Curcumin Micelles Entrapped in Eudragit S-100 Matrix: a Synergistic Strategy for Enhanced Oral Delivery

Abstract

Background: Therapeutic activities of curcumin (CUR) via oral administration are hampered by the lack of bioavailability due to its poor water solubility and rapid degradation in GI tract. Materials & methods: This preliminary study developed CUR micelle-eudragit S100 (EUD) dry powder (CM-EDP) spray-dried formulations. Poloxamer 407 was used as a micelle-forming agent and EUD as an entrapping matrix for protection over hydrolysis and enzymes in the GI tract. Results: The morphology of CM-EDP showed agglomeration with cratering on the surface of particles. Differential thermal analysis and x-ray diffractometry data exhibited evidence that CUR was converted into amorphous solid. An increased concentration of micelle-forming and dispersion matrix polymers resulted in a high fraction of drug being converted into the amorphous state. A significant increase in dissolution by 7–10 times was achieved compared with that of raw CUR. Conclusion: The present study disclosed the CM-EDP potency for future development of CUR oral formulation.

Lay abstract

Curcumin (CUR) is a natural compound that shows several pharmacological activities, including anti-inflammatory and potential actions against Parkinson’s and Alzheimer’s. However, several drawbacks need to be addressed its application as a therapeutic agent via oral administration. These drawbacks include its poor water solubility and rapid degradation in the GI tract. The present study developed CUR micelle-eudragit S100 (EUD) dry powder formulation involving poloxamer 407 as solubilizing agent and EUD as entrapping matrix for protection in acidic environments and the enzymes in the GI tract. The final product is in the form of dry powder, which showed potency in enhancing CUR absorption following oral administration.

Keywords:

• curcumin
• eudragit s-100
• micelles
• poloxamer 407
• powder
• spray drying

Author contributions

H Yusuf, MAS Rijal, RA Rahmawati and D Isadiartuti were responsible for study conception and design. H Yusuf, MAS Rijal, RA Rahmawati and D Isadiartuti were responsible for acquisition of data; H Yusuf, M AS Rijal, RA Rahmawati and D Isadiartuti were responsible for data analysis, drafting and revision of the manuscript; H Yusuf, MAS Rijal, RA Rahmawati and D Isadiartuti were contributed to the final approval of the manuscript. H Yusuf, MAS Rijal, RA Rahmawati and D Isadiartuti were accountable for all aspects of the work.

Financial& competing interests disclosure

The authors acknowledge support from the Faculty of Pharmacy, Universitas Airlangga, during the development of the project. This research was supported by The Directorate General of Higher Education, The Republic of Indonesia, under the PTUPT 2020 grant. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.