Article
Pharmacology & Pharmacy
Eva Petrikova, Jan Patera, Olga Gorlova
Summary: Preformulation is a crucial step in drug development, where the compatibility between API and excipients is determined by Hansen solubility parameters (HSPs) which can also describe the surface properties of substances. In this study, the HSPs of six selected APIs with different chemical nature were determined using inverse gas chromatography (IGC), revealing the influence of API structure on HSPs and the sensitivity of the method to different chemical substances. This provides valuable insights into API behavior during drug development.
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2021)
Article
Chemistry, Physical
Loraine Soumoy, Luca Fusaro, Damien P. Debecker, Carmela Aprile
Summary: The mechanism underlying the growth of hollow silica nanotubes or nanospheres was revealed through in situ liquid-phase transmission electron microscopy. The combination of a surfactant and a swelling agent was crucial for the development of targeted nanostructures. The quantity of surfactant-stabilized toluene droplets was identified as the key parameter guiding the formation of tubular or spherical nanostructures. These findings have led to the preparation of tubular and spherical carriers for the release of an active pharmaceutical ingredient (API).
CHEMISTRY OF MATERIALS
(2023)
Article
Multidisciplinary Sciences
Erik Svensson Grape, Victoria Rooth, Mathias Nero, Tom Willhammar, A. Ken Inge
Summary: In this study, advanced electron microscopy techniques were used to determine the structure of bismuth subsalicylate, a commercially significant compound in over-the-counter medications. The results showed that these techniques provide valuable insights into the structure of active pharmaceutical ingredients that are difficult to characterize using conventional methods.
NATURE COMMUNICATIONS
(2022)
Article
Chemistry, Multidisciplinary
Isaac J. Sugden, Doris E. Braun, David H. Bowskill, Claire S. Adjiman, Constantinos C. Pantelides
Summary: This study proposes a computational approach to identify API/coformer pairs that are unlikely to form experimentally observable cocrystals, saving considerable experimental effort.
CRYSTAL GROWTH & DESIGN
(2022)
Article
Pharmacology & Pharmacy
Ivo B. Rietveld, Hassan Allouchi, Maria Barrio, Rene Ceolin, Josep-Lluis Tamarit
Summary: The crystal structures of dimorphic benzylthiouracil, a drug against hyperthyroidism, have been redetermined, and the atom coordinates of the two independent molecules of form I have been obtained for the first time. The study showed that the low-temperature form II transforms endothermically into form I at 405.4(1.0) K, with form I melting at 496.8(1.0) K. It was also found that form II is denser than form I, and form II is the stable polymorph under ambient conditions.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2021)
Article
Chemistry, Inorganic & Nuclear
Erik Svensson Grape, Victoria Rooth, Simon Smolders, Ambre Thiriez, Sofia Takki, Dirk De Vos, Tom Willhammar, A. Ken Inge
Summary: This study investigates the effect of solvent on the synthesis of bismuth gallate compounds. It was found that using methanol as a solvent resulted in two new bismuth gallates, which transformed into a layered coordination polymer after extended synthesis times. Ethanol, on the other hand, only formed a metal-organic framework (MOF) phase. The methanol-based layered material showed higher stability and was used as a Lewis acid catalyst.
DALTON TRANSACTIONS
(2022)
Article
Chemistry, Multidisciplinary
Mohamed Labib, Laura Grabowski, Christian Bruesseler, Nicolai Kallscheuer, Luisa Wachtendonk, Thomas Fuchs, Andreas Jupke, Wolfgang Wiechert, Jan Marienhagen, Doerte Rother, Stephan Noack
Summary: This study achieved the microbial production of pyruvate and L-alanine in a one-pot fermentation process, and then transformed them into Metaraminol with high yields and stereoselectivity through a series of reactions.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2022)
Article
Chemistry, Applied
David J. J. Lamberto, Eric Sirota, George Zhou
Summary: Drying of a crystalline hydrate form of an active pharmaceutical ingredient was studied using a small-scale flow cell methodology. A new experimental tool was developed, which used a segregated column technique to quickly identify different drying mechanisms with minimal experiments. The results showed that increasing vacuum levels improved solvent removal, while nitrogen flow through the solids facilitated water removal. The impact of crystallization solvent system and washing on drying behavior and cake properties were also assessed, and a system that improved drying performance was identified.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2023)
Article
Chemistry, Applied
Muhid Shahid, Chloe Faure, Sara Ottoboni, Leo Lue, Chris Price
Summary: The study aims to improve pharmaceutical product quality, increase sustainability, and reduce manufacturing cost through optimizing the washing process. It is important to avoid product dissolution and impurity precipitation during washing, especially caused by wash solvents acting as antisolvents. Constant rate filtration allows for collection of separate aliquots during washing stages to optimize the washing strategy.
ORGANIC PROCESS RESEARCH & DEVELOPMENT
(2022)
Article
Chemistry, Multidisciplinary
Fabian Herbrik, Miguel Sanz, Alessandra Puglisi, Sergio Rossi, Maurizio Benaglia
Summary: This study investigated the continuous flow, enantioselective, organophotoredox catalytic asymmetric alkylation of aldehydes using a homemade photoreactor. Significant productivity increase was achieved compared to batch reactions, and the synthesis of an active pharmaceutical ingredient (API) in high enantioselectivity was successfully demonstrated.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Bernhard Blank-Landeshammer, Gerald Klanert, Lisa Mitter, Sophia Turisser, Nicolas Nusser, Alice Koenig, Marcus Iken, Julian Weghuber
Summary: Intestinal absorption of lipophilic micronutrients and phytochemicals is usually low, but plant extracts can enhance their bioavailability. This study investigated the effects of extracts from curcuma, ginger, and black pepper on the uptake and transport rates of lutein, zeaxanthin, and soy isoflavones. It was found that curcuma extract increased lutein uptake, while curcuma and ginger extracts enhanced isoflavone transport rates.
Review
Biotechnology & Applied Microbiology
Vinod Kumar, Vasudha Bansal, Aravind Madhavan, Manoj Kumar, Raveendran Sindhu, Mukesh Kumar Awasthi, Parameswaran Binod, Saurabh Saran
Summary: The aim of this article is to develop a framework for bio-based economy through the effective utilization of biomass from agriculture in order to produce potential bio-based products such as pharmaceuticals and active pharmaceutical ingredients. The article also discusses the conservation of bioenergy and the development of bio-based products and biofuels. It showcases the fundamental principles for producing these by-products. The creation of these products is necessary to meet the local needs for bio-based materials and energy by small-scale farmers, and the establishment of small markets will provide opportunities for larger markets.
Article
Chemistry, Multidisciplinary
Jessica L. Andrews, Stuart R. Kennedy, Dmitry S. Yufit, James F. McCabe, Jonathan W. Steed
Summary: We present an approach to stabilize metastable polymorphs of the pharmaceutical salt mexiletine hydrochloride using drug-mimetic supramolecular gelators. The gelators led to the discovery of new solvated solid forms of mexiletine, including highly polymorphic and difficult-to-nucleate forms. These findings highlight the potential of drug-mimetic supramolecular gels in pharmaceutical polymorph screens.
CRYSTAL GROWTH & DESIGN
(2022)
Article
Chemistry, Multidisciplinary
Jessica L. Andrews, Stuart R. Kennedy, Dmitry S. Yufit, James F. McCabe, Jonathan W. Steed
Summary: We present a method to stabilize the polymorphic forms of mexiletine hydrochloride, a highly polymorphic antiarrhythmic drug, using drug-mimetic supramolecular gelators. Through crystallization within the gels, various metastable forms and solid forms that cannot be obtained in solution were obtained. This approach has potential applications in pharmaceutical polymorph screens for accessing highly metastable or difficult-to-nucleate solid forms.
CRYSTAL GROWTH & DESIGN
(2022)
Article
Chemistry, Multidisciplinary
Samir Diab, Mateen Raiyat, Dimitrios I. Gerogiorgis
Summary: Continuous flow synthesis offers improved mixing and heat transfer, leading to higher yields and reaction selectivity. Estimating reaction kinetic parameters from flow synthesis data is crucial for developing reactor models in drug substance manufacturing.
REACTION CHEMISTRY & ENGINEERING
(2021)
Review
Chemistry, Multidisciplinary
Mithun Rajendra Dethe, A. Prabakaran, Hafiz Ahmed, Mukta Agrawal, Upal Roy, Amit Alexander
Summary: Stimuli-responsive hydrogels have been extensively studied in biomedical applications due to their biodegradability and biocompatibility. The emergence of in situ stimuli-responsive hydrogels is the result of advancements in synthetic chemistry and materials science. The copolymer PCL-PEG, recognized by the FDA, can form thermosensitive injectable hydrogels that exhibit rapid and reversible gelation behavior.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Pharmacology & Pharmacy
Mukta Agrawal, Madhulika Pradhan, Gautam Singhvi, Ravish Patel, Ajazuddin, Amit Alexander
Summary: Curcumin has been shown to have antioxidant, anti-inflammatory, amyloid inhibition, and neuroprotective properties, but its poor solubility, lipophilicity, rapid metabolism, and short half-life limit its efficacy in treating AD. This study developed curcumin-loaded solid lipid nanoparticles (CSL) to improve the physicochemical properties and achieved prolonged release. However, the loading reduced the antioxidant potency of curcumin.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Vivek Phatale, Klaudi K. Vaiphei, Shikha Jha, Dnyaneshwar Patil, Mukta Agrawal, Amit Alexander
Summary: Transdermal drug delivery system (TDDS) is a potential approach for effective drug delivery, with advantages such as easy administration, controlled release, and prolonged therapeutic effect. Poor skin permeability is a primary challenge, but can be overcome through fusion with other methods. This article summarizes the fundamental features, components, and design of TDDS, as well as methods for assessing skin permeability. It also explores the application of active methods and passive methods in transdermal drug delivery.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Medicine, Research & Experimental
Sarita Rani, Rakesh K. Sahoo, Vinay Kumar, Akash Chaurasiya, Onkar Kulkarni, Ashutosh Mahale, Sumeet Katke, Kaushik Kuche, Vivek Yadav, Sanyog Jain, Kartik T. Nakhate, Ajazuddin, Umesh Gupta
Summary: Breast cancer is the deadliest disease among women, and multidrug therapy has shown greater efficacy compared to monodrug therapy. Caffeic acid and bortezomib have potential anticancer and antioxidant properties. A HP-PCL PMCs system was developed for simultaneous delivery of bortezomib and caffeic acid in breast cancer treatment. In vitro and in vivo experiments demonstrated that the designed PMCs system exhibited enhanced therapeutic efficiency against breast cancer.
MOLECULAR PHARMACEUTICS
(2023)
Article
Polymer Science
Urushi Rehman, Mohammed A. S. Abourehab, Amit Alexander, Prashant Kesharwani
Summary: Pancreatic cancer (PC) is a deadly disease with a low 5-year survival rate and is expected to become the second leading cause of cancer-related deaths in the United States by 2030. Treatment options are limited and the tumor microenvironment hinders therapeutic agents. Combining chemotherapeutics using nanoparticle-mediated delivery, such as micelles, shows promise in improving treatment outcomes and reducing side effects.
EUROPEAN POLYMER JOURNAL
(2023)
Review
Chemistry, Multidisciplinary
Tejas Girish Agnihotri, Amit Alexander, Mukta Agrawal, Sunil Kumar Dubey, Aakanchha Jain
Summary: Understanding the interaction between nanoparticles and biological systems is a challenge in nanotherapeutics. Protein corona plays a crucial role in cellular uptake and in vivo behavior of nanoparticles. In vitro dissolution testing and in vitro in vivo correlation (IVIVC) are useful approaches to evaluate the fate of nanoparticles. This review emphasizes the importance of protein corona, factors affecting the interaction, and various dissolution media for different nanocarrier systems, and discusses the limitations and regulatory perspective of IVIVC.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Chemistry, Inorganic & Nuclear
Krushna Rathod, Hafiz Ahmed, Shyam Sudhakar Gomte, Sourav Chougule, A. Prabakaran, Mithun Rajendra Dethe, Ravish J. Patel, P. V. P. Deepak Bharadwaj, Amit Alexander
Summary: Berberine chloride was loaded into synthesized mesoporous silica nanoparticles (MSNs) with high surface area and pore volume, and the drug loading and release kinetics were studied. The study demonstrated the superior anti-inflammatory efficacy of BBR-MSNs in animal models.
JOURNAL OF SOLID STATE CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Darshani Patil, Ajazuddin, Sankha Bhattacharya
Summary: Autoimmune diseases are increasing in prevalence, and biologicals are playing a crucial role in their treatment by targeting specific cytokines and suppressing inflammation. Tumor Necrosis Factor-alpha (TNFa) inhibitors and Interleukin Inhibitors (IL) are common classes of biologics used for treating autoimmune diseases. In addition, nanomedicine has shown promising results in delivering drugs to targeted organs or tissues without causing unwanted immune effects. This article provides an overview of biologics in autoimmune disease treatment, their mechanisms, and the use of nanosystems in clinical trials.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2023)
Article
Parasitology
Mukesh Sharma, Amit Alexander, Kartik T. Nakhate, Kapil Kumar Nagwanshi, Ajazuddin
Summary: In this study, the larvicidal efficacy of Lantana camara and Ocimum gratissimum juices against mosquito larvae was evaluated. The results showed significant larvicidal activity after 24 hours of exposure, indicating that these plant juices may serve as effective, economical, and eco-friendly larvicidal agents.
EXPERIMENTAL PARASITOLOGY
(2023)
Review
Pharmacology & Pharmacy
Dhananjay Bhatane, Sharon Rose Pamshong, Santosh Sarnaik, A. Prabakaran, Amit Alexander
Summary: Neurological disorders pose an emerging threat to public health, and traditional therapy is unable to fully cure these disorders due to poor blood-brain barrier permeability. Scientists have focused on developing novel drug delivery carriers, such as mesoporous silica nanoparticles, to improve drug delivery to the brain. These nanoparticles have unique properties that make them suitable for delivering drugs to the brain and have been extensively studied for treating neurological disorders.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Chemistry, Physical
Nidhi Malviya, A. Prabakaran, Amit Alexander
Summary: The present study aimed to improve the permeability of sinapic acid (SA) across the skin by preparing vesicular nanoformulations such as transferosomes and ethosomes. The results showed that ethosomes exhibited higher permeability compared to transferosomes and plain SA hydrogel, which was attributed to their flexibility across the skin.
JOURNAL OF MOLECULAR LIQUIDS
(2023)
Review
Chemistry, Multidisciplinary
Shailvi Shah, Amit A. A. Patel, Bhupendra G. G. Prajapati, Amit Alexander, Vidhi Pandya, Nidhi Trivedi, Punit Pandey, Samir G. G. Patel, Ravish J. J. Patel
Summary: The exponential growth of nanotechnology has led to the development of nanocarriers for therapeutic purposes, particularly in the treatment of brain disorders. Nanostructured lipid carriers (NLC) have gained significant attention as alternative pharmaceutical delivery systems, offering improved stability and various applications such as gene therapy and cancer treatment. This review thoroughly covers the uses and significance of NLCs in combating brain diseases, highlighting their potential through recent research papers and patents. NLCs show promise in nose-to-brain drug delivery, offering targeted delivery, reduced toxicity, and increased bioavailability.
JOURNAL OF NANOPARTICLE RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Ravish Patel, Rashesh Desai, Amit Patel, Shailvi Shah, Bhupendra Prajapati, Viral Patel, Amit Alexander
Summary: Burns can result from electricity, radiation, chemicals, or friction, causing severe damage to the skin and potentially leading to cell death. Burns are a painful and crucial issue that can result in disabilities and even mortality. The severity of burns is classified into three degrees, with third-degree burns being the most severe and requiring critical care.
JOURNAL OF RESEARCH IN PHARMACY
(2023)
Article
Biophysics
Sharon Rose Pamshong, Dhananjay Bhatane, Santosh Sarnaik, Amit Alexander
Summary: Proteins and peptides (PPs) have advantages as therapeutics, but their effective delivery and bioavailability are challenging due to their large size and susceptibility to environmental conditions. Nanoparticle-based delivery systems, such as mesoporous silica nanoparticles (MSNs), show potential for protecting and delivering PPs to the target site.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2023)
Article
Chemistry, Medicinal
Saeed Reza Simaei, Vahid Reza Askari, Mahboobeh Rostami, Mohammad Kamalinejad, Mohammad Hosein Farzaei, Mohammadreza Morovati, Fatemeh Heydarpour, Zahra Jafari, Vafa Baradaran Rahimi
Summary: This study demonstrates that lavender and metformin have similar effects in treating PCOS patients, as both significantly increase progesterone levels and regulate menstrual cycles.
Article
Chemistry, Medicinal
Peng-Ran Cao, Xiao Ren, Jie Lin, Yun-Long Mu, Yue-Qi Shan, Jing-Tong Zhu, Rong-Yi Xu, Xue-Xia Zhang, Wei-Guo Hu, Xin-Hua Lu
Summary: Four previously unknown angucyclinones umezawaones A-D (1-4) were isolated from the liquid cultures of Umezawaea beigongshangensis. Their structures were determined using spectroscopic analysis, single crystal X-ray diffraction, quantum chemical 13C NMR, and electronic circular dichroism calculations. All compounds exhibited potent inhibitory activities against indoleamine 2,3-dioxygenase and tryptophan-2,3-dioxygenase in enzymatic assays, with compound 2 showing the highest activity.
Article
Chemistry, Medicinal
Marwa Mersni, Bingqing Zhou, Guillaume Reversat, Mohamed Larbi Khouja, Alexandre Guy, Camille Oger, Jean-Marie Galano, Thierry Durand, Chokri Messaoud, Claire Vigor
Summary: The relevance of oxylipins as biomarkers of oxidative stress has been established in recent years. This study evaluated the lipidomic profiling of different aerial parts of Acacia cyanophylla Lindl. using LC-MS/MS technology for the first time. The analysis revealed the existence of six PhytoPs and three PhytoFs, with stems having the highest amount of these metabolites. This study provides a foundation for exploring Acacia cyanophylla Lindl. as a potential source of plant oxylipins for therapeutic or pharmaceutical uses.
Review
Chemistry, Medicinal
Lorenzo Buzzelli, Andrea Segreti, Daniela Di Gioia, Erika Lemme, Maria Rosaria Squeo, Antonio Nenna, Giuseppe Di Gioia
Summary: This review provides a comprehensive assessment of red yeast rice, including its biochemical composition, historical studies, cardiovascular disease prevention, and other clinical effects. Red yeast rice preparations have been proven safe and effective in improving lipid profiles, with a potential role in reducing cardiovascular risk.
Article
Chemistry, Medicinal
Xiuwen Zheng, Yuxin Zhang, Yinfeng Tan, Yonghui Li, Qianrong Xue, Hailong Li, Xuguang Zhang, Yipeng Pan, Jian Xu, Junqing Zhang
Summary: Alpinia officinarum Hance (AOH) may protect against diabetic gastroparesis (DGP) through multiple mechanisms, including lowering blood glucose levels, increasing gastrointestinal propulsion rate, improving gastric histological morphology, and regulating gut microbiota.
Article
Chemistry, Medicinal
Na Chen, Rui Xie, Jia-pei Chen, Ying-li Zhong, Xian-wen Zhang, Qing-wen Gui, Chun Guo, Hua Yang
Summary: The study clones the SinSyn gene from Sinomenium acutum and analyzes its catalytic activity, confirming the biosynthetic pathway of sinoacutine and discussing its classification and pharmacological action.
Article
Chemistry, Medicinal
Noura Bentarhlia, Badr Eddine Kartah, Mouhcine Fadil, Said El Harkaoui, Bertrand Matthaeus, Oualid Abboussi, Hanaa Abdelmoumen, Omar Bouhnik, Hanae El Monfalouti
Summary: The lipidic extract of Dittrichia viscosa exhibits significant wound healing activity and antimicrobial effects. It is rich in fatty acids such as linolenic acid, oleic acid, and linoleic acid, as well as compounds like gamma-tocopherols and sterols.
Article
Chemistry, Medicinal
Hawraa Zbeeb, Hala Khalifeh, Giulio Lupidi, Francesca Baldini, Lama Zeaiter, Mohamad Khalil, Annalisa Salis, Gianluca Damonte, Laura Vergani
Summary: This study assessed the biological properties of S. spinosum fruits and found that the ethanolic extract exhibited significant anti-steatotic and antioxidant activities.
