Article
Biochemistry & Molecular Biology
Sofia Teixeira, Maria Alice Carvalho, Elisabete M. S. Castanheira
Summary: Cancer is a major cause of death worldwide. To overcome the problems associated with chemotherapy, the scientific community has developed functionalized nanosystems to deliver drugs to cancer cells, targeting overexpressed receptors, proteins, and organelles. This review focuses on the recent developments of liposomes and albumin-based nanosystems as carriers for poorly water-soluble drugs.
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
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
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)
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)
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
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
Pharmacology & Pharmacy
Xinyue Zhang, Jie Li, Rong Rong, Dangge Wang, Donghai Wang, Yanling Yu, Pei Wu, Yaping Li, Zhiwen Zhang
Summary: A solid nanodispersion system of poorly water-soluble amisupride (AMS) was designed by dispersing AMS into a polymeric matrix. The system exhibited a transformation into nanometer-sized particles upon exposure to gastrointestinal fluids and significantly improved the oral bioavailability of AMS. Compared to the AMS suspension, the absorption of AMS in different parts of the gastrointestinal tract increased significantly by 8.02, 32.18, and 9.11-fold, and the oral bioavailability of AMS was enhanced by 8.58-fold.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Pharmacology & Pharmacy
Eun Ji Ha, Jeong In Seo, Shaheed Ur Rehman, Hyung Soon Park, Sang-Ku Yoo, Hye Hyun Yoo
Summary: In order to address the issue of bioavailability estimation for poorly water-soluble drugs, this study explored a method using a stable isotope tracer. A bioanalytical method using LC-MS/MS was developed to determine the concentration of HGR4113 and its deuterated analog, HGR4113-d7, in rat plasma. The results showed that the current method reduced measurement errors in bioavailability when compared to the conventional approach by eliminating the differences in clearance between oral and intravenous dosages. This study suggests a prominent method for evaluating the bioavailability of drugs with poor aqueous solubility in preclinical studies.
Article
Biophysics
Claudia Pigliacelli, Peter Belton, Peter Wilde, Francesca Baldelli Bombelli, Paul A. Kroon, Mark S. Winterbone, Sheng Qi
Summary: Formulating poorly soluble drugs with polymers as solid dispersions is a common method for improving drug dissolution. This study found that endogenous surface-active species in the gut, such as bile salts and lecithin, play a key role in enhancing the solubilization of lipids and poorly soluble drugs. The addition of a model bile salt, sodium taurocholate (NaTC), to spray dried solid dispersions containing piroxicam and Hydroxypropyl Methylcellulose (HPMC) further improved drug solubilization and resulted in the formation of NaTC-HPMC complexes and other mixed colloidal species. Cellular level absorption studies confirmed that the combination of solid dispersion delivery, bile salts, and lecithin significantly enhanced drug absorption.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Pharmacology & Pharmacy
Denise Steiner, Marius Tidau, Jan Henrik Finke
Summary: The poor bioavailability of newly developed APIs is a challenge in formulation development. Strategies like ASDs, lipid nanocarriers, and nanoparticle wet-milling have been introduced to overcome this issue. Orodispersible films (ODFs) are a promising delivery platform for APIs, as they disintegrate in the mouth. In this study, fenofibrate and naproxen were formulated using different strategies and embedded in ODFs, with ASD-ODFs and API-loaded lipid nanoemulsion films showing the most promising results, reducing dissolution time and achieving short disintegration times.
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
Ayat Abdelkader, Eduard Preis, Cornelia M. Keck
Summary: smartFilm tablets are an innovative and cost-effective formulation approach for improving the oral delivery of poorly water-soluble drugs, demonstrating enhanced dissolution rate and potential for industrial feasibility.
Article
Multidisciplinary Sciences
Riki Kadokawa, Tetsuo Fujie, Gyanendra Sharma, Kojiro Ishibashi, Kazuaki Ninomiya, Kenji Takahashi, Eishu Hirata, Kosuke Kuroda
Summary: This study found that trimethylglycine (TMG) has high solubility in water, which can help dissolve poorly water-soluble drugs such as the anticancer agent cisplatin, increase their concentration, and reduce the dose administered. Additionally, a dry powder can be produced from a cisplatin-containing TMG aqueous solution by freeze-drying for convenient storage and transportation.
SCIENTIFIC REPORTS
(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
Immunology
Carla B. Roces, Maryam T. Hussain, Signe T. Schmidt, Dennis Christensen, Yvonne Perrie
Review
Geriatrics & Gerontology
Zakia B. Shariff, Dania T. Dahmash, Daniel J. Kirby, Shahrzad Missaghi, Ali Rajabi-Siahboomi, Ian D. Maidment
JOURNAL OF THE AMERICAN MEDICAL DIRECTORS ASSOCIATION
(2020)
Article
Crystallography
Nikhila Miriyala, Daniel J. Kirby, Aude Cumont, Ruoying Zhang, Baogui Shi, Defang Ouyang, Haitao Ye
Article
Immunology
Giulia Anderluzzi, Gustavo Lou, Simona Gallorini, Michela Brazzoli, Russell Johnson, Derek T. O'Hagan, Barbara C. Baudner, Yvonne Perrie
Article
Pharmacology & Pharmacy
Carla B. Roces, Emily Charlotte Port, Nikolaos N. Daskalakis, Julia A. Watts, Jonathan W. Aylott, Gavin W. Halbert, Yvonne Perrie
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2020)
Article
Pharmacology & Pharmacy
Swapnil Khadke, Carla B. Roces, Rachel Donaghey, Valeria Giacobbo, Yang Su, Yvonne Perrie
JOURNAL OF PHARMACY AND PHARMACOLOGY
(2020)
Article
Pharmacology & Pharmacy
Zakia Shariff, Daniel Kirby, Shahrzad Missaghi, Ali Rajabi-Siahboomi, Ian Maidment
Article
Pharmacology & Pharmacy
Signe Tandrup Schmidt, Dennis Christensen, Yvonne Perrie
Article
Pharmacology & Pharmacy
Carla B. Roces, Gustavo Lou, Nikita Jain, Suraj Abraham, Anitha Thomas, Gavin W. Halbert, Yvonne Perrie
Article
Pharmacology & Pharmacy
Abdul Latif Ershad, Ali Rajabi-Siahboomi, Shahrzad Missaghi, Daniel Kirby, Afzal Rahman Mohammed
Summary: This study developed a fast, cost-effective, and repeatable swallowability ranking method to screen the in vitro swallowability of solid oral medicines, aiming to assist formulators and the pharmaceutical industry in developing easy-to-swallow formulations.
Article
Pharmacology & Pharmacy
Carlo Curti, Daniel J. Kirby, Craig A. Russell
Summary: The pharmaceutical applications of 3D printing technologies, particularly vat photopolymerisation techniques such as Stereolithography (SLA), have shown great potential in delivering personalized medicines. Traditional SLA apparatus face limitations in throughput and material selection, prompting the development of a novel SLA device for efficient screening of pharmaceutical photopolymer formulations.
Article
Chemistry, Medicinal
Sameer Joshi, Rajnish Sahu, Vida A. Dennis, Shree R. Singh
Summary: The research combines alginate and montmorillonite to produce a soft non-gelatin modified-release capsule, which was critically analyzed for appearance, functionality, and durability. These capsules offer unique advantages in terms of appearance, functionality, and durability.
Article
Pharmacology & Pharmacy
Dilawar Khan, Daniel Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: Due to anatomical and physiological differences between pediatric subsets, it is well established that children respond differently to drugs compared to adults. Orally disintegrating mini-tablets have been considered an age-appropriate formulation option for pediatric use due to their dose flexibility and superior stability.
Article
Pharmacology & Pharmacy
Dilawar Khan, Daniel Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: This article discusses the factors affecting the safety, toxicity, and efficacy of pediatric drug delivery systems, as well as the anatomical and physiological differences between children and adults. It evaluates the advantages, limitations, and acceptability of current pediatric dosage forms, and explores techniques to overcome barriers associated with non-adherence to pediatric medications.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Pharmacology & Pharmacy
Dilawar Khan, Raj Badhan, Daniel J. J. Kirby, Simon Bryson, Maryam Shah, Afzal Rahman Mohammed
Summary: The rapid onset of action of nifedipine can cause a sudden decrease in blood pressure, resulting in adverse effects related to sympathetic nervous system activation. However, there are currently no approved modified release formulations of nifedipine for pediatric use, leading to a lack of pharmacokinetic data in this population. The use of pharmacokinetic modeling, particularly physiological-based pharmacokinetics (PBPK), has revolutionized the ability to predict drug pharmacokinetics in children and support drug licensing and dosing.
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)