Hesperidin Gastroresistant Microparticles by Spray-Drying: Preparation, Characterization, and Dissolution Profiles |
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Authors: | Francesca Sansone Alessandra Rossi Pasquale Del Gaudio Francesco De Simone Rita Patrizia Aquino Maria Rosaria Lauro |
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Institution: | (1) Dipartimento di Scienze Farmaceutiche, Università degli Studi di Salerno, Via Ponte Don Melillo, 84084 Ficiano, SA, Italy;(2) Dipartimento Farmaceutico, Università degli Studi di Parma, V.le G. P. Usberti 27/A, 43100 Parma, Italy |
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Abstract: | Gastroresistant microparticles for oral administration of hesperidin (Hd) were produced by spray-drying using cellulose acetate
phthalate (CAP) as enteric polymer in different polymer/Hd weight ratio (1:1, 3:1, and 5:1), and a series of enhancers of
the dissolution rate, such as sodium carboxymethylcellulose crosslinked (CMC), sodium dodecylbenzene sulfonate (SDBS), or
Tween85. The raw materials and the microparticles were investigated by differential-scanning calorimetry, X-ray diffraction,
infrared spectroscopy and imaged using scanning electron and fluorescence microscopy. In vitro dissolution tests were conducted using a pH-change method to investigate the influence of formulative parameters on the dissolution/release
properties of the drug. CAP/Hd microparticles showed a good gastro-resistance but incomplete drug dissolution in the simulated
intestinal fluid (SIF). The presence of the enhancers in the formulation produced well-formed microparticles with different
size and morphology, containing the drug well coated by the polymer. All the enhancers were able to increase the dissolution
rate of Hd in the simulated intestinal environment without altering CAP ability to protect Hd in the acidic fluid. The spray-drying
technique and process conditions selected were effective in microencapsulating and stabilizing the flavonoid giving satisfactory
encapsulation efficiency, product yield, and microparticles morphology, and a complete drug release in the intestine. |
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Keywords: | enhancers of the dissolution rate gastroresistant spray-dried microparticles hesperidin morphological and physicochemical characterization |
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