Synthesis and Formulation of Ibuprofen Pro-Drugs For Enhanced Transdermal Absorption

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Journal Title, Volume, Page: 
International Journal of Pharmacy and Pharmaceutical Sciences. 01/2015
Year of Publication: 
Murad N Abualhasan
Mohyeddin Assali
Current Affiliation: 
Department of Pharmacy, Faculty of Medicine and Health Sciences, An-Najah National University, Nablus, Palestine
Abdel Naser Zaid
Nidal Jaradat
Rana Tarayra
Aseel Hamdan
Rula Ardah
Preferred Abstract (Original): 

Background: The transdermal delivery (TDD) is one of the most attractive routs for drug administration as it eliminates the GIT absorption variable, improves patient compliance and also reduces drug plasma fluctuations. However, TDD only drugs with suitable physico-chemical properties can be absorbed.
The oral administration of NSAIDs for long time can cause gastric mucosal damage, which may result in ulceration and bleeding. Thus, the development of a TDD of NSAIDs is of a great interest as it decreases GIT side effects.
Purpose: The aim is to synthesize ibuprofen prodrugs that have more suitable physicochemical properties and formulate them into liquid formulation for topical administration.
Method: the synthesis of ibuprofen alkyl esters was carried out by esterification reactions with methanol, ethanol, propanol, butanol, pentanol and hexanol. The formulated samples were then subjected to stability studies according to ICH guidelines.
Results: We have successfully synthesized and characterized various esters of ibuprofen. Moreover, ibuprofen butyl ester has been prepared as topical solutions. The formulated TDD was tested for stability according to ICH guidelines and the results showed no changes in the initial appearance during three months of study at room temperature & at 40 °C.
Conclusion: The assay and pH were within the pharmacopeial limits during the period of the study. In conclusion a stable topical formulation of Ibuprofen esters was obtained.

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