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Synthesis and Permeation Promoting Effect of Phenylalanine ester hydrochloride as a Small Molecular Biological Permeation Enhancer.

Byline: Xianhe Wang, Ying Li and Yunting Wang


Objective: The purpose was to employ P-toluene sulfonyl chloride (PTSC) as a catalyst is to synthesise a series of phenylalanine ester hydrochlorides. The synthesis process of L-phenylalanine methyl ester hydrochloride ((L-PM) was optimized by response surface method. Meanwhile, L-PM as the biological penetration enhancer was utilized to investigate the effect of caffeine and acyclovir on transdermal permeation. This study also investigates the effect of stereo configuration and dosage of L-PM on enhancing drug penetration.

Methods: Phenylalanine ester hydrochlorides were synthesized using phenylalanine, alcohol (C1-C4) and PTSC through the one-pot reaction. Meanwhile, the saturated acyclovir solution or 1% caffeine solution containing L-PM would be prepared as the test solution, while saline served as the acceptor. Subsequently, the test was performed on pig skin at 337.5AdegC, and the acceptor was taken at different time points for liquid phase analysis.

Results: The results of process optimization show that the optimum reaction conditions: reaction temperature 76.80AdegC, reaction time 12 hours, n(L-try-ptophan):n (PTSC) 0.15:1.0. The results of transdermal penetration test show that L-PM had a better effect the acyclovir and the caffeine. The dosage of 0.5% L-PM had the best penetration effect on acyclovir. L-PM could significantly promote the percutaneous absorption of acyclovir either alone or the combination of L-PM and menthol.

Conclusion: In conclusion, PTSC can increase the yields of the products and reduce the cost. This study also shows that the stereo configuration and dosage of L-PM has noticeable effect on enhancing drug penetration.

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Author:Xianhe Wang, Ying Li and Yunting Wang
Publication:Journal of Pakistan Medical Association
Date:Jul 31, 2020
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