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Research Article
Murad Abualhasan
An-Najah National University
Corresponding Author
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Background
Rutin is available in the market as a topical formulation for the treatment of several diseases such as internal bleeding, hemorrhoids, and varicose veins. However, these gels have low solubility and limited bioavailability due to their decreased lipid solubility. In this study, we aimed to synthesize a potentially novel lipophilic rutin prodrug. The suggested library of these prodrugs of rutin is to change the solubility profile to facilitate rutin transport across the biological barrier and therefore improve drug delivery through topical application.
Method:
Six derivatives of the Rutin based on ester pro-drug strategy were synthesized. The synthesized compounds were formulated into a topical ointment and their permeability through Franz diffusion was measured. UV analytical method was developed in our labs to quantify rutin derivatives both as raw material and in the final dosage form. The analytical method was then validated.
Results
The synthesized derivative esters of the Rutin were successfully achieved. The results of Franz diffusion showed that the transdermal permeability was best for decaacetylated rutin compared to the other esterified rutins. A simple analytical method for the analysis of the formulated rutin ester was developed and validated. Moreover, the formulated ointment of decaacetylated rutin in our research laboratory was found to be stable under stability accelerated conditions.
Conclusion
The Synthesis of potentially more lipophilic give novel rutin prodrugs suitable is for topical formulation. This project provides a synthetic approach for many similar natural products. The research idea and strategy followed in this research project is can be adapted by pharmaceutical and herbal establishments.
Keywords
rutin derivatives, analytical method, lipophilic
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No competing interests reported.
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This is a preprint. It has not completed peer review.
Research Article
Murad Abualhasan
An-Najah National University
Corresponding Author
Badges
Prescreen
This manuscript passed our Prescreen assessment
Complete author information
Appropriate declaration statements
Potential risks to human health
Prescreen
History
CURRENT STATUS: Posted
Version 1
Posted 25 Mar, 2021
No community comments so far
Metrics
Comments: 0
PDF Downloads: ...
HTML Views: ...
License:
This work is licensed under a CC BY 4.0 License. Read Full License
Background
Rutin is available in the market as a topical formulation for the treatment of several diseases such as internal bleeding, hemorrhoids, and varicose veins. However, these gels have low solubility and limited bioavailability due to their decreased lipid solubility. In this study, we aimed to synthesize a potentially novel lipophilic rutin prodrug. The suggested library of these prodrugs of rutin is to change the solubility profile to facilitate rutin transport across the biological barrier and therefore improve drug delivery through topical application.
Method:
Six derivatives of the Rutin based on ester pro-drug strategy were synthesized. The synthesized compounds were formulated into a topical ointment and their permeability through Franz diffusion was measured. UV analytical method was developed in our labs to quantify rutin derivatives both as raw material and in the final dosage form. The analytical method was then validated.
Results
The synthesized derivative esters of the Rutin were successfully achieved. The results of Franz diffusion showed that the transdermal permeability was best for decaacetylated rutin compared to the other esterified rutins. A simple analytical method for the analysis of the formulated rutin ester was developed and validated. Moreover, the formulated ointment of decaacetylated rutin in our research laboratory was found to be stable under stability accelerated conditions.
Conclusion
The Synthesis of potentially more lipophilic give novel rutin prodrugs suitable is for topical formulation. This project provides a synthetic approach for many similar natural products. The research idea and strategy followed in this research project is can be adapted by pharmaceutical and herbal establishments.
Figure 1
Figure 2
Figure 3
Figure 4
Figure 5
Figure 6
Figure 7
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