Read by QxMD icon Read

drug formulation

E Sawicki, J H M Schellens, J H Beijnen, B Nuijen
Dissolution from the pharmaceutical formulation is a prerequisite for complete and consistent absorption of any orally administered drug, including anticancer agents (oncolytics). Poor dissolution of an oncolytic can result in low oral bioavailability, high variability in blood concentrations and with that suboptimal or even failing therapy. This review discusses pharmaceutical formulation aspects and absorption pharmacokinetics of currently licensed orally administered oncolytics. In nearly half of orally dosed oncolytics poor dissolution is likely to play a major role in low and unpredictable absorption...
September 20, 2016: Cancer Treatment Reviews
Ingo Hoffmann, Miriam Simon, Anja Hörmann, Thorsten Gravert, Peggy Heunemann, Sarah E Rogers, Michael Gradzielski
Nanoemulsions are metastable emulsions with droplet sizes between 20 and 100 nm with a wide range of applications e.g. in polymerization, in pharmaceutical and cos- metic formulations and as drug delivery systems. Even though they are not in ther- modynamic equilibrium, they can be metastable over relatively long times and have the advantage that they can be formed easily by low energy input methods. In par- ticular, the phase inversion concentration method (PIC) allows to form nanoemulsions simply by diluting a suitable mixture of oil and surfactants with water...
October 24, 2016: Langmuir: the ACS Journal of Surfaces and Colloids
Xia Song, Yuting Wen, Jing-Ling Zhu, Feng Zhao, Zhongxing Zhang, Jun Li
Paclitaxel (PTX), a hydrophobic anticancer drug, is facing several clinical limitations such as low bioavailability and drug resistance. To solve the problems, a well-defined b-cyclodextrin-poly(N-isopropylacrylamide) star polymer was synthesized and used as a nanocarrier to improve the water solubility and aim to thermoresponsive delivery of PTX to cancer cells. The star polymer was able to form supramolecular self-assembled inclusion complex with PTX via host-guest interaction at room temperature, which is below the low critical solution temperature (LCST) of the star polymer, significantly improving the solubilization of PTX...
October 24, 2016: Biomacromolecules
Yiqiong Pu, Xitong Zhang, Qi Zhang, Bing Wang, Yuxi Chen, Chuanqi Zang, Yuqin Wang, Tina Ting-Xia Dong, Tong Zhang
20(S)-Protopanaxadiol (PPD), a bioactive compound extracted from ginseng, possesses cardioprotective, neuroprotective, anti-inflammatory, antiestrogenic, anticancer and anxiolytic effects. However, the clinical application of PPD is limited by its weak aqueous solubility. In this study, we optimized an efficient method of preparing its phospholipid complex (PPD-PLC) using a central composite design and response surface analysis. The prepared PPD-PLC was characterized by differential scanning calorimetric, powder X-ray diffraction, Fourier-transformed infrared spectroscopy and nuclear magnetic resonance analyses associated with molecular docking calculation...
October 19, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Shuo Wang, Heinz Schattler
We consider cancer chemotherapy as an optimal control problem with the aim to minimize a combination of the tumor volume and side effects over an a priori specified therapy horizon when the tumor consists of a heterogeneous agglomeration of many subpopulations. The mathematical model, which accounts for different growth and apoptosis rates in the presence of cell densities, is a finite-dimensional approximation of a model originally formulated by Lorz et al. [18,19] and Greene et al. [10,11] with a continuum of possible traits...
December 1, 2016: Mathematical Biosciences and Engineering: MBE
Subhash Chandra Bose Penjuri, Saritha Damineni, Nagaraju Ravouru, Srikanth Reddy Poreddy Reddy Poreddy
BACKGROUND: The objective of this investigation was to develop a self emulsifying drug delivery system (SEDDS) of naproxen, a poorly water soluble drug, which could improve its solubility and oral bioavailability. Methoda: The recent patents on SEDDS of abiraterone acetate (WO2014/009434 A1) and tamoxifen (WO2013/0080083) helped in selecting the naproxen and excipients. Phase diagrams were constructed and the formulations were taken from the micro emulsion region. Formulations were subjected to thermodynamic stability, dispersibility and precipitation tests for optimization...
October 19, 2016: Recent Patents on Drug Delivery & Formulation
Md Akhlaquer Rahman, Md Mujahid, Arshad Hussain
AIMS: The purpose of the current study was to investigate the feasibility of producing solid self-emulsifying pellets using the extrusion/spheronization technique with an aim to increase the bioavailability of selected drug and also to encounter the problems associated with liquid lipid formulations. Self-emulsifying formulations are experiencing a very active development as reflected by the numerous publications and patents being granted on these systems. The patents on self-emulsifying formulation (US20036630150) and (US20006054136) helped in selecting the drug and excipients...
October 21, 2016: Recent Patents on Drug Delivery & Formulation
Thao Td Tran, Phuong Hl Tran
Poorly water-soluble drugs, which commonly face the issue of poor absorption and low bioavailability, have been under ongoing research of many formulation scientists for the past few decades. Solid dispersion is one of the most effective strategies in concerns for improving bioavailability of poorly water-soluble drugs. Either application of solid dispersions in dissolution enhancement of poorly water-soluble drugs or the use of swellable polymers in controlled drug release has been reported in pharmaceutical designs widely...
October 21, 2016: Current Pharmaceutical Design
Ekaterina S Dolinina, Elena V Parfenyuk
BACKGROUND: Warfarin, commonly used anticoagulant in clinic, has serious shortcomings due to its unsatisfactory pharmacodynamics. One of efficient ways of improvement of pharmacological and consumer properties of drugs is development of optimal drug delivery systems. OBJECTIVE: The aim of this work is synthesis of novel warfarin - silica composites and study in vitro the drug release kinetics to obtain the composites with controlled release. METHODS: The composites of warfarin with unmodified (UMS) and mercaptopropy modified silica (MPMS) were synthesized by sol-gel method...
October 21, 2016: Current Drug Delivery
Arvin Eskandari, Janine N Boodram, Paul B Cressey, Chunxin Lu, Peter M Bruno, Michael T Hemann, Kogularamanan Suntharalingam
We report the cancer stem cell (CSC) potency of a novel series of copper(ii)-phenanthroline complexes bearing nonsteriodial anti-inflammatory drugs: naproxen, tolfenamic acid, and indomethacin (2a-3c). Two of the complexes, 2a and 3c, kill breast CSC-enriched HMLER-shEcad cells (grown in both monolayer and three-dimensional cell cultures) to a significantly better extent than salinomycin, a well-established CSC toxin. The most potent complex in the series, 3c induces its cytotoxic effect by generating intracellular reactive oxygen species (ROS) and inhibiting cyclooxgenase-2 (COX-2) activity...
October 24, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Madhavi G Patel, Kilambi Pundarikakshudu
In India, Vatari Guggulu has been traditionally used in the Ayurvedic system of medicine to treat rheumatoid arthritis (RA). The current study was undertaken to evaluate anti-arthritic activity of alcoholic extract of Vatari Guggulu in rats. Arthritis was induced by administration of formaldehyde (2%v/v) or Complete Freund's Adjuvant (CFA) into the sub-plantar surface of left hind paw of the animals. The extract was administered to the rats by oral gavages in different doses. Joint swelling was measured in formaldehyde induced arthritis...
October 2016: Journal of Traditional and Complementary Medicine
Jeong Yeon Kang, Jieming Gao, Dae Hwan Shin, Celeste Alvarez, Weixiong Zhong, Glen S Kwon
BACKGROUND: Delivery of monomeric Amphotericin B (AmB), i.e. deaggregated AmB, has been a major tactic in the reduction of renal toxicity at a membrane level, taking advantage of the selectivity of monomeric AmB for binding ergosterol over cholesterol. OBJECTIVE: The aim of this study was to characterize the pharmacokinetic (PK) and renal toxicity of monomeric AmB in rats following a multiple dose regimen. METHOD: AmB existed primarily in a monomeric state in poly(ethylene glycol)-block-poly(N-hexyl stearate L-aspartamide) (PEG-b-PHSA) micelles (mAmB) at 2:1 ratio (mol:mol), whereas AmB as its standard formulation, Fungizone(®), was highly self-aggregated based on absorption spectroscopy...
2016: Pharm Nanotechnol
Marco Siccardi, Phillip Martin, Darren Smith, Paul Curley, Tom McDonald, Marco Giardiello, Neill Liptrott, Steve Rannard, Andrew Owen
Solid drug nanoparticles (SDNs) are a nanotechnology with favourable characteristics to enhance drug delivery and improve the treatment of several diseases, showing benefit for improved oral bioavailability and injectable long-acting medicines. The physicochemical properties and composition of nanoformulations can influence the absorption, distribution, and elimination of nanoparticles; consequently, the development of nanoparticles for drug delivery should consider the potential role of nanoparticle characteristics in the definition of pharmacokinetics...
September 2016: J Interdiscip Nanomed
Anil K Deshantri, Sander A A Kooijmans, Sylvia A Kuijpers, Maria Coimbra, Astrid Hoeppener, Gert Storm, Marcel H A M Fens, Raymond M Schiffelers
Cancers are abundantly infiltrated by inflammatory cells that are modulated by tumor cells to secrete mediators fostering tumor cell survival and proliferation. Therefore, agents that interfere with inflammatory signaling molecules or specific immune cell populations have been investigated as anticancer drugs. Corticosteroids are highly potent anti-inflammatory drugs, whose activity is intensified when targeted by nanocarrier systems. Liposome-targeted corticosteroids have been shown to inhibit tumor growth in different syngeneic murine tumor models as well as human xenograft mouse models, which is attributed to a switch in the tumor microenvironment from a pro-inflammatory to an anti-inflammatory state...
October 20, 2016: Journal of Controlled Release: Official Journal of the Controlled Release Society
Stefanie Funke, Julia Matilainen, Heiko Nalenz, Karoline Bechtold-Peters, Hanns-Christian Mahler, Wolfgang Friess
A significant number of therapeutic proteins are marketed as pre-filled syringes or other drug/device combination products and have been safely used in these formats for years. Silicone oil, which is used as lubricant, can migrate into the drug product and may interact with therapeutic proteins. In this study, particles in the size range of 0.2-5 μm and ≥1 μm as determined by resonant mass measurement and micro-flow imaging/light obscuration, respectively, resulted from silicone sloughing off the container barrel after agitation...
October 20, 2016: Journal of Pharmaceutical Sciences
Graciliana Lopes, Eugénia Pinto, Lígia Salgueiro
The increased incidence of fungal infections, associated with the widespread use of antifungal drugs, has resulted in the development of resistance, making it necessary to discover new therapeutic alternatives. Among fungal infections, dermatophytoses constitute a serious public health problem, affecting 20-25 % of the world population. Medicinal plants represent an endless source of bioactive molecules, and their volatile and non-volatile extracts are clearly recognized for being the historical basis of therapeutic health care...
October 22, 2016: Mycopathologia
Ira Shah
No abstract text is available yet for this article.
October 8, 2016: Indian Pediatrics
Preeti Pandey, Peter J Cabot, Benjamin Wallwork, Benedict J Panizza, Harendra S Parekh
Mucoadhesive in situ gelling systems (soluble gels) have received considerable attention recently as effective stimuli-transforming vectors for a range of drug delivery applications. Considering this fact, the present work involves systematic formulation development, optimization, functional evaluation and ex vivo performance of thermosensitive soluble gels containing dexamethasone 21-phosphate disodium salt (DXN) as the model therapeutic. A series of in situ gel-forming systems comprising the thermoreversible polymer poloxamer-407 (P407), along with hydroxypropyl methyl cellulose (HPMC) and chitosan were first formulated...
October 19, 2016: European Journal of Pharmaceutical Sciences
Rahul B Chavan, Rajesh Thipparaboina, Dinesh Kumar, Nalini R Shastri
Solubility is one of the major problems associated with most of the new chemical entities that can be reasonably addressed by drug amorphization. However, being a high-energy form, it usually tends to re-crystallize, necessitating new formulation strategies to stabilize amorphous drugs. Polymeric amorphous solid dispersion (PASD) is one of the widely investigated strategies to stabilize amorphous drug, with major limitations like limited polymer solubility and hygroscopicity. Co amorphous system (CAM), a new entrant in amorphous arena is a promising alternative to PASD...
October 19, 2016: International Journal of Pharmaceutics
Ameya R Kirtane, Robert Langer, Giovanni Traverso
The human immunodeficiency virus has infected millions of people and the epidemic continues to grow rapidly in some parts of the world. Antiretroviral (ARV) therapy has provided improved treatment and prolonged the life expectancy of patients. Moreover, there is growing interest in using ARVs to protect against new infections. Hence, ARVs have emerged as our primary strategy in combating the virus. Unfortunately, several challenges limit the optimal performance of these drugs. First, ARVs often require life-long use and complex dosing regimens...
October 19, 2016: Journal of Pharmaceutical Sciences
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"