model for the in vitro-in vivo relationship (IVIVR) has been challenging. This study suggests that drug absorption may be overestimated in in vitro dissolution-permeation (D/P) setups, and proposes a modified D/P setup to improve predictability by avoiding direct dissolution of drug particles in the permeation barrier.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(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)
Review
Pharmacology & Pharmacy
Yuehua Deng, Shiyuan Liu, Yanbin Jiang, Ines C. B. Martins, Thomas Rades
Summary: Multicomponent solid forms can enhance the properties of low molecular weight drugs, but predicting their formation in the early stages of formulation development is challenging. Empirical and computational methods have been developed, with artificial intelligence being the latest research focus.
Article
Chemistry, Multidisciplinary
Ines C. B. Martins, Anders S. Larsen, Anders O. Madsen, Olivia Aalling Frederiksen, Alexandra Correia, Kirsten M. O. Jensen, Henrik S. Jeppesen, Thomas Rades
Summary: Polyamorphism is a controversial solid-state phenomenon that is still not fully understood. In this study, three distinct polyamorphic forms of hydrochlorothiazide were discovered and their interconversions were investigated. Molecular dynamics simulations revealed differences in dihedral angle distributions between two of the polyamorphs, which may explain their different physicochemical properties.
Article
Pharmacology & Pharmacy
Greta Camilla Magnano, Marika Quadri, Elisabetta Palazzo, Roberta Lotti, Francesca Loschi, Stefano Dall'Acqua, Michela Abrami, Francesca Larese Filon, Alessandra Marconi, Dritan Hasa
Summary: This study aimed to investigate the loading of sildenafil citrate in three commercial transdermal vehicles using 3D full-thickness skin equivalent and compare the results with permeability experiments using porcine skin. The results showed that the results obtained using the 3D skin equivalent were comparable to those obtained using porcine skin, suggesting that the 3D skin model can be a valid alternative for ex-vivo skin absorption experiments.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
Article
Pharmacology & Pharmacy
James W. Mckeage, Andrew Z. H. Tan, Andrew J. Taberner
Summary: Needle-free jet injection is a promising alternative drug delivery technique that offers rapid, non-invasive, and large-volume injections. The study presents a prototype multi-orifice nozzle and a computational fluid dynamic model to demonstrate the feasibility and effectiveness of this technology.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2024)
