Acylcarnitine Chain Length Influences Carnitine‐enhanced Drug Flux through the Spinal Meninges: In Vitro

  title={Acylcarnitine Chain Length Influences Carnitine‐enhanced Drug Flux through the Spinal Meninges: In Vitro},
  author={Wolfgang C. Ummenhofer and Christopher M. Bernards},
Background Palmitoyl carnitine has been shown to improve the penetration of hydrophilic drugs through the spinal meninges. Naturally occurring acylcarnitines, however, exist as a homologous series of different acyl chain lengths. The purpose of this study was to determine the most effective acylcarnitine chain length to increase meningeal permeability. Methods The transmeningeal flux of mannitol, morphine, and sufentanil through monkey spinal meninges was determined before and after adding… 

The Role of Drug-Lipid Interactions on the Disposition of Liposome-Formulated Opioid Analgesics In Vitro and In Vivo

It is most important to note that increasing the lipid content of morphine liposomes increased the proportion of drug reaching the intrathecal space, and increasing the Liposome encapsulation efficiency was significantly more for sufentanil (100%) than for the other opioids (25%–30%).

Onset and offset of intrathecal morphine versus nalbuphine for postoperative pain relief after total hip replacement

This study aims to compare the postoperative analgesic effects of intrathecal morphine and nalbuphine, the endpoints being onset and offset of action.

Synthesis of a series of validoxylamine A esters and their biological activities.

Combining the results, esterification of VAA by introducing different acyl donors was beneficial for the development of new eco-friendly drugs in the field of pesticides.



Palmitoyl Carnitine Increases the Transmeningeal Flux of Hydrophilic but Not Hydrophobic Compounds In Vitro

Palmitoyl carnitine's ability to selectively increase the transmeningeal flux of hydrophilic compounds in vitro offers the possibility of improving the spinal bioavailability of this group of epidurally administered drugs in vivo.

Effect of (hydroxypropyl)-beta-cyclodextrin on flux of morphine, fentanyl, sufentanil, and alfentanil through the spinal meninges of monkey.

  • C. Bernards
  • Biology
    Journal of pharmaceutical sciences
  • 1994
It is found that cyclodextrin effectively decreases sufentanil's hydrophobicity by formation of inclusion complexes in the aqueous environments of the spinal meninges, which suggests that the rate-limiting step in opioid transfer was diffusion through the meninges not dissociation of the opioid cyclodesxtrin complex.

Kinetic analysis of phospholipid exchange between phosphatidylcholine/taurocholate mixed micelles : effect of the acyl chain moiety of the micellar phosphatidylcholine

The results argue that the hydrophobicity of the lipophilic core of bile salt/phospholipid mixed micelles is the predominant determinants of the rate of formation of transfer-competent, transient micelle fusions and a major determinant of the rates of micelle to water phospholipids dissociation.

Physical and chemical properties of drug molecules governing their diffusion through the spinal meninges.

The data suggest that it should be possible to design novel analgesics for which meningeal permeability is maximal, and that drugs that were either very hydrophilic or very Hydrophobic had permeability coefficients that were significantly less than drugs of intermediate hydrophobicity.

Morphine and alfentanil permeability through the spinal dura, arachnoid, and pia mater of dogs and monkeys.

In vitro measuring the permeability of morphine and alfentanil through the different components of the spinal meninges-dura mater, arachnoid mater, and pia mater-of dogs and monkeys concludes that this in vitro model has significant utility for studies aimed at predicting in vivo meningeal permeability and hence the potency and rapidity of action of any opioid administered by the epidural route.

Temperature dependence of membrane ion conductance analyzed by using the amphiphilic anion 5/6-carboxyfluorescein.

The results indicate that the rate of release of electrically charged dyes, such as 5/6-carboxyfluorescein from sealed lipid vesicles can be tightly coupled to the counterion leakage rate and hence can provide an accurate and convenient assay of relative ion flux across phospholipid bilayers.