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https://www.readbyqxmd.com/read/28642346/detergent-induced-self-assembly-and-controllable-photosensitizer-activity-of-diester-phenylene-ethynylenes
#1
Patrick L Donabedian, Matthew N Creyer, Florencia A Monge, Kirk S Schanze, Eva Y Chi, David G Whitten
Photodynamic therapy, in which malignant tissue is killed by targeted light exposure following administration of a photosensitizer, can be a valuable treatment modality but currently relies on passive transport and local irradiation to avoid off-target oxidation. We present a system of excited-state control for truly local delivery of singlet oxygen. An anionic phenylene ethynylene oligomer is initially quenched by water, producing minimal fluorescence and no measurable singlet oxygen generation. When presented with a binding partner, in this case an oppositely charged surfactant, changes in solvent microenvironment result in fluorescence unquenching, restoration of intersystem crossing to the triplet state, and singlet oxygen generation, as assayed by transient absorption spectroscopy and chemical trapping...
June 22, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28633547/lipid-based-nanosystem-of-edaravone-development-optimization-characterization-and-in-vitro-in-vivo-evaluation
#2
Ankit Parikh, Krishna Kathawala, Chun Chuan Tan, Sanjay Garg, Xin-Fu Zhou
Edaravone (EDR) is a well-recognized lipophilic free radical scavenger for diseases including neurodegenerative disease, cardiovascular disease, and cancer. However, its oral use is restricted due to poor oral bioavailability (BA). The aim of present research was to enable its oral use by developing a lipid-based nanosystem (LNS). The components of LNS including oil, surfactants, and co-surfactants were selected based on their potential to maximize the solubilization in gastrointestinal (GI) fluids, reduce its glucuronidation and improve transmembrane permeability...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28628923/cremophor-el-alters-the-plasma-protein-binding-and-pharmacokinetic-profile-of-valspodar-in-rats
#3
Ziyad Binkhathlan
Cremophor EL is a nonionic surfactant widely used in pharmaceutical formulations. Nonetheless, there are several reports on the influence of this excipient on the protein binding, pharmacokinetics, and pharmacodynamics of drugs. Valspodar is an investigational non-immunosuppressive derivative of cyclosporine A, used in clinical trials for treatment of multidrug resistant tumors. The formulation of valspodar (Amdray(®)) contains cremophor EL and ethanol as solubilizing agents. The main aim of the current study was to assess the plasma protein binding (in vitro) and the pharmacokinetic profile of valspodar in the cremophor EL-based formulation in comparison to a cremophor EL-free formulation following intravenous (i...
June 19, 2017: Drug Research
https://www.readbyqxmd.com/read/28569744/delivery-room-interventions-to-prevent-bronchopulmonary-dysplasia-in-extremely-preterm-infants
#4
E E Foglia, E A Jensen, H Kirpalani
Bronchopulmonary dysplasia (BPD) is the most common chronic respiratory complication of preterm birth. Preterm infants are at risk for acute lung injury immediately after birth, which predisposes to BPD. In this article, we review the current evidence for interventions applied during neonatal transition (delivery room and first postnatal hours of life) to prevent BPD in extremely preterm infants: continuous positive airway pressure (CPAP), sustained lung inflation, supplemental oxygen use during neonatal resuscitation, and surfactant therapy including less-invasive surfactant administration...
June 1, 2017: Journal of Perinatology: Official Journal of the California Perinatal Association
https://www.readbyqxmd.com/read/28569515/self-emulsifying-drug-delivery-system-sedds-of-ibuprofen-formulation-in-vitro-and-in-vivo-evaluation
#5
Subhash Chandra Bose Penjuri, Saritha Damineni, Nagaraju Ravouru, Srikanth Reddy Poreddy
The goal of the present study was to develop a self-emulsifying drug delivery system for the oral poorly water-soluble drug ibuprofen and to evaluate its oral bioavailability. Phase diagrams were constructed to determine the phase behaviour of the microemulsions and to compare the efficiency of various surfactant-oil mixtures. The SEDDS formulations of ibuprofen were prepared from a mixture of Labrafil M2125, Cremophor RH40, and Plurol oleique. The prepared emulsions were characterized for in vitro and in vivo behaviour...
2017: Ceská a Slovenská Farmacie
https://www.readbyqxmd.com/read/28557649/sustained-release-docetaxel-incorporated-lipid-nanoparticles-with-improved-pharmacokinetics-for-oral-and-parenteral-administration
#6
Omer Salman Qureshi, Hyung-Seo Kim, Alam Zeb, Jin-Seok Choi, Hoo-Seong Kim, Jung-Eun Kwon, Myung-Sic Kim, Jong-Ho Kang, Chongsuk Ryou, Jeong-Sook Park, Jin-Ki Kim
The aim of this study was to develop docetaxel-incorporated lipid nanoparticles (DTX-NPs) to improve the pharmacokinetic behaviour of docetaxel (DTX) after oral and parenteral administration via sustained release. DTX-NPs were prepared by nanotemplate engineering technique with palmityl alcohol as a solid lipid and Tween-40/Span-40/Myrj S40 as a surfactants mixture. Spherical DTX-NPs below 100 nm were successfully prepared with a narrow particle size distribution, 96% of incorporation efficiency and 686 times increase in DTX solubility...
June 15, 2017: Journal of Microencapsulation
https://www.readbyqxmd.com/read/28553114/ravuconazole-self-emulsifying-delivery-system-in-vitro-activity-against-trypanosoma-cruzi-amastigotes-and-in-vivo-toxicity
#7
Pollyanna Álvaro Spósito, Ana Lia Mazzeti, Caroline de Oliveira Faria, Julio A Urbina, Gwenaelle Pound-Lana, Maria Terezinha Bahia, Vanessa Furtado Mosqueira
Self-emulsifying drug delivery systems (SEDDSs) are lipid-based anhydrous formulations composed of an isotropic mixture of oil, surfactant, and cosurfactants usually presented in gelatin capsules. Ravuconazole (Biopharmaceutics Classification System [BCS] Class II) is a poorly water-soluble drug, and a SEDDS type IIIA was designed to deliver it in a predissolved state, improving dissolution in gastrointestinal fluids. After emulsification, the droplets had mean hydrodynamic diameters <250 nm, zeta potential values in the range of -45 mV to -57 mV, and showed no signs of ravuconazole precipitation...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28543309/adenovirus-vector-expressing-keratinocyte-growth-factor-using-cag-promoter-impaired-pulmonary-function-of-elastase-induced-emphysema
#8
Hiroshi Oki, Takuya Yazawa, Yasuko Baba, Yumi Kanegae, Hanako Sato, Seiko Sakamoto, Takahisa Goto, Izumu Saito, Kiyoyasu Kurahashi
Pulmonary emphysema impairs quality of life and increases mortality. Previous studies demonstrated that administration of KGF before elastase instillation prevented pulmonary emphysema in mice. We hypothesized that KGF could improve pulmonary function, and that the therapeutic administration of KGF would restore damaged lungs caused by elastase instillation in an animal model. We constructed KGF expressing adenovirus vector, which prevented bleomycin induced pulmonary fibrosis in the previous study. Adenovirus vector (1...
May 24, 2017: Microbiology and Immunology
https://www.readbyqxmd.com/read/28540346/less-invasive-surfactant-administration-reduces-the-need-for-mechanical-ventilation-in-preterm-infants-a-meta-analysis
#9
Christine S M Lau, Ronald S Chamberlain, Shyan Sun
Neonatal respiratory distress syndrome due to surfactant deficiency is associated with high morbidity and mortality in preterm infants, and the use of less invasive surfactant administration (LISA) has been increasingly studied. This meta-analysis found that LISA via thin catheter significantly reduced the need for mechanical ventilation within the first 72 hours (relative risk [RR] = 0.677; P = .021), duration of mechanical ventilation (difference in means [MD] = -39.302 hours; P < .001), duration of supplemental oxygen (MD = -68...
2017: Global Pediatric Health
https://www.readbyqxmd.com/read/28538236/surfactant-for-respiratory-distress-syndrome-new-ideas-on-a-familiar-drug-with-innovative-applications
#10
H J Niemarkt, M C Hütten, Boris W Kramer
In the last 4 decades, advances in neonatology have led to a significant increase in the survival of preterm infants. One of the biggest advances was the introduction of surfactant replacement therapy for the treatment of respiratory distress syndrome. This is the main cause of respiratory insufficiency in preterm infants and is one of the major causes of perinatal morbidity and mortality. Surfactant replacement therapy is already a well-investigated and established therapy in neonatology. However, surfactant replacement therapy has progressed and been refined over recent decades, especially with the increasing care for preterm infants born before 26 weeks' gestational age and the recent clinical focus on avoiding mechanical ventilation...
2017: Neonatology
https://www.readbyqxmd.com/read/28536023/development-of-long-circulating-docetaxel-loaded-poly-3-hydroxybutyrate-co-3-hydroxyvalerate-nanoparticles-optimization-pharmacokinetic-cytotoxicity-and-in-vivo-assessments
#11
Harsh Vardhan, Pooja Mittal, Sandeep K Reddy Adena, Mansi Upadhyay, Brahmeshwar Mishra
Long-circulating nanoparticles (NPs) are promising drug delivery vehicles which target solid tumors via enhanced permeation and retention effect. Plackett-Burman (PBD) and Box-Behnken (BBD) designs were adopted to study the effects of factors viz. polymer concentration, surfactant concentration, homogenizer speed, homogenization time and ultrasonication time on responses. A graphical and numerical optimization technique was used to obtain predicted value of the response. The drug entrapment efficiency was approximately 39±0...
May 20, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28510235/surfactants-in-acute-respiratory-distress-syndrome-in-infants-and-children-past-present-and-future
#12
REVIEW
Angela Amigoni, Andrea Pettenazzo, Valentina Stritoni, Maria Circelli
There is a lack of definitive data on the effective management of acute respiratory distress syndrome (ARDS) in infants and children. The development and validation of the Berlin definition (BD) for ARDS and the Pediatric Acute Lung Injury Consensus Conference (PALICC) recommendations in children represented a major advance in optimizing research and treatment, mainly due to the introduction of a severe ARDS category. Proposed reasons for the lack of consistent results with surfactants in children and infants compared with neonates include different causes, type of lung damage (direct or indirect), timing and mode of administration as well as the type of surfactant used...
May 16, 2017: Clinical Drug Investigation
https://www.readbyqxmd.com/read/28499879/developing-a-flexible-pediatric-dosage-form-for-antiretroviral-therapy-a-fast-dissolving-tablet
#13
Manjari Lal, Manshun Lai, Marcus Estrada, Changcheng Zhu
Current presentations of the anti-HIV drugs lopinavir and ritonavir make appropriate dosing for children difficult. We conducted a feasibility study to develop a formulation for these drugs with child-safe excipients in a flexible dosage form for children across the pediatric age spectrum. The freeze-drying in blister approach was used to produce fast-dissolving tablets (FDTs), as these can be dispersed in fluids for easy administration, even to infants, and appropriate portions of the dispersion can be given for different ages/weights...
May 10, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28495500/microemulsion-utility-in-pharmaceuticals-implications-for-multi-drug-delivery
#14
REVIEW
Shannon P Callender, Jessica A Mathews, Katherine Kobernyk, Shawn D Wettig
Emulsion technology has been utilized extensively in the pharmaceutical industry. This article presents a comprehensive review of the literature on an important subcategory of emulsions, microemulsions. Microemulsions are optically transparent, thermodynamically stable colloidal systems, 10-100nm diameter, that form spontaneously upon mixing of oil, water and emulsifier. This review is the first to address advantages and disadvantages, as well as considerations and challenges in multi-drug delivery. For the period 1 January 2011-30 April 2016, 431 publications related to microemulsion drug delivery were identified and screened according to microemulsion, drug classification, and surfactant types...
May 7, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28480758/loratadine-bioavailability-via-buccal-transferosomal-gel-formulation-statistical-optimization-in-vitro-in-vivo-characterization-and-pharmacokinetics-in-human-volunteers
#15
Mohammed H Elkomy, Shahira F El Menshawe, Heba A Abou-Taleb, Marwa H Elkarmalawy
Loratadine (LTD) is an antihistaminic drug that suffers limited solubility, poor oral bioavailability (owing to extensive first-pass metabolism), and highly variable oral absorption. This study was undertaken to develop and statistically optimize transfersomal gel for transbuccal delivery of LTD. Transfersomes bearing LTD were prepared by conventional thin film hydration method and optimized using sequential Quality-by-Design approach that involved Placket-Burman design for screening followed by constrained simplex-centroid design for optimization of a Tween-80/Span-60/Span-80 mixture...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28472058/poractant-alfa-versus-bovine-lipid-extract-surfactant-for-infants-24-0-to-31-6-weeks-gestational-age-a-randomized-controlled-trial
#16
Brigitte Lemyre, Christoph Fusch, Georg M Schmölzer, Nicole Rouvinez Bouali, Deepti Reddy, Nicholas Barrowman, Nicole Huneault-Purney, Thierry Lacaze-Masmonteil
OBJECTIVES: To compare the efficacy and safety of poractant alfa and bovine lipid extract surfactant in preterm infants. STUDY DESIGN: Randomized, partially-blinded, multicenter trial. Infants <32 weeks needing surfactant before 48 hours were randomly assigned to receive poractant alfa or bovine lipid extract surfactant. The primary outcome was being alive and extubated at 48 hours post-randomization. Secondary outcomes included need for re-dosing, duration of respiratory support and oxygen, bronchopulmonary dysplasia, mortality and complications during administration...
2017: PloS One
https://www.readbyqxmd.com/read/28456852/fluid-induced-lung-injury-role-of-trpv4-channels
#17
Shailesh Bihari, Dani-Louise Dixon, Mark D Lawrence, Dylan De Bellis, Claudine S Bonder, David P Dimasi, Andrew D Bersten
Administration of bolus intravenous fluid is associated with respiratory dysfunction and increased mortality, findings with no clear mechanistic explanation. The objective of this study was to examine whether bolus intravenous (i.v.) fluid administration results in acute lung injury in a rat model and further, to examine whether this injury is associated with transient receptor potential vallinoid (TRPV)4 channel function and endothelial inflammatory response. Healthy male Sprague-Dawley rats were administered 60 ml/kg 0...
April 29, 2017: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28443559/the-evolution-of-modern-respiratory-care-for-preterm-infants
#18
REVIEW
Louise S Owen, Brett J Manley, Peter G Davis, Lex W Doyle
Preterm birth rates are rising, and many preterm infants have breathing difficulty after birth. Treatments for infants with prolonged breathing difficulty include oxygen therapy, exogenous surfactant, various modes of respiratory support, and postnatal corticosteroids. In this Series paper, we review the history of neonatal respiratory care and its effect on long-term outcomes, and we outline the future direction of the research field. The delivery and monitoring of oxygen therapy remains controversial, despite being in use for more than 50 years...
April 22, 2017: Lancet
https://www.readbyqxmd.com/read/28438206/exogenous-gene-transfer-of-rab-3-8-small-gtpase-ameliorates-aberrant-lung-surfactant-homeostasis-in-ruby-rats
#19
Kazuhiro Osanai, Keisuke Nakase, Takashi Sakuma, Kazuaki Nishiki, Masafumi Nojiri, Ryo Kato, Masatoshi Saito, Yuki Fujimoto, Shiro Mizuno, Hirohisa Toga
BACKGROUND: Rab(3)8 small GTPase regulates intracellular transport in melanocytes and alveolar type II epithelial cells. Ruby rats carrying Rab(3)8 and other gene mutations exhibit oculocutaneous albinism, bleeding diathesis, and hence, are a rat model of human Hermansky-Pudlak syndrome (HPS). We previously showed that Long Evans Cinnamon (LEC) rats, one strain of the Ruby rats, developed aberrant lung surfactant homeostasis with remarkably enlarged lamellar bodies in alveolar type II cells...
April 24, 2017: Respiratory Research
https://www.readbyqxmd.com/read/28435650/postnatal-transitional-weight-loss-and-adverse-outcomes-in-extremely-premature-neonates
#20
Rita P Verma, Syed Shibli, Eugene Komaroff
The early postnatal weight loss (EPWL) is highly variable in the extremely low birth weight infants (birth weight <1000 g, ELBW). It is reported to be unassociated with adverse outcomes within a range of 3-21% of birth weight. Its wide range might have contributed to this lack of association. The aim of our paper is to study the effects of maximum EPWL, graded as low, medium and large on clinical outcomes in ELBW infants. In a retrospective cohort observational study EPWL was measured as maximum weight loss from birth weight (MWL) in ELBW infants and grouped as low (5-12%) moderate (18...
March 22, 2017: Pediatric Reports
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