Article
Pharmacology & Pharmacy
Thorsteinn Loftsson
Summary: Benzodiazepines are a class of drugs used to treat a variety of conditions such as anxiety, seizures, and insomnia. They are typically poorly soluble in water and require the use of organic solvents or aqueous solutions with organic cosolvents and surfactants. Midazolam is an exception, being soluble and stable in water without the need for additional solvents.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Article
Medicine, Research & Experimental
Chihiro Tsunoda, Kanji Hasegawa, Ryosuke Hiroshige, Takahiro Kasai, Hideshi Yokoyama, Satoru Goto
Summary: This study investigates the effect of cyclodextrin (CD) on the solubility of drugs in the presence of multiple drug interactions. The results show that ss CD has a synergistic effect on increasing solubility in drug-drug combinations and can effectively improve the dissolution rate of drugs.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Physical
Amy Oo, Panupong Mahalapbutr, Kuakarun Krusong, Ponsiri Liangsakul, Sariyarach Thanasansurapong, Vichai Reutrakul, Chutima Kuhakarn, Phornphimon Maitarad, Atit Silsirivanit, Peter Wolschann, Siyaporn Putthisen, Khanittha Kerdpol, Thanyada Rungrotmongkol
Summary: Encapsulation with beta-cyclodextrin (β-CD) has been explored to enhance the solubility of emodin (ED) for pharmaceutical applications. In this study, inclusion complexation of ED with β-CD and its derivatives was performed to identify the most promising drug carrier. The ED/DM-β-CD complex showed the highest stability and water solubility, followed by ED/SBE7-β-CD and ED/HP-β-CD complexes. The SEM micrographs and DSC thermograms confirmed the inclusion complex formation, and molecular docking suggested C-form insertion as the preferred binding mode. Moreover, the inclusion complexes, especially ED/DM-β-CD, showed significantly higher anti-proliferative effects on cancer cell lines compared to ED alone.
JOURNAL OF MOLECULAR LIQUIDS
(2022)
Article
Medicine, Research & Experimental
Syed Faisal Badshah, Naveed Akhtar, Muhammad Usman Minhas, Kifayat Ullah Khan, Samiullah Khan, Orva Abdullah, Abid Naeem
Summary: The aim of this study was to enhance the solubility of Chlorthalidone by developing beta-cyclodextrin crosslinked hydrophilic nanomatrices. Nine different formulations were fabricated and characterized, showing successful enhancement of solubility. The synthesized nanomatrices exhibited satisfactory in vitro drug release profiles and high solubility compared to the drug alone, with confirmed biocompatibility.
Article
Pharmacology & Pharmacy
Tatyana V. Volkova, Olga R. Simonova, German L. Perlovich
Summary: This study investigated the complex formation of antiandrogen bicalutamide (BCL) with methylated and acetylated beta-cyclodextrins, and its effect on dissolution/permeation processes. The results revealed a higher binding affinity of BCL to acetylated beta-cyclodextrin compared to methylated beta-cyclodextrin. The solid dispersion of BCL with acetylated beta-cyclodextrin showed improved dissolution and supersaturation compared to the raw drug and physical mixture. The presence of polymers (PVP and HPMC) prolonged the supersaturation state and enhanced dissolution and permeation processes.
Article
Polymer Science
Lili Cai, Xueru Xiong, Mingyu Qiao, Jianwei Guo, Huatang Zhang, Jiawei Lin, Sa Liu, Yong-Guang Jia
Summary: In this work, a fluorescent self-healing hydrogel with a dual network structure was developed, where the fluorescence behavior was modulated through host-guest recognition, allowing for fast self-healing and high fluorescence intensity. This hydrogel shows potential for applications as an alpha-amylase sensor or indicator of viscoelastic behavior.
Article
Pharmacology & Pharmacy
Siva Ram Munnangi, Ahmed Adel Ali Youssef, Nagarjuna Narala, Preethi Lakkala, Sateesh Kumar Vemula, Rohit Alluri, Feng Zhang, Micheal A. Repka
Summary: This study evaluated the use of solvent-free hot-melt extrusion for improving the solubility and dissolution of ibuprofen. The results showed that high polymer concentration and high screw speeds had a positive impact on solubility, while higher temperatures had a negative effect. The ternary inclusion complexes produced through hot-melt extrusion exhibited high dissolution.
Article
Biochemistry & Molecular Biology
Elias Christoforides, Athena Andreou, Andreas Papaioannou, Kostas Bethanis
Summary: This study investigates the inclusion complexes of piperine with various cyclodextrins. The crystal structure analysis reveals the formation of stable 1:2 guest:host inclusion complexes in different cyclodextrins. The phase-solubility studies indicate different stoichiometry for the complexes formed between piperine and cyclodextrins.
Article
Pharmacology & Pharmacy
Hina Shoukat, Fahad Pervaiz, Sadia Rehman, Sobia Noreen
Summary: This study aimed to develop and analyze interpenetrating polymer network (IPN) nanogels using hydrophilic polymers beta-cyclodextrin (beta-CD) and chitosan (CS) to enhance the solubility of rosuvastatin (RST). The fabricated nanogels showed improved drug solubility and release parameters, as well as good physicochemical properties and biocompatibility. In vivo experiments demonstrated the antihyperlipidic efficiency of the developed nanogels in hyperlipidemic induced animals.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Pharmacology & Pharmacy
Bhupendra Raj Giri, Hyun Seok Yang, Im-Sook Song, Han-Gon Choi, Jung Hyun Cho, Dong Wuk Kim
Summary: This study developed spray-dried amorphous inclusion complexes of methotrexate (MTX) with beta-cyclodextrin derivatives to enhance the drug's solubility, stability, and oral bioavailability in rats. The findings showed significant improvements in pharmacokinetic profiles with DM-beta-CD as the host, indicating a successful oral formulation technique for preventing drug degradation and enhancing pharmacological properties.
Article
Chemistry, Physical
Emily B. Mobley, Natalie Byrd, Matthew G. Yim, Rachel Gariepy, Maya Rieder, Sandra Ward
Summary: Supramolecular amphiphiles sensitive to GSH were prepared for drug delivery, releasing encapsulated cargo through induced degradation in high GSH concentrations; the dynamic covalent disulfide bond at the vesicle surface can be used for post-modification via thiol-disulfide exchange to enhance targeting.
Article
Chemistry, Multidisciplinary
Suchitra D. Panigrahi, Collin M. Mayhan, Ajaz Ahmad Dar, Steven P. Kelley, Alexander I. Greenwood, Daniel J. Hassett, Carol A. Deakyne, Harshita Kumari
Summary: Host-guest complexes have great potential as supra-molecular drugs in pharmaceutical sciences due to their ability to enhance the activity of antibacterial agents. This study investigated the complexation of macrocyclic hosts with pirfenidone, a FDA-approved antifibrotic drug, to develop a microbiologically potent supramolecular drug. The results revealed an unprecedented interplay between the antibacterial activity of the hosts and their chemical interaction with pirfenidone, thereby improving the overall antibacterial activity of the drug.
CRYSTAL GROWTH & DESIGN
(2023)
Article
Pharmacology & Pharmacy
Phatsawee Jansook, Hay Marn Hnin, Pitsiree Praphanwittaya, Thorsteinn Loftsson, Einar Stefansson
Summary: This study aimed to increase the aqueous solubility of angiotensin II receptor blockers (ARBs) by forming cyclodextrin inclusion complexes and determine their chemical stability in aqueous solutions. The results showed that the solubility of drugs increased by forming inclusion complexes with gamma-cyclodextrin and by increasing their intrinsic solubility in phosphate buffer. The formation of inclusion complexes was confirmed by molecular docking. Salt formation using various organic salts enhanced the solubilization of drugs with gamma-cyclodextrin, but chemical instability was observed at high salt concentrations.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Article
Chemistry, Physical
Qianqian Geng, Pingyang Sun, Gang Tang, Pingliang Li, Yuxiu Zhai
Summary: The water solubility of fludioxonil was improved by generating an inclusion complex with beta-cyclodextrin, leading to enhanced fungicidal activity and reduced toxicity to non-target organisms.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Review
Chemistry, Medicinal
Thorsteinn Loftsson
Summary: Most drugs have limited solubility in water, but cyclodextrins can enhance drug solubility and are preferred in parenteral formulations. Their favorable toxicological and pharmacokinetic profiles make them a preferred choice over other solubilizing techniques.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Engineering, Chemical
Thiago Caon, Jadel Muller Kratz, Gislaine Kuminek, Melina Heller, Ricardo Augusto Konig, Gustavo Amadeu Micke, Leticia Scherer Koester, Claudia Maria Oliveira Simoes
Article
Engineering, Chemical
Manoela Klueppel Riekes, Thiago Caon, Jose da Silva, Regina Sordi, Gislaine Kuminek, Larissa Sakis Bernardi, Carlos Renato Rambo, Carlos Eduardo Maduro de Campos, Daniel Fernandes, Hellen Karine Stulzer
Review
Pharmacology & Pharmacy
Gislaine Kuminek, Fengjuan Cao, Alanny Bahia de Oliveira da Rocha, Simone Goncalves Cardoso, Nair Rodriguez-Hornedo
ADVANCED DRUG DELIVERY REVIEWS
(2016)
Article
Behavioral Sciences
Fabiana K. Ludka, Lori de Fatima Tandler, Gislaine Kuminek, Gislaine Olescowicz, Jonatha Jacobsen, Simone Molz
BEHAVIOURAL PHARMACOLOGY
(2016)
Article
Chemistry, Multidisciplinary
G. Kuminek, N. Rodriguez-Hornedo, S. Siedler, H. V. A. Rocha, S. L. Cuffini, S. G. Cardoso
CHEMICAL COMMUNICATIONS
(2016)
Article
Pharmacology & Pharmacy
Thiago Caon, Jadel Muller Kratz, Gislaine Kuminek, Melina Heller, Gustavo Amadeu Micke, Bibiana Verlindo de Araujo, Leticia Scherer Koester, Claudia Maria Oliveira Simoes
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
(2017)
Article
Chemistry, Multidisciplinary
Alanny B. O. Rocha, Gislaine Kuminek, Tatiane C. Machado, Juliana Rosa, Gabriela S. Rauber, Paola A. A. Borba, Sana Siedler, Hellen K. Stulzer, Silvia Lucia Cuffini, Nair Rodriguez-Hornedo, Simone G. Cardoso
Article
Chemistry, Applied
Manoela Klueppel Riekes, Gislaine Kuminek, Gabriela Schneider Rauber, Carlos Eduardo Maduro de Campos, Adailton Joao Bortoluzzi, Hellen Karine Stulzer
CARBOHYDRATE POLYMERS
(2014)
Article
Chemistry, Multidisciplinary
Manoela K. Riekes, Gislaine Kuminek, Gabriela S. Rauber, Silvia L. Cuffini, Hellen K. Stulzer
CENTRAL EUROPEAN JOURNAL OF CHEMISTRY
(2014)
Article
Behavioral Sciences
Fabiana K. Ludka, Leandra Celso Constantino, Gislaine Kuminek, Luisa Bandeira Binder, Andrea D. E. Zomkowski, Mauricio P. Cunha, Tharine Dal-Cim, Ana Lucia S. Rodrigues, Carla I. Tasca
PHARMACOLOGY BIOCHEMISTRY AND BEHAVIOR
(2014)
Article
Medicine, Research & Experimental
Yaohui Huang, Gislaine Kuminek, Lilly Roy, Katie L. Cavanagh, Quxiang Yin, Nair Rodriguez-Hornedo
MOLECULAR PHARMACEUTICS
(2019)
Article
Chemistry, Multidisciplinary
Gislaine Kuminek, Katie L. Cavanagh, M. Fatima M. da Piedade, Nair Rodriguez-Hornedo
CRYSTAL GROWTH & DESIGN
(2019)
Article
Medicine, Research & Experimental
Katie L. Cavanagh, Gislaine Kuminek, Nair Rodriguez-Hornedo
MOLECULAR PHARMACEUTICS
(2020)
Article
Medicine, Research & Experimental
Niloufar Salehi, Gislaine Kuminek, Jozef Al-Gousous, David C. Sperry, Dale E. Greenwood, Nicholas M. Waltz, Gordon L. Amidon, Robert M. Ziff, Gregory E. Amidon
Summary: Orally dosed drugs need to dissolve in the GI tract before absorption, and in vivo drug dissolution depends on factors such as pH, residence time, and drug properties. Manipulating environmental pH with pH-modifying agents can enhance the dissolution of ionizable drugs. The selection of suitable pH modifiers can improve the dissolution rate and extent of monobasic and dibasic drug compounds under high-gastric pH conditions.
MOLECULAR PHARMACEUTICS
(2021)
Article
Medicine, Research & Experimental
Gislaine Kuminek, Niloufar Salehi, Nicholas M. Waltz, David C. Sperry, Dale E. Greenwood, Siddhi S. Hate, Gregory E. Amidon
Summary: This article discusses the use of in vitro and in silico tools to predict the effect of gastric pH and pH modifiers on the dissolution and absorption of weakly basic drugs. The study successfully predicted drug dissolution and anticipated the impact of proton pump inhibitors and pH-modifying agents using a gastrointestinal simulator and an absorption model. These tools can aid in the development of orally administered formulations to overcome the effect of elevated gastric pH.
MOLECULAR PHARMACEUTICS
(2023)
Article
Materials Science, Biomaterials
Mohammadreza Kasravi, Alireza Yaghoobi, Tahereh Tayebi, Mahsa Hojabri, Abdolkarim Talebi Taheri, Fatemeh Shirzad, Bahram Jambar Nooshin, Radman Mazloomnejad, Armin Ahmadi, Fatemeh A. Tehrani, Ghasem Yazdanpanah, Mohammad Hadi Farjoo, Hassan Niknejad
Summary: As a promising approach in translational medicine, the decellularization of discarded livers to produce bioscaffolds that support recellularization has potential in overcoming the limitations of conventional liver transplantation. In this study, the researchers investigated the use of matrix metalloproteinase (MMP) inhibition to preserve the extracellular matrix (ECM) during liver decellularization. The results demonstrated that the application of an MMP inhibitor significantly improved the preservation of ECM components and mechanical properties of the bioscaffolds, which supported cell viability and function in vitro. The study also confirmed that the MMP inhibition led to the inhibition of MMP2 and MMP9, providing a novel method to enhance ECM preservation during liver decellularization.
BIOMATERIALS ADVANCES
(2024)
Article
Materials Science, Biomaterials
Mohammadsadegh Nadimifar, Weiguang Jin, Clara Coll-Satue, Gizem Bor, Paul Joseph Kempen, Ali Akbar Moosavi-Movahedi, Leticia Hosta-Rigau
Summary: This study presents a metal-phenolic self-assembly approach that can prepare nanoparticles fully made of hemoglobin. The nanoparticles exhibit good oxygen binding and releasing capabilities.
BIOMATERIALS ADVANCES
(2024)
Article
Materials Science, Biomaterials
Jyoti Kumari, Roel Hammink, Jochem Baaij, Frank A. D. T. G. Wagener, Paul H. J. Kouwer
Summary: Fibrosis is the formation of fibrous connective tissue in response to injury, leading to organ dysfunction. A novel hybrid hydrogel combining synthetic polyisocyanide with hyaluronic acid has been developed, showing strong antifibrotic properties.
BIOMATERIALS ADVANCES
(2024)
Letter
Materials Science, Biomaterials
Melissa Machado Rodrigues, Cristian Padilha Fontoura, Charlene Silvestrin Celi Garcia, Sandro Tomaz Martins, Joao Antonio Pegas Henriques, Carlos Alejandro Figueroa, Mariana Roesch Ely, Cesar Aguzzoli
BIOMATERIALS ADVANCES
(2024)
Article
Materials Science, Biomaterials
Jessica Polak, David Sachs, Nino Scherrer, Adrian Suess, Huan Liu, Mitchell Levesque, Sabine Werner, Edoardo Mazza, Gaetana Restivo, Mirko Meboldt, Costanza Giampietro
Summary: Human skin equivalents (HSEs) play a crucial role in tissue engineering. This study introduces a 3D-printed culture insert to apply a static radial constraint on HSEs and examines its effects on tissue characteristics. The results show that the diameter of the culture insert significantly influences tissue contraction, fibroblast and matrix organization, keratinocyte differentiation, epidermal stratification, and basement membrane formation. This study provides important insights for the design of skin tissue engineering.
BIOMATERIALS ADVANCES
(2024)
Review
Materials Science, Biomaterials
Shiliang Chen, Tianming Du, Hanbing Zhang, Jing Qi, Yanping Zhang, Yongliang Mu, Aike Qiao
Summary: This paper reviewed the primary methods for improving the overall properties of biodegradable zinc stents. It discussed the mechanical properties, degradation behavior, and biocompatibility of various improvement strategies. Alloying was found to be the most common, simple, and effective method for improving mechanical properties. Deformation processing and surface modification further improved the mechanical properties and biological activity of zinc alloys. Meanwhile, structural design could endow stents with special properties. Manufacturing zinc alloys with excellent properties and exploring their interaction mechanism with the human body are areas for future research.
BIOMATERIALS ADVANCES
(2024)
