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Rosa Camacho-Sandoval, Eréndira N Sosa-Grande, Edith González-González, Alejandra Tenorio-Calvo, Carlos A López-Morales, Marco Velasco-Velázquez, Lenin Pavón-Romero, Sonia Mayra Pérez-Tapia, Emilio Medina-Rivero
Physicochemical and structural properties of proteins used as active pharmaceutical ingredients of biopharmaceuticals are determinant to carry out their biological activity. In this regard, the assays intended to evaluate functionality of biopharmaceuticals provide confirmatory evidence that they contain the appropriate physicochemical properties and structural conformation. The validation of the methodologies used for the assessment of critical quality attributes of biopharmaceuticals is a key requirement for manufacturing under GMP environments...
March 30, 2018: Journal of Pharmaceutical and Biomedical Analysis
Andrea Arsiccio, Roberto Pisano
PURPOSE: Surfactants are common stabilizers, often added to biopharmaceuticals formulations, but the mechanisms at the basis of their activity are unclear. The aim of this work is to provide insight into the molecular factors underlying surfactant effectiveness as protectants. METHODS: Molecular Dynamics simulations of human growth hormone (hGH) in the presence of Tween 20 were performed. The effect of Tween 20 was compared with the activity of commonly used protectants, such as the disaccharides...
April 10, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Young-Im Kim, Hyun-Woo Shin, Yang-Sook Chun, Jong-Wan Park
The final strategies to care patients with end-stage renal fibrosis rely on dialysis and kidney transplantation. Because such treatments are invasive and cause health problems eventually, it is necessary to develop new therapeutic strategies for delaying the disease progress. We here searched for cytokines showing an anti-fibrotic activity in cell-based experiments. Cystatin C (CST3) and Growth differentiation factor 15 (GDF15) were identified to have anti-fibrotic activities in a cytokine array screening. In primary fibroblasts isolated from the mouse kidneys subjected to ureteral obstruction-induced fibrosis, each cytokine induced apoptotic cell death and reduced collagen production...
April 13, 2018: Biochemical and Biophysical Research Communications
Manmeet S Ahluwalia, Kevin Becker, Benjamin P Levy
Central nervous system (CNS) metastases are a common complication in patients with epidermal growth factor receptor (EGFR)-mutated non-small cell lung cancer (NSCLC), resulting in a poor prognosis and limited treatment options. Treatment of CNS metastases requires a multidisciplinary approach, and the optimal treatment options and sequence of therapies are yet to be established. Many systemic therapies have poor efficacy in the CNS due to the challenges of crossing the blood-brain barrier (BBB), creating a major unmet need for the development of agents with good BBB-penetrating biopharmaceutical properties...
April 12, 2018: Oncologist
Gangliang Huang, Hualiang Huang
Hyaluronic acid (HA) is a natural polysaccharide with good biocompatibility and degradability. HA and its derivatives can be used as sustained-release carriers for drugs, which can delay the release of drugs and have a long-acting effect. They can be used for the delivery of various drugs such as proteins, nucleic acids and anti-tumor drugs. HA and its derivatives can specifically bind to multiple receptors on the cell surface and can be used for targeted drug delivery, especially for the delivery of anti-tumor drugs...
April 9, 2018: Journal of Controlled Release: Official Journal of the Controlled Release Society
Frank Theil, Johanna Milsmann, Sankaran Anantharaman, Holger van Lishaut
The preparation of an amorphous solid dispersion (ASD) by dissolving a poorly water-soluble active pharmaceutical ingredient (API) in a polymer matrix can improve the bioavailability by orders of magnitude. Crystallization of the API in the ASD, though, is an inherent threat for bioavailability. Commonly, the impact of crystalline API on the drug release of the dosage form is studied with samples containing spiked crystallinity. These spiked samples possess implicit differences compared to native crystalline samples, regarding size and spatial distribution of the crystals as well as their molecular environment...
April 12, 2018: Molecular Pharmaceutics
Joanna Rucker-Pezzini, Lindsay Arnold, Kevin Hill-Byrne, Tom Sharp, Maksim Avazhanskiy, Chris Forespring
The concept of continuous manufacturing has gained significant interest from the biopharmaceutical industry over the past several years. Benefits include increased manufacturing productivity, improved quality control, reduction in plant footprint, and more flexible management of facility capacity. There are several technologies currently available that enable continuous processing for chromatography and ultrafiltration. However, a single pass diafiltration design that meets the required small molecule clearance and has been integrated into a fully continuous monoclonal antibody purification process has not been previously published...
April 12, 2018: Biotechnology and Bioengineering
Aditya Tulsyan, Christopher Garvin, Cenk Undey
Biopharmaceutical manufacturing comprises of multiple distinct processing steps that require effective and efficient monitoring of many variables simultaneously in real-time. The state-of-the-art real-time multivariate statistical batch process monitoring (BPM) platforms have been in use in recent years to ensure comprehensive monitoring is in place as a complementary tool for continued process verification to detect weak signals. This article addresses a longstanding, industry-wide problem in BPM, referred to as the 'Low-N' problem, wherein a product has a limited production history...
April 6, 2018: Biotechnology and Bioengineering
Noriyasu Kamei, Ai Yamaoka, Yukiko Fukuyama, Rei Itokazu, Mariko Takeda-Morishita
To overcome the difficulty in delivery of biopharmaceuticals such as peptides and proteins to the brain, several approaches combining the ligands and antibodies targeting the blood-brain barrier (BBB) have been tried. However, these are inefficient in terms of their permeability through the BBB and structural modification of bioactive drugs. In the present study, we therefore examined the usefulness of a noncovalent method using the cell-penetrating peptides (CPPs) such as octaarginine (R8) as a suitable brain delivery strategy for biopharmaceuticals...
2018: Biological & Pharmaceutical Bulletin
Shimul Halder, Aiko Tabata, Yoshiki Seto, Hideyuki Sato, Satomi Onoue
Carvedilol (CAR) belongs to biopharmaceutics classification system class-II drugs, with poor aqueous solubility and pH-dependent solubility. The present study aimed to develop a novel amorphous solid dispersion (ASD) of CAR with acidic counter ions for pH modifications in microenvironment to improve the pharmacokinetic properties under hypochlorhydric conditions. CAR-ASD was prepared by freeze-drying in combination with counter ions and hydroxypropyl cellulose, and their physicochemical properties including dissolution behavior, storage stability, and photostability were characterized...
April 2, 2018: Biopharmaceutics & Drug Disposition
Colin M McGill, Timothy J Brown, Yuan-Yin Cheng, Lindsey N Fisher, Sriram S Shanmugavelandy, Sally J Gustafson, Kriya L Dunlap, Mary Ann Lila, Mark Kester, Paul T Toran, David F Claxton, Brian M Barth
Acute myeloid leukemia (AML) is an aggressive hematological malignancy with high incidence in the aging population. In addition, AML is one of the more common pediatric malignancies. Unfortunately, both of these patient groups are quite sensitive to chemotherapy toxicities. Investigation of blueberries specifically as an anti-AML agent has been limited, despite being a prominent natural product with no reported toxicity. In this study, blueberry extracts are reported for the first time to exert a dietary therapeutic effect in animal models of AML...
January 2018: International Journal of Biopharmaceutical Sciences
Manuel Ibarra, Cristian Valiante, Patricia Sopeña, Alejandra Schiavo, Marianela Lorier, Marta Vázquez, Pietro Fagiolino
Bioequivalence implementation in developing countries where a high proportion of similar drug products are being marketed has found several obstacles, impeding regulatory agencies to move forward with this policy. Biopharmaceutical quality of these products, several of which are massively prescribed, remains unknown. In this context, an in vitro-in silico-in vivo approach is proposed as a mean to screen product performance and target specific formulations for bioequivalence assessment. By coupling in vitro biorelevant dissolution testing in USP-4 Apparatus (flow-through cell) with physiologically-based pharmacokinetic (PBPK) modeling in PK-Sim® software (Bayer, Germany), the performance of seven similar products of carvedilol tablets containing 25 mg available in the Uruguayan market were compared with the brand-name drug Dilatrend®...
March 29, 2018: European Journal of Pharmaceutical Sciences
J Gross, N Herrmann, M Blech, S R Pinnapireddy, P Garidel, U Bakowsky
Particle detection and analysis techniques are essential in biopharmaceutical industries to evaluate the quality of various parenteral formulations regarding product safety, product quality and to meet the regulations set by the authority agencies. Several particle analysis systems are available on the market, but for the operator, it is quite challenging to identify the suitable method to analyze the sample. At the same time these techniques are the basis to gain a better understanding in biophysical processes, e...
March 28, 2018: International Journal of Pharmaceutics
Maximilian Sager, Philipp Jedamzik, Simon Merdivan, Michael Grimm, Felix Schneider, Marie-Luise Kromrey, Mahmoud Hasan, Stefan Oswald, Jens Kühn, Mirko Koziolek, Werner Weitschies
Improving our knowledge about human gastrointestinal physiology and its impact on oral drug delivery is crucial for the development of new therapies and effective drug delivery systems. The aim of this study was to develop an in vivo tool to determine gastric emptying of water by administration of a caffeine as a tracer substance followed by subsequent saliva caffeine analysis. For this purpose, 35mg of caffeine were given to six healthy volunteers after a 10h overnight together with 240mL of tap water either on a fasted stomach or 30min after the high-caloric, high-fat breakfast recommended for bioavailability/bioequivalence (BA/BE) studies...
March 27, 2018: European Journal of Pharmaceutics and Biopharmaceutics
Kashappa Goud Desai, Hirokazu Obayashi, James D Colandene, Douglas P Nesta
Japan represents the third largest pharmaceutical market in the world. Developing a new biopharmaceutical drug product for the Japanese market is a top business priority for global pharmaceutical companies while aligning with ethical drivers to treat more patients in need. Understanding Japan-specific key regulatory requirements is essential to achieve successful approvals. Understanding the full context of Japan-specific regulatory requirements/expectations is challenging to global pharmaceutical companies due to differences in language and culture...
March 27, 2018: Journal of Pharmaceutical Sciences
Jun-Rui Zhao, Xiao-Liang Ren, Meng Wang
Nuciferin is the main active ingredients in Nelumbinis Folium, which was proved to have good hypolipidemic, antioxidative and anti-inflammatory bioactivities. Currently, in vivo pharmacokinetic studies of nuciferin showed different results based on different animal models. In vitro evaluation experiments were low-cost, stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable in vitro simulation method to evaluate the bioavailability of oral drugs. It was a scientific framework for classifying drugs or active pharmaceutical ingredients(API) according to their solubility and impermeability in vitro ...
February 2018: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
Marton Szigeti, Jeff Chapman, Beata Borza, Andras Guttman
The attached carbohydrates at the highly conserved asparagine-linked glycosylation site in the CH 2 domain of the fragment crystallizable (Fc) region of monoclonal antibody therapeutics can play an essential role in their mechanism of action, including ADCC, CDC, anti-inflammatory functions, and serum half-life. Thus, this particular glycosylation represents one of the important critical quality attributes (CQA) of therapeutic monoclonal antibodies, which should be closely monitored and controlled during all stages of biopharmaceutical manufacturing...
March 30, 2018: Electrophoresis
Atul Jain, Rajpreet Kaur, Sarwar Beg, Varun Kushwah, Sanyog Jain, Bhupinder Singh
The work describes systematic development of nanomicellar cationic supersaturable self-nanoemulsifying drug delivery systems (CS-SNEDDS) for augmenting oral biopharmaceutical performance of raloxifene hydrochloride. Plain SNEDDS formulation containing Capryol 90, Cremophor RH 40, and Transcutol HP was optimized using D-optimal mixture design. SNEDDS were characterized for emulsification time, globule size, in vitro drug release, and ex vivo permeation. The CS-SNEDDS formulation was prepared from the optimized SNEDDS by adding oleylamine as the cationic charge inducer and HPMC as the polymeric precipitation inhibitor...
March 27, 2018: Drug Delivery and Translational Research
Julia Carolin Hollerweger, Isabel Josephin Hoppe, Christof Regl, Lorenz Gottfried Stock, Christian G Huber, Urs Lohrig, Hanno Stutz, Hans Brandstetter
Protein function critically depends on structure. However, current analytical tools to monitor consistent higher-order structure with high sensitivity, as for instance required in the development of biopharmaceuticals, are limited. To complement existing assays, we present the analytical cascade of enzymes (ACE), a method based on enzymatic modifications of target proteins, which serve to exponentially amplify structural differences between them. The method enables conformational and chemical fingerprinting of closely related proteins, allowing for the sensitive detection of heterogeneities in protein preparations with high precision...
March 27, 2018: Analytical Chemistry
Eric Lahrsen, Ann-Kathrin Schoenfeld, Susanne Alban
Fucose-containing sulfated glycans (syn. fucoidans) from brown algae exhibit a wide range of bioactivities and are therefore considered promising candidates for health-supporting and medical applications. In this study, we investigated the pharmacological activities of fucoidan from Fucus vesiculosus and 18 gradually depolymerized fractions, which were obtained by hydrothermal and H2 O2 treatment, respectively. All the activities decreased with decreasing molecular mass (Mw ) but to a different extent resulting in some modified pharmacological profiles in dependence on the Mw as well as on the degradation method...
June 1, 2018: Carbohydrate Polymers
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