Hesperidin gastroresistant microparticles by spray-drying: preparation, characterization, and dissolution profiles

Area of Science:

• Pharmaceutical Technology
• Materials Science
• Drug Delivery

Background:

• Hesperidin (Hd) is a flavonoid with potential therapeutic benefits but poor oral bioavailability.
• Developing effective oral delivery systems for flavonoids like Hd is crucial for their therapeutic application.
• Gastroresistant formulations are needed to protect drugs from degradation in the stomach and ensure release in the intestine.

Purpose of the Study:

• To develop gastroresistant microparticles for oral administration of hesperidin (Hd) using spray-drying.
• To evaluate the effect of cellulose acetate phthalate (CAP) enteric polymer and dissolution enhancers on Hd release.
• To optimize the formulation for improved dissolution and complete intestinal release of Hd.

Main Methods:

• Microparticles were produced by spray-drying using CAP as the enteric polymer at various ratios (1:1, 3:1, 5:1) with Hd.
• Dissolution enhancers including sodium carboxymethylcellulose crosslinked (CMC), sodium dodecylbenzene sulfonate (SDBS), and Tween85 were incorporated.
• Characterization involved differential-scanning calorimetry, X-ray diffraction, infrared spectroscopy, scanning electron microscopy, and fluorescence microscopy.
• In vitro dissolution tests were performed using a pH-change method to assess gastroresistance and intestinal release.

Main Results:

• Spray-dried CAP/Hd microparticles exhibited good gastroresistance but incomplete dissolution in simulated intestinal fluid (SIF).
• Incorporation of enhancers (CMC, SDBS, Tween85) resulted in well-formed microparticles with improved Hd dissolution rates in SIF.
• Enhancers increased dissolution without affecting the protective nature of CAP in acidic conditions.
• The spray-drying process ensured satisfactory encapsulation efficiency, product yield, and microparticle morphology, leading to complete drug release.

Conclusions:

• Spray-drying is an effective technique for producing gastroresistant microparticles of hesperidin (Hd).
• Dissolution enhancers significantly improve the intestinal release rate of Hd from CAP microparticles.
• The developed formulation ensures gastroprotection and complete drug release in the intestine, enhancing oral bioavailability potential.