NDLI: Optimization of Naltrexone Diclofenac Codrugs for Sustained Drug Delivery Across Microneedle-Treated Skin

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Optimization of Naltrexone Diclofenac Codrugs for Sustained Drug Delivery Across Microneedle-Treated Skin

Content Provider	Semantic Scholar
Author	Ghosh, Priyanka E. Lee, Domin Kim, Kyung Bo Stinchcomb, Audra L.
Copyright Year	2013
Abstract	ABSTRACTPurposeThe purpose of this work was to optimize the structure of codrugs for extended delivery across microneedle treated skin. Naltrexone, the model compound was linked with diclofenac, a nonspecific cyclooxygenase inhibitor to enhance the pore lifetime following microneedle treatment and develop a 7 day transdermal system for naltrexone.MethodsFour different codrugs of naltrexone and diclofenac were compared in terms of stability and solubility. Transdermal flux, permeability and skin concentration of both parent drugs and codrugs were quantified to form a structure permeability relationship.ResultsThe results indicated that all codrugs bioconverted in the skin. The degree of conversion was dependent on the structure, phenol linked codrugs were less stable compared to the secondary alcohol linked structures. The flux of naltrexone across microneedle treated skin and the skin concentration of diclofenac were higher for the phenol linked codrugs. The polyethylene glycol link enhanced solubility of the codrugs, which translated into flux enhancement.ConclusionThe current studies indicated that formulation stability of codrugs and the flux of naltrexone can be enhanced via structure design optimization. The polyethylene glycol linked naltrexone diclofenac codrug is better suited for a 7 day drug delivery system both in terms of stability and drug delivery.
Starting Page	148
Ending Page	159
Page Count	12
File Format	PDF HTM / HTML
DOI	10.1007/s11095-013-1147-8
PubMed reference number	23943543
Journal	Medline
Volume Number	31
Alternate Webpage(s)	https://permegear.com/?mdocs-file=8331
Alternate Webpage(s)	https://doi.org/10.1007/s11095-013-1147-8
Journal	Pharmaceutical Research
Language	English
Access Restriction	Open
Content Type	Text
Resource Type	Article

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