scholarly journals Novel Bone-Targeting Agent for Enhanced Delivery of Vancomycin to Bone

2015 ◽  
Vol 60 (3) ◽  
pp. 1865-1868 ◽  
Author(s):  
Zaineb A. F. Albayati ◽  
Manjula Sunkara ◽  
Suzannah M. Schmidt-Malan ◽  
Melissa J. Karau ◽  
Andrew J. Morris ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Targeted Delivery ◽  
Therapeutic Outcome ◽  
Surgical Debridement ◽  
High Affinity ◽  
Bone Infections ◽  
Bone Targeting ◽  
Pharmacokinetic Properties

We examined the pharmacokinetic properties of vancomycin conjugated to a bone-targeting agent (BT) with high affinity for hydroxyapatite after systemic intravenous administration. The results confirm enhanced persistence of BT-vancomycin in plasma and enhanced accumulation in bone relative to vancomycin. This suggests that BT-vancomycin may be a potential carrier for the systemic targeted delivery of vancomycin in the treatment of bone infections, potentially reducing the reliance on surgical debridement to achieve the desired therapeutic outcome.

A Comprehensive Insight Towards Pharmaceutical Aspects of Graphene Nanosheets

2020 ◽  
Vol 21 (11) ◽  
pp. 1016-1027 ◽  
Author(s):  
Fatemeh Emadi ◽  
Arash Emadi ◽  
Ahmad Gholami
Keyword(s):  
Targeted Delivery ◽  
Graphene Nanosheets ◽  
High Surface ◽  
High Surface Area ◽  
Charge Carriers ◽  
Pharmaceutical Sciences ◽  
Pharmacokinetics And Pharmacodynamics ◽  
Mobility Of Charge Carriers ◽  
Graphene Derivatives ◽  
Pharmacokinetic Properties

Graphene Derivatives (GDs) have captured the interest and imagination of pharmaceutical scientists. This review exclusively provides pharmacokinetics and pharmacodynamics information with a particular focus on biopharmaceuticals. GDs can be used as multipurpose pharmaceutical delivery systems due to their ultra-high surface area, flexibility, and fast mobility of charge carriers. Improved effects, targeted delivery to tissues, controlled release profiles, visualization of biodistribution and clearance, and overcoming drug resistance are examples of the benefits of GDs. This review focuses on the application of GDs for the delivery of biopharmaceuticals. Also, the pharmacokinetic properties and the advantage of using GDs in pharmaceutics will be reviewed to achieve a comprehensive understanding about the GDs in pharmaceutical sciences.

scholarly journals Physicochemical Effects of the Major Quassinoids in a Standardized Eurycoma longifolia Extract (Fr 2) on the Bioavailability and Pharmacokinetic Properties, and their Implications for Oral Antimalarial Activity

2011 ◽  
Vol 6 (3) ◽  
pp. 1934578X1100600 ◽  
Author(s):  
Bin-Seng Low ◽  
Chin-Hoe Teh ◽  
Kah-Hay Yuen ◽  
Kit-Lam Chan
Keyword(s):  
Oral Administration ◽  
Intravenous Administration ◽  
Antimalarial Activity ◽  
Elimination Rate ◽  
Rat Plasma ◽  
Chemical Degradation ◽  
Absolute Bioavailability ◽  
Phytochemical Analysis ◽  
Eurycoma Longifolia ◽  
Pharmacokinetic Properties

A simple validated LC-UV method for the phytochemical analysis of four bioactive quassinoids, 13α(21)-epoxyeurycomanone (EP), eurycomanone (EN), 13α,21-dihydroeurycomanone (ED) and eurycomanol (EL) in rat plasma following oral (200 mg/kg) and intravenous administration (10 mg/kg) of a standardized extract Fr 2 of Eurycoma longifolia Jack was developed for pharmacokinetic and bioavailability studies. The extract Fr 2 contained 4.0%, 18.5%, 0.7% and 9.5% of EP, EN, ED and EL, respectively. Following intravenous administration, EP displayed a relatively longer biological half-life (t½ = 0.75 ± 0.25 h) due primarily to its lower elimination rate constant (ke) of 0.84 ± 0.26 h−1) when compared with the t½ of 0.35 ± 0.04 h and ke of 2.14 ± 0.27 h−1, respectively of EN. Following oral administration, EP showed a higher Cmax of 1.61± 0.41 μg/mL over that of EN (Cmax = 0.53 ± 0.10 μg/mL). The absolute bioavailability of EP was 9.5-fold higher than that of EN, not because of chemical degradation since both quassinoids were stable at the simulated gastric pH of 1. Instead, the higher log Kow value of EP (-0.43) contributed to greater membrane permeability over that of EN (log Kow = −1.46) at pH 1. In contrast, EL, being in higher concentration in the extract than EP, was not detected in the plasma after oral administration because of substantial degradation by the gastric juices after 2 h. Similarly, ED, being unstable at the acidic pH and together with its low concentration in Fr 2, was not detectable in the rat plasma. In conclusion, upon oral administration of the bioactive standardized extract Fr 2, EP and EN may be the only quassinoids contributing to the overall antimalarial activity; this is worthy of further investigation.

Continuous Infusion of Naloxone in the Treatment of Narcotic Overdose

1981 ◽  
Vol 15 (12) ◽  
pp. 945-950 ◽  
Author(s):  
J. Chris Bradberry ◽  
Marsha A. Raebel
Keyword(s):  
Continuous Infusion ◽  
Intravenous Administration ◽  
Clinical Studies ◽  
Case Reports ◽  
Mode Of Administration ◽  
Pharmacokinetic Properties ◽  
Infusion Method

This paper describes case reports and pharmacokinetic information regarding the continuous intravenous administration of naloxone in treatment of narcotic overdose. Continuous naloxone infusion has been used successfully in acutely narcotized patients, and a review of the pharmacodynamic and pharmacokinetic properties of naloxone indicate the reasons for this mode of administration. Summaries of clinical studies in support of the infusion method are given. A naloxone protocol is outlined.

scholarly journals Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring

MedChemComm ◽  
2017 ◽  
Vol 8 (8) ◽  
pp. 1697-1705 ◽  
Author(s):  
Dominik Heimann ◽  
Corinna Lueg ◽  
Henk de Vries ◽  
Bastian Frehland ◽  
Dirk Schepmann ◽  
...  
Keyword(s):  
High Affinity ◽  
Bioisosteric Replacement ◽  
Pharmacokinetic Properties

Three pairs of regioisomeric 1,2,4- and 1,3,4-oxadiazoles were synthesized as selective CB2 ligands. Although the 1,3,4-oxadiazoles should have better physicochemical and pharmacokinetic properties, their CB2 affinity was reduced.

Targeted delivery of chlorotoxin-modified DNA-loaded nanoparticles to glioma via intravenous administration

Biomaterials ◽  
2011 ◽  
Vol 32 (9) ◽  
pp. 2399-2406 ◽  
Author(s):  
Rongqin Huang ◽  
Weilun Ke ◽  
Liang Han ◽  
Jianfeng Li ◽  
Shuhuan Liu ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Targeted Delivery ◽  
Modified Dna

Targeted Delivery of DNA Encoding Cytotoxic Proteins through High-Affinity Fibroblast Growth Factor Receptors

1998 ◽  
Vol 9 (17) ◽  
pp. 2565-2575 ◽  
Author(s):  
Diana K. Hoganson ◽  
Lois A. Chandler ◽  
Graham A. Fleurbaaij ◽  
Wenbin Ying ◽  
Margaret E. Black ◽  
...  
Keyword(s):  
Growth Factor ◽  
Fibroblast Growth Factor ◽  
Targeted Delivery ◽  
Growth Factor Receptors ◽  
Fibroblast Growth ◽  
Dna Encoding ◽  
Fibroblast Growth Factor Receptors ◽  
High Affinity ◽  
Cytotoxic Proteins

scholarly journals Bone-targeting carbon dots: effect of nitrogen-doping on binding affinity

RSC Advances ◽  
2019 ◽  
Vol 9 (5) ◽  
pp. 2708-2717 ◽  
Author(s):  
Kyung Kwan Lee ◽  
Jae-Geun Lee ◽  
Chul Soon Park ◽  
Sun Hyeok Lee ◽  
Naren Raja ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Carbon Dots ◽  
Nitrogen Doping ◽  
Binding Activity ◽  
Rat Femur ◽  
Targeted Imaging ◽  
High Affinity ◽  
Bone Targeting ◽  
Fluorescent Carbon Dots ◽  
Strong Binding Activity

Fluorescent carbon dots selectively bind to skull tissues with high affinity, including a strong binding activity for calcium deficient hydroxyapatite, and rat femur, for bone targeted imaging.

scholarly journals Biopharmaceutical Characterization of Nebulized Antimicrobial Agents in Rats: 2. Colistin

2014 ◽  
Vol 58 (7) ◽  
pp. 3950-3956 ◽  
Author(s):  
Aline Vidal Lacerda Gontijo ◽  
Nicolas Grégoire ◽  
Isabelle Lamarche ◽  
Patrice Gobin ◽  
William Couet ◽  
...  
Keyword(s):  
Intravenous Administration ◽  
Antimicrobial Agents ◽  
Plasma Concentrations ◽  
Central Compartment ◽  
Plasma Drug ◽  
Pulmonary Infections ◽  
Epithelial Lining Fluid ◽  
Drug Concentrations ◽  
Pharmacokinetic Properties

ABSTRACTThe purpose of this study was to investigate the pharmacokinetic properties of colistin following intrapulmonary administration of colistin sulfate in rats. Colistin was infused or delivered in nebulized form at a dose of 0.35 mg/kg of body weight in rats, and plasma drug concentrations were measured for 4 h after administration. Bronchoalveolar lavages (BAL) were also conducted at 0.5, 2, and 4 h after intravenous (i.v.) administration and administration via nebulized drug to estimate epithelial lining fluid (ELF) drug concentrations. Unbound colistin plasma concentrations at distribution equilibrium (2 h postdosing) were almost identical after i.v. infusion and nebulized drug inhalation. ELF drug concentrations were undetectable in BAL samples after i.v. administration, but they were about 1,800 times higher than unbound plasma drug levels at 2 h and 4 h after administration of the nebulized drug. Simultaneous pharmacokinetic modeling of plasma and ELF drug concentrations was performed with a model characterized by a fixed physiological volume of ELF (VELF), a passive diffusion clearance (QELF) between plasma and ELF, and a nonlinear influx transfer from ELF to the central compartment, which was assessed by reducing the nebulized dose of colistin by 10-fold (0.035 mg kg−1). Thekmwas estimated to be 133 μg ml−1, and theVmax, in-to-Kmratio was equal to 2.5 × 10−3liter h−1kg−1, which was 37 times higher than theQELF(6.7 × 10−5liter h−1kg−1). This study showed that with the higher ELF drug concentrations after administration via nebulized aerosol than after intravenous administration, for antibiotics with low permeability such as colistin, nebulization offers a real potential over intravenous administration for the treatment of pulmonary infections.

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