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https://www.readbyqxmd.com/read/28449309/tumor-targeting-with-an-isodgr-drug-conjugate
#1
Simone Zanella, Simona Angerani, Pina Arianna, Paula López Rivas, Clelia Giannini, Silvia Panzeri, Daniela Arosio, Michele Caruso, Fabio Gasparri, Ivan Fraietta, Clara Albanese, Aurelio Marsiglio, Luca Pignataro, Laura Belvisi, Umberto Piarulli, Cesare Gennari
Here we report the first example of an isoDGR-drug conjugate (2), designed to release paclitaxel selectively within cancer cells expressing integrin αVβ3. Conjugate 2 was synthesized by connecting the isoDGR peptidomimetic 5 with paclitaxel via the lysosomally cleavable Val-Ala dipeptide linker. Conjugate 2 displayed a low nanomolar affinity for the purified integrin αVβ3 receptor (IC50 = 11.0 nM). The tumor targeting ability of conjugate 2 was assessed in vitro in anti-proliferative assays on two isogenic cancer cell lines characterized by different integrin αVβ3 expression: human glioblastoma U87 (αVβ3 +) and U87 β3-KO (αVβ3 -)...
April 27, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28449218/development-and-pharmacologic-characterization-of-the-rat-6-hz-model-of-partial-seizures
#2
Cameron S Metcalf, Peter J West, Kyle E Thomson, Sharon F Edwards, Misty D Smith, H S White, Karen S Wilcox
OBJECTIVE: The mouse 6 Hz model of psychomotor seizures is a well-established and commonly used preclinical model for antiseizure drug (ASD) discovery. Despite its widespread use both in the identification and differentiation of novel ASDs in mice, a corresponding assay in rats has not been developed. We established a method for 6 Hz seizure induction in rats, with seizure behaviors similar to those observed in mice including head nod, jaw clonus, and forelimb clonus. METHODS: A convulsive current that elicits these seizure behaviors in 97% of rats (CC97 ) was determined using a Probit analysis...
April 27, 2017: Epilepsia
https://www.readbyqxmd.com/read/28449198/systematic-review-of-sex-work-interventions-in-sub-saharan-africa-examining-combination-prevention-approaches
#3
George Awungafac, Therese Delvaux, Bea Vuylsteke
OBJECTIVE: The incidence of HIV and sexually transmitted infections is disproportionately high among sex workers (SW). We aimed to update the evidence on the effectiveness of SW interventions in sub-Saharan Africa and to provide more insights into combination prevention. METHODS: Systematic review following PRISMA guidelines in a search of PUBMED and POPLINE for peer-reviewed literature published between January 1, 2000 and July 22, 2016 (registration number on PROSPERO: CRD42016042529)...
April 27, 2017: Tropical Medicine & International Health: TM & IH
https://www.readbyqxmd.com/read/28448900/dual-responsive-magnetic-composite-nanogels-for-thermo-chemotherapy
#4
S Indulekha, P Arunkumar, D Bahadur, R Srivastava
With the onset of hyperthermia and their advantage in increasing vascular perfusion and permeability in the cancer milieu, thermo-responsive polymers have become an attractive candidate for designing therapeutic nano-vehicles for targeted on-demand delivery of bioactive agents. For this purpose, we developed a dual (thermo- and pH-) responsive nanotherapeutic composite system rendering a combinational therapy of hyperthermia mediated drug delivery. This composite system comprises of magnetic chitosan-g-PNVCL (MCP) polymeric nanogels loaded with anticancer drug, Doxorubicin (DOX)...
April 19, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28448868/protective-effects-of-teucrium-polium-aqueous-extract-and-ascorbic-acid-on-hematological-and-some-biochemical-parameters-against-carbon-tetrachloride-ccl4-induced-toxicity-in-rats
#5
Fatma Rahmouni, Latifa Hamdaoui, Riadh Badraoui, Tarek Rebai
Herbal drugs play a crucial function to protect organisms from the toxic effect of some compounds. The present study was designed to evaluate the protective effects of Teucrium Polium (TP) aqueous extract and vitamin C (Vit C) against carbon tetrachloride (CCl4) which induced toxicity in rats. Male albino Wistar rats were divided into six groups: group I was used as controls, group II received CCl4 in olive oil (0.5ml/kg) by gavage, and group III received CCl4 in olive oil (0.5ml/kg) by gavage after three days of receiving TP (5g/l), orally, for seven days; Group IV received TP (5g/l) alone, orally, for seven days, Group V received CCl4 in olive oil (0...
April 24, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28448783/effectiveness-of-a-clinical-pharmacist-medication-therapy-management-program-in-discontinuation-of-drugs-to-avoid-in-the-elderly
#6
Nicole Caffiero, Thomas Delate, Mercy D Ehizuelen, Kris Vogel
BACKGROUND: Despite evidence of fall risk associated with some drugs to avoid in the elderly (DAEs), many aged patients continue to receive them. OBJECTIVE: To assess the effectiveness of a clinical pharmacist medication therapy management program (MTM) on discontinuation of prescribed DAEs. METHODS: This was a retrospective cohort study conducted at an integrated health care delivery system. Kaiser Permanente Colorado beneficiaries aged ≥65 years who were MTM-eligible and targeted for a DAE dispensing between 01/01/2015 and 09/30/2015 were included in the observation group...
May 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28448781/assessment-of-clinical-pharmacy-interventions-to-reduce-outpatient-use-of-high-risk-medications-in-the-elderly
#7
Sarah C Weddle, A Shaun Rowe, Julie W Jeter, Rachel C Renwick, Shaunta' M Chamberlin, Andrea S Franks
BACKGROUND: Use of high-risk medications in the elderly (HRME) and drug-disease (Rx-DIS) interactions in the elderly, as defined by the Healthcare Effectiveness Data and Information Set (HEDIS) Measures, are significantly associated with mortality, hospital admission, and need for emergency care. No published studies to date evaluate interventions to reduce the use of HEDIS-defined HRME, although many studies have postulated a beneficial effect of such interventions. OBJECTIVE: To evaluate the effect of pharmacist interventions on use of HRME and Rx-DIS interactions in the outpatient elderly population...
May 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28448780/integration-strategies-of-pharmacists-in-primary-care-based-accountable-care-organizations-a-report-from-the-accountable-care-organization-research-network-services-and-education
#8
Tina Joseph, Genevieve M Hale, Sara M Eltaki, Yesenia Prados, Renee Jones, Matthew J Seamon, Cynthia Moreau, Stephanie A Gernant
BACKGROUND: The accountable care organization (ACO) is an innovative health care delivery model centered on value-based care. ACOs consisting of primary care providers are increasingly becoming commonplace in practice; however, medication management remains suboptimal. PROGRAM DESCRIPTION: As experts in medication management, pharmacists perform direct patient care and assist in the transition from one provider to another, which places them in an ideal position to manage multiple aspects of patient care...
May 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28448772/the-effect-of-a-federal-controlled-substance-act-schedule-change-on-hydrocodone-combination-products-claims-in-a-medicaid-population
#9
Stephanie Tran, Pavel Lavitas, Karen Stevens, Bonnie C Greenwood, Karen Clements, Caroline J Alper, Kimberly Lenz, Mylissa Price, Tasmina Hydery, Jennifer L Arnold, Mito Takeshita, Rachel Bacon, Justin P Peristere, Paul L Jeffrey
BACKGROUND: In 2012, hydrocodone combination products (HCPs) were the most prescribed medications in the United States. Under the Controlled Substance Act of 1970, hydrocodone alone was classified as a Schedule II drug, while HCPs were classified as Schedule III, indicating a lower risk for abuse and misuse. However, according to a Drug Enforcement Agency analysis, the addition of nonopioids has not been shown to diminish abuse potential of hydrocodone. In response to concerns for drug abuse and overdose, the Drug Enforcement Agency rescheduled HCPs to Schedule II in October 2014, with the intent of limiting overprescribing and increasing awareness of their abuse potential...
May 2017: Journal of Managed Care & Specialty Pharmacy
https://www.readbyqxmd.com/read/28448684/statistical-modeling-for-bayesian-extrapolation-of-adult-clinical-trial-information-in-pediatric-drug-evaluation
#10
Margaret Gamalo-Siebers, Jasmina Savic, Cynthia Basu, Xin Zhao, Mathangi Gopalakrishnan, Aijun Gao, Guochen Song, Simin Baygani, Laura Thompson, H Amy Xia, Karen Price, Ram Tiwari, Bradley P Carlin
Children represent a large underserved population of "therapeutic orphans," as an estimated 80% of children are treated off-label. However, pediatric drug development often faces substantial challenges, including economic, logistical, technical, and ethical barriers, among others. Among many efforts trying to remove these barriers, increased recent attention has been paid to extrapolation; that is, the leveraging of available data from adults or older age groups to draw conclusions for the pediatric population...
April 27, 2017: Pharmaceutical Statistics
https://www.readbyqxmd.com/read/28448574/fusion-expression-of-occludin-extracellular-loops-and-an-%C3%AE-helical-bundle-a-new-research-model-for-tight-junction
#11
Xiaojing Chi, Xia Zhao, Wei Wang, Yuqiang Niu, Min Cheng, Xiuying Liu, Sheng Cui, Wei Yang
Tight junctions (TJs) are the outermost structures of intercellular junctions and are highly specialized membrane domains involved in many important cellular processes. However, most TJ proteins are four-time transmembrane proteins and are difficult to express in their correct soluble form, which limits their functional study and therapeutic application. Human occludin (OCLN) is a major component of TJs and an essential co-receptor for hepatitis C virus (HCV) cell entry. To explore expression strategy for recombinant TJ proteins possessing integrated and functional extracellular loops, OCLN was here used as a model molecule, and several prokaryotic fusion constructs were designed by docking OCLN extracellular loops (ECLs) to HIV-1 gp41 NHR and CHR six-helical bundle (6HV1); then their biophysical features and anti-HCV activity were evaluated...
2017: PloS One
https://www.readbyqxmd.com/read/28448491/relevant-units-of-analysis-for-applied-and-basic-research-dealing-with-neglected-transmissible-diseases-the-predominant-clonal-evolution-model-of-pathogenic-microorganisms
#12
REVIEW
Michel Tibayrenc, Francisco J Ayala
The predominant clonal evolution (PCE) model seeks to formulate a common population genetics framework for all micropathogens (namely, parasitic protozoa, fungi and yeasts, bacteria, and viruses). It relies on a definition of clonality that is only based on population structure features (namely, strongly restrained genetic recombination). Its clear-cut properties make it of strong interest for applied and basic research, since it permits the definition of stable, clearly delimited units of analysis below the species level: clonal genotypes and discrete genetic subdivisions ("near-clades")...
April 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28448477/evaluation-of-gelatin-tannate-against-symptoms-of-acute-diarrhea-in-pediatric-patients
#13
Eren Çağan, Saime Ceylan, Şenay Mengi, Havva Hasret Çağan
BACKGROUND Acute diarrhea is the second most common cause of morbidity and mortality worldwide, especially in children aged ≤3 years. Some drugs (e.g., the mucoprotector gelatin tannate) plus a reduced osmolality oral rehydration solution (ORS) may effectively reduce symptom duration and severity. The current trial was therefore designed to assess the efficacy and safety of gelatin tannate in pediatric patients with acute diarrhea. MATERIAL AND METHODS This was a randomized, controlled, double-blind, parallel-group, single-center study comparing gelatin tannate plus ORS (103 patients) with ORS plus placebo (100 patients) in children aged 3 months to 12 years with infectious or noninfectious acute diarrhea...
April 27, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28448195/design-characteristics-of-the-corrona-japan-rheumatoid-arthritis-registry
#14
Hisashi Yamanaka, Mitsumasa Kishimoto, Dimitrios A Pappas, Jeffrey D Greenberg, Joel M Kremer, Yoshiya Tanaka
OBJECTIVES: The primary objective is to prospectively study the comparative safety and effectiveness of older and newer classes of nonbiologic DMARDs (Disease-modifying antirheumatic drugs), biologic DMARDs and targeted synthetic therapies approved for rheumatoid arthritis (RA) in a real-world patient population in Japan. METHODS: Prospective, multicenter, noninterventional, observational study across geographic distribution of both private and public institutions for patients with RA who are newly prescribed one of the following medications: (1) methotrexate; (2) anti-TNF biologic DMARDs; (3) non-TNF biologic DMARDs; and (4) approved JAK inhibitors at the time of enrollment into the registry...
April 27, 2017: Modern Rheumatology
https://www.readbyqxmd.com/read/28448185/addition-of-spironolactone-in-patients-with-resistant-hypertension-a-meta-analysis-of-randomized-controlled-trials
#15
Liping Liu, Bing Xu, Yunfeng Ju
This study was designed to assess the effect of additional spironolactone on blood pressure in patients with resistant hypertension. MEDLINE, EMBASE, and Cochrane Library were searched to identify randomized controlled trials (RCTs) that determined the effect of add-on spironolactone on blood pressure in patients with resistant hypertension compared with a control group. A total of five RCTs met the inclusion criteria. Spironolactone reduced office systolic blood pressure (SBP) by 15.73 mmHg (95% CI -20.45 to -11...
2017: Clinical and Experimental Hypertension: CHE
https://www.readbyqxmd.com/read/28447980/disposable-dosators-for-pulmonary-insufflation-of-therapeutic-agents-to-small-animals
#16
Phillip G Durham, Shumaila N Hanif, Lucia Garcia Contreras, Ellen F Young, Miriam S Braunstein, Anthony J Hickey
Development of new therapeutic products requires efficacy testing in an animal model. The pulmonary route of administration can be utilized to deliver drugs locally and systemically. Evaluation of dry powder aerosols necessitates an efficient dispersion mechanism to maintain high concentrations in an exposure chamber or for direct endotracheal administration. While solutions exist to expose animals by passive inhalation to dry powder aerosols, most require masses of powder in large excess of the dose delivered...
March 30, 2017: Journal of Visualized Experiments: JoVE
https://www.readbyqxmd.com/read/28447892/intracellular-localization-of-proteins-to-specific-cellular-areas-by-nanocapsule-mediated-delivery
#17
Huabin Wang, Ligang Chen, Xianchao Sun, Ailing Fu
Nanocapsules are promising carriers with great potential for intracellular protein transport. Although many studies have intended to improve cell uptake efficacy, there is an increasing interest in understanding of subcellular distribution of cargoes inside cells, which is essential for purposeful delivery of biomolecules into specific sites within cells. Herein, we interrogate the intracellular localization of exogenous proteins, including fluorescein isothiocyanate (FITC)-labeled bovine serum albumin (BSA) and green fluorescent protein (GFP), mediated by specially designed nanocapsules...
April 27, 2017: Journal of Drug Targeting
https://www.readbyqxmd.com/read/28447799/enhanced-transdermal-delivery-by-combined-application-of-dissolving-microneedle-patch-on-serum-treated-skin
#18
Suyong Kim, Manita Dangol, Geonwoo Kang, Shayan F Lahiji, Huisuk Yang, Mingyu Jang, Yonghao Ma, Chengguo Li, Sang Gon Lee, Chang Hyun Kim, Young Wook Choi, So Jeong Kim, Ja Hyun Ryu, Ji Hwoon Baek, Jaesuk Koh, Hyungil Jung
Dissolving microneedle (DMN), a transdermal drug delivery system in which drugs are encapsulated in a biodegradable polymeric micro-structure, is designed to dissolve after skin penetration and release the encapsulated drugs into the body. However, due to limited loading capacity of drugs within micro-sized structures, only small dosage can be delivered which are often insufficient for patients. We propose a novel DMN application that combines topical and DMN application simultaneously to improve skin permeation efficiency...
April 27, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28447766/supervised-dosing-with-a-long-acting-opioid-medication-in-the-management-of-opioid-dependence
#19
REVIEW
Rosella Saulle, Simona Vecchi, Linda Gowing
BACKGROUND: Opioid dependence (OD) is an increasing clinical and public health problem worldwide. International guidelines recommend opioid substitution treatment (OST), such as methadone and buprenorphine, as first-line medication treatment for OD. A negative aspect of OST is that the medication used can be diverted both through sale on the black market, and the unsanctioned use of medications. Daily supervised administration of medications used in OST has the advantage of reducing the risk of diversion, and may promote therapeutic engagement, potentially enhancing the psychosocial aspect of OST, but costs more and is more restrictive on the client than dispensing for off-site consumption...
April 27, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28447687/can-dual-ligand-targeting-enhance-cellular-uptake-of-nanoparticles
#20
Qiang-Sheng Xia, Hong-Ming Ding, Yu-Qiang Ma
Dual ligand targeting to different types of over-expressed receptors on cell surfaces is a promising strategy in nanomedicine. Here, by using dissipative particle dynamics simulations, the effect of the surface distribution and physicochemical properties of dual ligands on the cellular uptake of nanoparticles is systematically studied. It is found that the spontaneous rearrangement of dual ligands (from random to patterned distribution) on the nanoparticle surface can enhance the cellular uptake of nanoparticles...
April 27, 2017: Nanoscale
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