Review
Pharmacology & Pharmacy
Xiaowen Liu, Limin Zhao, Baojian Wu, Fener Chen
Summary: Poorly water-soluble drugs pose a significant challenge in pharmaceutical development due to their low solubility, which can result in reduced bioavailability and therapeutic effectiveness. Efforts have been made to improve the solubility of these drugs for better pharmacokinetics and pharmacodynamics. Protein-based strategies, which offer natural advantages such as versatile interactions with hydrophobic drugs, biocompatibility, biodegradation, and protein metabolism, have gained special interest. This review summarizes the advancements in using proteins, including plant proteins, mammalian proteins, and recombinant proteins, to enhance the water solubility of poorly water-soluble drugs.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
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
Biochemistry & Molecular Biology
Dixit Bhalani, Bhingaradiya Nutan, Avinash Kumar, Arvind K. Singh Chandel
Summary: The low water solubility of pharmacoactive molecules limits their pharmacological potential, and the pharmaceutical industry faces challenges in enhancing the solubility and bioavailability of drugs. However, there are various technologies available to improve the solubility of poorly water-soluble drugs.
Review
Pharmacology & Pharmacy
Naveen K. Thakral, Eva Meister, Corinne Jankovsky, Li Li, Robert Schwabe, Laibin Luo, Shirlynn Chen
Summary: This review explores options for predicting in vivo supersaturation and precipitation of poorly water-soluble drugs, emphasizing the use of a combination of appropriate in vitro tools to obtain optimal predictive information. It discusses theoretical background and relevant case studies to address empirical issues encountered during small-scale and full-scale in vitro predictive testing, and recommends practical considerations for selecting appropriate tools at various stages of drug development. Additionally, upcoming technologies that may further reduce in vivo studies and expedite the drug development process are also discussed.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Review
Chemistry, Physical
Ambreen Shoaib, Bharti Mangla, Shamama Javed, Muhammad H. Sultan, Saad S. Alqahtani, Faiyaz Shakeel
Summary: A drug product should have aqueous solubility to prevent bioavailability issues, which can hinder safety and efficacy. Techniques such as pharmaceutical nanoparticle engineering, specifically liquid crystal technology, have been developed to enhance drug solubility and bioavailability. These new technologies offer potential for improving drug dissolution and efficacy.
JOURNAL OF MOLECULAR LIQUIDS
(2021)
Article
Pharmacology & Pharmacy
Malte Bogh Senniksen, Juliane Fjelrad Christfort, Riccardo Marabini, Erik Spillum, Wayne Matthews, Luigi Da Via, Jakob Plum, Thomas Rades, Anette Mullertz
Summary: This study developed a microgram scale video-microscopic method for screening the dissolution rates of poorly water-soluble drugs. The dissolution rates and particle behavior of the drugs were investigated by tracking particle surface area over time. This method offers a high-throughput approach for drug screening.
Article
Chemistry, Multidisciplinary
Yuntian Xiao, Chuanhua Wu, Shanshan Feng, Kui Chen, Ling Zhou, Qiuxiang Yin
Summary: Addressing the low water solubility challenge of herbicides is crucial to improve their bioavailability and efficacy. Cocrystal engineering has emerged as a promising solution, enhancing dissolution rates and release dynamics of herbicides, improving weed control effectiveness and mitigating environmental impacts.
CRYSTAL GROWTH & DESIGN
(2023)
Article
Pharmacology & Pharmacy
Kazuya Sugita, Noriyuki Takata, Etsuo Yonemochi
Summary: The study found that using solubilizer additive SLS under non-sink conditions can increase the total permeated amount of high-permeable drugs, while not significantly affecting the permeation rate of low-permeable drugs. Even exceeding solubility, the total permeated amount of high-permeable drugs would increase, while that of low-permeable drugs remains almost constant.
Article
Biochemistry & Molecular Biology
Min-Jong Choi, Mi Ran Woo, Han-Gon Choi, Sung Giu Jin
Summary: The study aimed to improve the solubility and dissolution rate of poorly soluble drug rivaroxaban (RXB) by using hydrophilic polymers in a solid dispersion formulation. The optimized polyvinyl alcohol (PVA) and gelatin-based solid dispersion formulations showed significantly higher drug solubilities and improved dissolution rates compared to pure RXB powder.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Elena V. Uspenskaya, Tatiana V. Pleteneva, Ilaha V. Kazimova, Anton V. Syroeshkin
Summary: The most important task in the design of dosage forms is to modify the structure of pharmaceutical substances to increase solubilization, targeted delivery, and bioavailability, with water being the most widely used solvent in the pharmaceutical industry. Modern studies show that isotopic transformations of water can be used to improve the pharmacokinetic properties of medicinal substances.
Article
Pharmacology & Pharmacy
Michaela Slamova, Katerina Prausova, Julie Epikaridisova, Jana Brokesova, Martin Kuentz, Jan Patera, Petr Zamostny
Summary: Co-milling with a proper co-former can enhance the solubility of drugs, and the choice of co-former and consideration of drug properties are important factors affecting dissolution rate. Even without substantial amorphization, co-milling can still positively impact the dissolution behavior of drugs.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Review
Pharmacology & Pharmacy
Smita Salunke, Fiona O'Brien, David Cheng Thiam Tan, David Harris, Marie-Christine Math, Tina Arien, Sandra Klein, Carsten Timpe
Summary: Selecting the appropriate formulation and solubility-enabling technology is crucial for developing formulations for paediatric patients. However, there is a lack of literature in this area, and the need for flexible dosing and adaptations for paediatric subjects pose challenges. An efficient and systematic approach is required to select the best drug delivery system that considers the drug's properties and patient requirements.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Article
Pharmacology & Pharmacy
Miklos Tamas Katona, Lili Nagy-Katona, Reka Szabo, Eniko Borbas, Peter Tonka-Nagy, Krisztina Takacs-Novak
Summary: The purpose of this study was to investigate the applicability of the Gastrointestinal Simulator (GIS) in predicting the in vivo performance of BCS Class IIa compounds. Four immediate release ibuprofen 200 mg formulations were tested using the GIS, and the dissolution results indicated supersaturation in the gastric compartment. A Level A in vitro-in vivo correlation model was established, and the predicted pharmacokinetic parameters matched the statistical output of the clinical study.
Article
Pharmacology & Pharmacy
Fan Xie, Jernej Slak, Pedro Fardim, Guy Van den Mooter
Summary: Cellulose beads modified with ethylenediamine (EDA) were prepared to address the shrinkage and closed pore problem of cellulose beads, and they exhibited acid-responsive swelling ability. The size and ratio of amine groups of the beads influenced the release behavior of model drugs. The cationic beads improved the solubility and dissolution rate of the drugs compared with the crystalline drug. Moreover, the itraconazole-loaded beads maintained a non-crystalline state under certain temperature/humidity conditions.
INTERNATIONAL JOURNAL OF PHARMACEUTICS-X
(2023)
Article
Pharmacology & Pharmacy
Yong-Han Kim, Seong-Bo Kim, Se-Hee Choi, Thi-Thao-Linh Nguyen, Sung-Hoon Ahn, Kyung-Sun Moon, Kwan-Hyung Cho, Tae-Yong Sim, Eun-Ji Heo, Sung Tae Kim, Hyun-Suk Jung, Jun-Pil Jee, Han-Gon Choi, Dong-Jin Jang
Summary: The purpose of this study is to develop and evaluate a self-microemulsifying drug delivery system (SMEDDS) to improve the oral absorption of poorly water-soluble olaparib. The study focused on selecting pharmaceutical excipients and identifying self-emulsifying regions. Various physicochemical properties of the microemulsion incorporating olaparib were investigated, and its improved dissolution and absorption were confirmed. The optimal microemulsion formulation was generated using specific ingredients, and it exhibited good dispersion and stability.
Article
Pharmacology & Pharmacy
Giovanna Bruni, Lauretta Maggi, Loredana Tammaro, Rosadele Di Lorenzo, Valeria Friuli, Sharon D'Aniello, Mariarosa Maietta, Vittorio Berbenni, Chiara Milanese, Alessandro Girella, Amedeo Marini
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2016)
Article
Pharmacology & Pharmacy
Giuseppina Sandri, Maria Cristina Bonferoni, Silvia Rossi, Alessio Delfino, Federica Riva, Antonia Icaro Cornaglia, Giorgio Marrubini, Giorgio Musitelli, Claudia Del Fante, Cesare Perotti, Carla Caramella, Franca Ferrari
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2016)
Article
Chemistry, Applied
P. Capra, G. Musitelli, P. Perugini
INTERNATIONAL JOURNAL OF COSMETIC SCIENCE
(2017)
Article
Chemistry, Medicinal
Doretta Capsoni, Irene Quinzeni, Giovanna Bruni, Valeria Friuli, Lauretta Maggi, Marcella Bini
JOURNAL OF PHARMACEUTICAL SCIENCES
(2018)
Article
Chemistry, Medicinal
Giovanna Bruni, Lauretta Maggi, Piercarlo Mustarelli, Mirena Sakaj, Valeria Friuli, Chiara Ferrara, Vittorio Berbenni, Alessandro Girella, Chiara Milanese, Amedeo Marini
JOURNAL OF PHARMACEUTICAL SCIENCES
(2019)
Article
Thermodynamics
Giovanna Bruni, Mirena Sakaj, Vittorio Berbenni, Lauretta Maggi, Valeria Friuli, Alessandro Girella, Chiara Milanese, Amedeo Marini
JOURNAL OF THERMAL ANALYSIS AND CALORIMETRY
(2019)
Article
Chemistry, Inorganic & Nuclear
Marcella Bini, Francesco Monteforte, Irene Quinzeni, Valeria Friuli, Lauretta Maggi, Giovanna Bruni
JOURNAL OF SOLID STATE CHEMISTRY
(2019)
Article
Polymer Science
Francesco Monteforte, Giovanna Bruni, Irene Quinzeni, Valeria Friuli, Lauretta Maggi, Doretta Capsoni, Marcella Bini
JOURNAL OF INORGANIC AND ORGANOMETALLIC POLYMERS AND MATERIALS
(2020)
Article
Dermatology
Paola Perugini, Stefano Sacchi, Giorgio Musitelli
SKIN RESEARCH AND TECHNOLOGY
(2020)
Article
Pharmacology & Pharmacy
Margherita Bonetti, Marcello Bracchi, Giorgio Musitelli, Paola Perugini
Summary: Studies using bovine hoof membranes as a nail in vitro model primarily focus on permeability, with limited reference to safety and efficacy evaluation of products. The production and characterization of hoof membranes are non-standardized procedures, which can impact the reliability of the model; assessing mechanical properties is particularly challenging due to limited scientific literature coverage. This research presents a feasibility protocol for obtaining a suitable nail model for drug permeability studies or safety and efficacy assessments of final products.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Dalila Miele, Cristian Nomicisio, Giorgio Musitelli, Cinzia Boselli, Antonia Icaro Cornaglia, Rita Sanchez-Espejo, Barbara Vigani, Cesar Viseras, Silvia Rossi, Giuseppina Sandri
Summary: This study aimed to design and develop polydioxanone (PDO) microfibers for tissue engineering using centrifugal spinning. Centrifugal spinning is a more sustainable method that uses centrifugal force and melted materials to produce fibers. Deep eutectic solvents (DES) were used to improve the spinnability of PDO. The multidisciplinary approach allowed for extensive characterization to develop PDO-based microfibers as a medical device for treating full-thickness skin wounds.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Veterinary Sciences
Lauretta Maggi, Valeria Friuli, Paola Perugini, Giorgio Musitelli, Luigi Venco
Summary: The study compared variability in veterinary and human drug products, finding differences in tablet splitting consistency and drug dissolution rates. Some products showed wide variability in tablet splitting, potentially leading to fluctuations in diuretic effects.
OPEN VETERINARY JOURNAL
(2021)
Article
Chemistry, Medicinal
Giovanna Bruni, Vittorio Berbenni, Lauretta Maggi, Piercarlo Mustarelli, Valeria Friuli, Chiara Ferrara, Francesca Pardi, Federica Castagna, Alessandro Girella, Chiara Milanese, Amedeo Marini
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
(2018)