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Literature DB >> 20451376

Novel 3-O-pegylated carboxylate and 3-O-pegylated carbamate prodrugs of naltrexone for microneedle-enhanced transdermal delivery.

Thirupathi Reddy Yerramreddy¹, Mikolaj Milewski, Narsimha Reddy Penthala, Audra L Stinchcomb, Peter A Crooks.

Abstract

A small library of novel 3-O-pegylated carboxylate prodrugs (4a-4b) and 3-O-pegylated carbamate prodrugs (9a-9b) of naltrexone were synthesized. The goal behind the design of these prodrugs was to investigate their potential for microneedle-enhanced transdermal delivery. All the synthesized 3-O-pegylated carboxylate prodrugs (4a-4b) and 3-O-pegylated carbamate prodrugs (9a-9b) of naltrexone were found to have adequate stability in a transdermal formulation and improved apparent solubility compared to naltrexone. Viscosity effects were postulated to be responsible for the observed non-linearity in the flux-concentration profile of these prodrugs. Copyright 2010 Elsevier Ltd. All rights reserved.

Entities: Chemical Disease Species

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Year: 2010 PMID： 20451376 PMCID： PMC3726000 DOI： 10.1016/j.bmcl.2010.04.049

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

25 in total

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Review 2. Effect of pegylation on pharmaceuticals.

Authors: J Milton Harris; Robert B Chess
Journal: Nat Rev Drug Discov Date: 2003-03 Impact factor: 84.694

Review 3. Rational treatment of addiction.

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Journal: Curr Opin Chem Biol Date: 1998-08 Impact factor: 8.822

4. Microfabricated microneedles: a novel approach to transdermal drug delivery.

Authors: S Henry; D V McAllister; M G Allen; M R Prausnitz
Journal: J Pharm Sci Date: 1998-08 Impact factor: 3.534

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

Authors: Mikolaj Milewski; Thirupathi Reddy Yerramreddy; Priyanka Ghosh; Peter A Crooks; Audra L Stinchcomb
Journal: J Control Release Date: 2010-06-04 Impact factor: 9.776

6. Naltrexone vs. nefazodone for treatment of alcohol dependence. A placebo-controlled trial.

Authors: H R Kranzler; V Modesto-Lowe; J Van Kirk
Journal: Neuropsychopharmacology Date: 2000-05 Impact factor: 7.853

7. Naltrexone and alcohol dependence. Role of subject compliance.

Authors: J R Volpicelli; K C Rhines; J S Rhines; L A Volpicelli; A I Alterman; C P O'Brien
Journal: Arch Gen Psychiatry Date: 1997-08

8. Physicochemical evaluation, in vitro human skin diffusion, and concurrent biotransformation of 3-O-alkyl carbonate prodrugs of naltrexone.

Authors: Omathanu Pillai; Mohamed O Hamad; Peter A Crooks; Audra L Stinchcomb
Journal: Pharm Res Date: 2004-07 Impact factor: 4.200

Novel 3-O-pegylated carboxylate and 3-O-pegylated carbamate prodrugs of naltrexone for microneedle-enhanced transdermal delivery.

1. Transdermal delivery of antisense oligonucleotides with microprojection patch (Macroflux) technology.

Review 2. Effect of pegylation on pharmaceuticals.

Review 3. Rational treatment of addiction.

4. Microfabricated microneedles: a novel approach to transdermal drug delivery.

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

6. Naltrexone vs. nefazodone for treatment of alcohol dependence. A placebo-controlled trial.

7. Naltrexone and alcohol dependence. Role of subject compliance.

8. Physicochemical evaluation, in vitro human skin diffusion, and concurrent biotransformation of 3-O-alkyl carbonate prodrugs of naltrexone.

9. Behavioral naltrexone therapy: an integrated treatment for opiate dependence.

10. Naltrexone in the treatment of alcohol dependence.

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

Review 2. Microneedles for drug and vaccine delivery.

3. Enhancement strategies for transdermal drug delivery systems: current trends and applications.