Ester prodrugs

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Synthesis of Naproxen Pro-Drugs for Enhanced Transdermal Absorption

Journal Title, Volume, Page: 
Journal of Chemical and Pharmaceutical Research 08/2014; 6(8):1-4
Year of Publication: 
2014
Authors: 
Mohyeddin Assali
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Abdel Nasr Zaid
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Murad N Abualhasan
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Nidal Jaradat
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Rana Tarayra
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Aseel Hamdan
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Rula Ardah
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Preferred Abstract (Original): 

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) such as Naproxen have been used for a long time for the treatment of acute and chronic inflammation conditions. However, the oral administration of NSAIDs for a long time can cause gastric mucosal damage, which may result in ulceration and bleeding. Therefore, the development of a transdermal drug delivery (TDD) system of NSAIDs is of a great interest as it decreases GIT side effect and provides a constant release of drug in a determined period of time. Moreover, one of the important parameters of TTD is improving the permeability of the drug through human skin, since the stratum corneum layer of the epidermis prevents the permeability of various drugs and the naproxen in particular. In this present paper, we have successfully synthesized and characterized various ester derivatives of naproxen (methyl, ethyl, propyl, butyl, pentyl and hexyl esters) that have more suitable physicochemical properties for TDD and the butyl ester derivative has been formulated into liquid formulation for topical administration. The formulation was tested for stability according to ICH guidelines. No change in the initial appearance was observed during three months of study at room temperature & at 40 °C. The assay and pH were within the international standard limits during the period of the study. So, stable topical formulation of naproxen ester has been obtained.

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Synthesis of Naproxen Pro-Drugs for Enhanced Transdermal Absorption

Journal Title, Volume, Page: 
Journal of Chemical and Pharmaceutical Research 08/2014; 6(8):1-4
Year of Publication: 
2014
Authors: 
Mohyeddin Assali
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Abdel Nasr Zaid
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Murad N Abualhasan
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Nidal Jaradat
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Rana Tarayra
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Aseel Hamdan
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Rula Ardah
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Preferred Abstract (Original): 

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) such as Naproxen have been used for a long time for the treatment of acute and chronic inflammation conditions. However, the oral administration of NSAIDs for a long time can cause gastric mucosal damage, which may result in ulceration and bleeding. Therefore, the development of a transdermal drug delivery (TDD) system of NSAIDs is of a great interest as it decreases GIT side effect and provides a constant release of drug in a determined period of time. Moreover, one of the important parameters of TTD is improving the permeability of the drug through human skin, since the stratum corneum layer of the epidermis prevents the permeability of various drugs and the naproxen in particular. In this present paper, we have successfully synthesized and characterized various ester derivatives of naproxen (methyl, ethyl, propyl, butyl, pentyl and hexyl esters) that have more suitable physicochemical properties for TDD and the butyl ester derivative has been formulated into liquid formulation for topical administration. The formulation was tested for stability according to ICH guidelines. No change in the initial appearance was observed during three months of study at room temperature & at 40 °C. The assay and pH were within the international standard limits during the period of the study. So, stable topical formulation of naproxen ester has been obtained.

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