Preparation and characterization of genistein containing poly(ethylene glycol) microparticles

Abstract

ABSTRACT:The purpose of this study was to prepare, characterize, and evaluate genistein-containing microparticles with enhanced dissolution profile using poly(ethylene glycol) (PEG) as polymer matrix. Genistein loaded microparticles were prepared by a solvent evaporation process and their surface, thermal, chemical, and dissolution properties were analyzed by microscopy, differential scanning calorimetry, ATR-FTIR spectroscopy, and USP dissolution apparatus II, respectively. The wettability index was also determined. Genistein exhibited an elongated crystal habit. However, the drug containing PEG microparticles were discrete and quasispherical. The ATR-FTIR studies performed on the formulation suggested hydrogen bonding between the drug and the polymer matrix. Thermal analysis indicated a conversion of the crystalline form of the drug to an amorphous form. Genistein, exhibiting low solubility and high permeability, is a Class II drug of the Biopharmaceutical Classification Scheme. However, there was a ϳ9-fold increase in the rate of dissolution of genistein in the case of all formulations as compared to native genistein. This study showed that genistein could be effectively encapsulated into PEG microparticles using an emulsion-solvent evaporation technique, therefore avoiding the potential disadvantages of other solid dispersion techniques. This approach provided a significant enhancement in the drug dissolution profile.

Genistein and Cancer: Current Status, Challenges, and Future Directions

“…Several studies, however, indicated that the oral bioavailability of genistin is higher than that of genistein (73). The limitation of genistein bioavailability after oral administration is generally due to its poor water solubility (74). Genistein also has a bitter taste (75), and formulations to overcome both the limitation of bioavailability and acceptable taste are necessary.…”

Peningkatan Laju Disolusi Dispersi Padat Amorf Genistein dengan PVP K-30

“…Kelarutan genistein yang rendah dalam air, membatasi penggunaan secara klinis. Beberapa studi terdahulu untuk meningkatkan kelarutan dan laju disolusi genistein telah dilaporkan, diantaranya; pembuatan nanopartikel dan mikropartikel dengan polimer hidrofilik, pembuatan kompleks inklusi dan formulasi polimerik misel [10,11,12,13]. Tujuan dari penelitian ini, adalah memperbaiki laju disolusi genistein dengan teknik sistem dispersi padat menggunakan polimer hidrofilik PVP K-30 dan melakukan karakterisasi sistem dispersi padat yang terbentuk dengan analisa difraksi sinar-X, analisa termal DSC, analisa spektroskopi FT-IR dan analisa mikroskopik SEM.…”

“…Genistein menunjukkan beberapa puncak puncak transmitan yang khas, terutama pada bilangan gelombang 3400 dan 3100 cm -1 , yang mengambarkan getaran regangan gugus OH dan CH. Perubahan pita bilangan geombang pada daerah bilangan gelombang 3100 -3400 cm -1 pada sistem dispersi padat genistein -PVP K-30 mengindikasikan terjadinya deformasi gugus OH pada genistein karena terbentuknya ikatan hidrogen antara genistein dan polimer PVP K-3 [10].…”

An Overview on Genistein and its Various Formulations

“…Several studies, however, indicated that the oral bioavailability of genistin is higher than that of genistein [45]. The limitation of genistein bioavailability after oral administration is generally due to its poor water solubility [37,46]. Genistein also has a bitter taste [47], and formulations to overcome both the limitation of bioavailability and acceptable taste are necessary.…”