scholarly journals Evaluation of the Percutaneous Absorption of Ketamine HCl, Gabapentin, Clonidine HCl, and Baclofen, in Compounded Transdermal Pain Formulations, Using the Franz Finite Dose Model

Pain Medicine ◽  
2016 ◽  
Vol 17 (2) ◽  
pp. 230-238 ◽  
Author(s):  
August S. Bassani ◽  
Daniel Banov
Keyword(s):  
Percutaneous Absorption ◽  
Drug Distribution ◽  
Drug Formulation ◽  
Specific Patient ◽  
Oral Pain ◽  
Peak Flux ◽  
Dose Model ◽  
Compounded Drug ◽  
Ketamine Hcl

Abstract Objective. This study evaluates the ability of four commonly used analgesics (ketamine HCl, gabapentin, clonidine HCl, and baclofen), when incorporated into two transdermal compounding bases, Lipoderm and Lipoderm ActiveMax, to penetrate human cadaver trunk skin in vitro , using the Franz finite dose model. Design. In vitro experimental study . Methods. Ketamine HCl 5% w/w, gabapentin 10% w/w, clonidine HCl 0.2% w/w, and baclofen 2% w/w were compounded into two transdermal bases, Lipoderm and Lipoderm ActiveMax. Each compounded drug formulation was tested on skin from three different donors and three replicate skin sections per donor. The Franz finite dose model was used in this study to evaluate the percutaneous absorption and distribution of drugs within each formulation. Results. Rapid penetration to peak flux was detected for gabapentin and baclofen at approximately 1 hour after application. Clonidine HCl also had a rapid penetration to peak flux occurring approximately 1 hour after application and had a secondary peak at approximately 40 hours. Ketamine HCl exhibited higher overall absorption rates than the other drugs, and peaked at 6–10 hours. Similar patterns of drug distribution within the skin were also observed using both transdermal bases. Conclusions. This study suggests that the combination of these 4 analgesic drugs can be successfully delivered transdermally, using either Lipoderm or Lipoderm ActiveMax. Compounded transdermal drug preparations may then provide physicians with an alternative to traditional oral pain management regimens that can be personalized to the specific patient with the potential for enhanced pain control.

Evaluation of Antibacterial and Antidiabetic Potential of Silver Nanoparticles using Eugenia Uniflora L. Seed Extract

2020 ◽  
Vol 13 (6) ◽  
pp. 5217-5225
Author(s):  
Guru Kumar Dugganaboyana ◽  
Chethankumar Mukunda ◽  
Suresh Darshini Inakanally
Keyword(s):  
Biomedical Applications ◽  
Pathogenic Bacteria ◽  
Seed Extract ◽  
Drug Formulation ◽  
Visible Spectroscopy ◽  
Plant Materials ◽  
X Ray ◽  
Eugenia Uniflora ◽  
Uv Visible

In recent years, green nanotechnology-based approaches using plant materials have been accepted as an environmentally friendly and cost-effective approach with various biomedical applications. In the current study, AgNPs were synthesized using the seed extract of the Eugenia uniflora L. (E.uniflora). Characterization was done using UV-Visible spectroscopy, X-ray diffraction (XRD), scanning electronic microscopy (SEM) and energy-dispersive X-ray spectroscopy (EDX) analyses. The formation of AgNPs has confirmed through UV-Visible spectroscopy (at 466 nm) by the change of color owing to surface Plasmon resonance. Based on the XRD pattern, the crystalline property of AgNPs was established. The functional group existing in seed of E.uniflora extract accountable for the reduction of Ag+ ion and the stabilization of AgNPs was investigated. The morphological structures and elemental composition was determined by SEM and EDX analysis. With the growing application of AgNPs in biomedical perspectives, the biosynthesized AgNPs were evaluated for their antibacterial and along with their antidiabetic potential. The results showed that AgNPs are extremely effective with potent antidiabetic potential at a very low concentration. It also exhibited potential antibacterial activity against the three tested human pathogenic bacteria. Overall, the results highlight the effectiveness and potential applications of AgNPs in biomedical fields such as in the treatment of acute illnesses as well as in drug formulation for treating various diseases such as cancer and diabetes. It could be concluded that E. uniflora seed extract AgNPs can be used efficiently for in vitro evaluation of their antibacterial and antidiabetic effects with potent biomedical applications.

scholarly journals A “Smart” Biosensor-Enabled Intravascular Catheter and Platform for Dynamic Delivery of Propofol to “Close the Loop” for Total Intravenous Anesthesia

2021 ◽  
Vol 186 (Supplement_1) ◽  
pp. 370-377
Author(s):  
Edward Chaum ◽  
Ernő Lindner
Keyword(s):  
Real Time ◽  
Drug Distribution ◽  
Population Based ◽  
Pharmacokinetic Data ◽  
Drug Infusion ◽  
Blood Concentrations ◽  
The Usa ◽  
The Difference ◽  
Automated Delivery

ABSTRACT Background Target-controlled infusion anesthesia is used worldwide to provide user-defined, stable, blood concentrations of propofol for sedation and anesthesia. The drug infusion is controlled by a microprocessor that uses population-based pharmacokinetic data and patient biometrics to estimate the required infusion rate to replace losses from the blood compartment due to drug distribution and metabolism. The objective of the research was to develop and validate a method to detect and quantify propofol levels in the blood, to improve the safety of propofol use, and to demonstrate a pathway for regulatory approval for its use in the USA. Methods We conceptualized and prototyped a novel “smart” biosensor-enabled intravenous catheter capable of quantifying propofol at physiologic levels in the blood, in real time. The clinical embodiment of the platform is comprised of a “smart” biosensor-enabled catheter prototype, a signal generation/detection readout display, and a driving electronics software. The biosensor was validated in vitro using a variety of electrochemical methods in both static and flow systems with biofluids, including blood. Results We present data demonstrating the experimental detection and quantification of propofol at sub-micromolar concentrations using this biosensor and method. Detection of the drug is rapid and stable with negligible biofouling due to the sensor coating. It shows a linear correlation with mass spectroscopy methods. An intuitive graphical user interface was developed to: (1) detect and quantify the propofol sensor signal, (2) determine the difference between targeted and actual propofol concentration, (3) communicate the variance in real time, and (4) use the output of the controller to drive drug delivery from an in-line syringe pump. The automated delivery and maintenance of propofol levels was demonstrated in a modeled benchtop “patient” applying the known pharmacokinetics of the drug using published algorithms. Conclusions We present a proof-of-concept and in vitro validation of accurate electrochemical quantification of propofol directly from the blood and the design and prototyping of a “smart,” indwelling, biosensor-enabled catheter and demonstrate feedback hardware and software architecture permitting accurate measurement of propofol in blood in real time. The controller platform is shown to permit autonomous, “closed-loop” delivery of the drug and maintenance of user-defined propofol levels in a dynamic flow model.

scholarly journals Single cell organization and cell cycle characterization of DNA stained multicellular tumor spheroids

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Karl Olofsson ◽  
Valentina Carannante ◽  
Madoka Takai ◽  
Björn Önfelt ◽  
Martin Wiklund
Keyword(s):  
Cell Cycle ◽  
Single Cell ◽  
Drug Distribution ◽  
In Vitro Models ◽  
Biological Information ◽  
Dimensional Structure ◽  
Multicellular Tumor Spheroids ◽  
Tumor Spheroids ◽  
Nuclear Segmentation

AbstractMulticellular tumor spheroids (MCTSs) can serve as in vitro models for solid tumors and have become widely used in basic cancer research and drug screening applications. The major challenges when studying MCTSs by optical microscopy are imaging and analysis due to light scattering within the 3-dimensional structure. Herein, we used an ultrasound-based MCTS culture platform, where A498 renal carcinoma MCTSs were cultured, DAPI stained, optically cleared and imaged, to connect nuclear segmentation to biological information at the single cell level. We show that DNA-content analysis can be used to classify the cell cycle state as a function of position within the MCTSs. We also used nuclear volumetric characterization to show that cells were more densely organized and perpendicularly aligned to the MCTS radius in MCTSs cultured for 96 h compared to 24 h. The method presented herein can in principle be used with any stochiometric DNA staining protocol and nuclear segmentation strategy. Since it is based on a single counter stain a large part of the fluorescence spectrum is free for other probes, allowing measurements that correlate cell cycle state and nuclear organization with e.g., protein expression or drug distribution within MCTSs.

In vitro percutaneous absorption of metal compounds

2007 ◽  
Vol 170 (1) ◽  
pp. 49-56 ◽  
Author(s):  
Francesca Larese ◽  
Adami Gianpietro ◽  
Marta Venier ◽  
Giovanni Maina ◽  
Nadia Renzi
Keyword(s):  
Percutaneous Absorption ◽  
Metal Compounds ◽  
In Vitro Percutaneous Absorption

In vitro percutaneous absorption of metronidazole and glucose: Comparison of o/w, w/o/w and w/o systems

1995 ◽  
Vol 121 (2) ◽  
pp. 169-179 ◽  
Author(s):  
L.A.M. Ferreira ◽  
J. Doucet ◽  
M. Seiller ◽  
J.L. Grossiord ◽  
J.P. Marty ◽  
...  
Keyword(s):  
Percutaneous Absorption ◽  
In Vitro Percutaneous Absorption

Oleic acid increases uptake and decreases the P-gp-mediated efflux of the veterinary anthelmintic Ivermectin

Drug Research ◽  
2018 ◽  
Vol 69 (03) ◽  
pp. 173-180 ◽  
Author(s):  
Bilal Houshaymi ◽  
Nadine Nasreddine ◽  
Mamdouh Kedees ◽  
Zeina Soayfane
Keyword(s):  
Oleic Acid ◽  
Intestinal Mucosa ◽  
Drug Formulation ◽  
Dependent Manner ◽  
Cancer Resistance ◽  
P Glycoprotein ◽  
Resistance Protein ◽  
Complex Micelles

AbstractThe bioavailability of ivermectin is modulated by lipid-based formulations and membrane efflux transporters such as Breast Cancer Resistance Protein and P-glycoprotein (BCRP and P-gp). We have investigated the effect of oleic acid on the uptake of ivermectin in vitro using Caco-2 cells and in vivo in the intestines of wild-type mice. Complex micelles (M) with oleic acid induced a significant increase (e. g. for M3 was 7-fold, p≤0.001) in the uptake of the drug in a time-dependent manner with no involvement of cholesterol in the mechanism. In vivo results showed a significant increase in the concentration of plasma and intestinal mucosa ivermectin (p≤0.01) in mice receiving oleic acid-based drug formulation. We also examined the expression of the drug efflux transporter, BCRP and P-gp in Caco-2 cells and found a significant decrease (p≤0.001) in their level in the presence of 5 mM oleic acid. Treatment of mice with oleic acid-based formulation showed a significant decrease in the activity of P-gp in the intestinal mucosa (p≤0.01). This study highlighted the effect of oleic acid in decreasing the expression and the activity of P-gp-mediated ivermectin efflux and in limiting the drug absorption by increasing its uptake and bioavailability in Caco-2 cells and intestine, respectively.

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