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Labeling and Imaging of Amyloid Plaques in Brain Tissue Using the Natural Polyphenol Curcumin

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Colon targeted curcumin microspheres laden with ascorbic acid for bioavailability enhancement.

Preeti G Karade¹, Namdeo R Jadhav²

¹a Department of Pharmaceutics , Appasaheb Birnale College of Pharmacy , Sangli , India.

Journal of Microencapsulation

|July 17, 2018

Summary

Ascorbic acid (AA) stabilized curcumin (CUR) in colon-specific microspheres (CSMS), enhancing oral bioavailability. This novel formulation successfully delivered CUR to the colon, proving effective for improved drug delivery.

Keywords:

Ascorbic acid–drug interactions bioavailability colon-specific curcumin in-vivo

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Area of Science:

Pharmaceutical Sciences
Drug Delivery Systems
Bioavailability Enhancement

Background:

Curcumin (CUR) exhibits poor oral bioavailability due to degradation in the gastrointestinal tract.
Colon-specific drug delivery systems are needed to overcome CUR's limitations and improve therapeutic efficacy.
Ascorbic acid (AA) has potential stabilizing properties for sensitive compounds.

Purpose of the Study:

To develop and optimize colon-specific chitosan microspheres (CSMS) loaded with curcumin (CUR) and ascorbic acid (AA).
To enhance the oral bioavailability of CUR through colon targeting.
To investigate the stabilizing effect of AA on CUR degradation.

Main Methods:

A 3^2 factorial design was employed to optimize CSMS containing CUR and AA.
Optimized CSMS were coated with Eudragit S-100 for colon-specific delivery.
In vitro drug release, in vivo pharmacokinetics, and organ distribution studies were conducted in Albino Wistar rats.

Main Results:

Ascorbic acid (AA) effectively stabilized curcumin (CUR) in alkaline pH, preventing degradation (98.5-100% stabilization).
Complete amorphization and molecular dispersion of CUR within the microspheres were observed.
Colon-specific delivery of CUR microspheres (MS) was achieved, with 90% of MS reaching the colon within 8 hours, leading to enhanced CUR bioavailability.

Conclusions:

Ascorbic acid (AA) within the microspheres effectively shielded curcumin (CUR) from degradation.
The developed double-coated microspheres represent a promising colon-targeted system for CUR.
This formulation significantly enhances CUR bioavailability, offering a viable strategy for improved oral drug delivery.