NDLI: In vitro permeation of a pegylated naltrexone prodrug across microneedle-treated skin.

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In vitro permeation of a pegylated naltrexone prodrug across microneedle-treated skin.

Content Provider	Semantic Scholar
Author	Milewski, Mikolaj Yerramreddy, Thirupathi Reddy Ghosh, Priyanka E. Crooks, Peter A. Stinchcomb, Audra L.
Copyright Year	2010
Abstract	Microneedles (MN) are a useful tool for increasing skin permeability to xenobiotics. Previous research showed marked improvement in the percutaneous flux of naltrexone (NTX) hydrochloride by the use of MN skin pretreatment alone; however, for better therapeutic effect, further enhancement is desired. The goal of this in vitro study was to combine microneedle skin pretreatment with the use of a highly water-soluble PEGylated naltrexone prodrug (polyethyleneglycol-NTX, PEG-NTX) to investigate its transdermal transport at varying concentrations. Solubility and stability of the prodrug were investigated. In vitro diffusion experiments employing MN-treated minipig skin were used to evaluate the performance of the PEGylated prodrug. The results revealed substantial deviation from ideal behavior, with the flux through MN-treated skin having a nonlinear relationship to the prodrug concentration in the donor solution. While in the lower concentration range tested the prodrug flux increase was proportional to the concentration increase, at high concentrations it showed no such dependence. Accounting for the decrease in the effective prodrug diffusivity accompanying the increase in viscosity, as predicted by the Stokes-Einstein equation, provided a rationale for the observed flux values. Increasing the viscosity of the donor solution is hypothesized to afford a curvilinear permeation profile for the PEGylated NTX prodrug.
Starting Page	37
Ending Page	44
Page Count	8
File Format	PDF HTM / HTML
PubMed reference number	20678989
Journal	Medline
Volume Number	146
Issue Number	1
Alternate Webpage(s)	https://permegear.com/?mdocs-file=8365
Alternate Webpage(s)	https://doi.org/10.1016/j.jconrel.2010.05.034
Journal	Journal of controlled release : official journal of the Controlled Release Society
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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