The comparison of different daidzein-PLGA nanoparticles in increasing its oral bioavailability

Abstract

Abstract:The aim of this research was to increase the oral bioavailability of daidzein by the formulations of poly(lactic-co-glycolic) acid (PLGA) nanoparticles loaded with daidzein. Amongst the various traditional and novel techniques of preparing daidzein-loaded PLGA nanoparticles, daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were selected. The average drug entrapment efficiency, particle size, and zeta potential of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles were 81.9% ± 5%, 309.2 ± 14.0 nm, −32.14 ± 2.53 mV and 83.2% ± 7.2%, 323.2 ± 4.8 nm, −18.73 ± 1.68 mV, respectively. The morphological characterization of nanoparticles was observed with scanning electron microscopy by stereological method and the physicochemical state of nanoparticles was valued by differential scanning calorimetry. The in vitro drug-release profile of both nanoparticle formulations fitted the Weibull dynamic equation. Pharmacokinetic studies demonstrated that after oral administration of daidzein-loaded phospholipid complexes PLGA nanoparticles and daidzein-loaded cyclodextrin inclusion complexes PLGA nanoparticles to rats at a dose of 10 mg/kg, relative bioavailability was enhanced about 5.57-and 8.85-fold, respectively, compared to daidzein suspension as control. These results describe an effective strategy for oral delivery of daidzein-loaded PLGA nanoparticles and might provide a fresh approach to enhancing the bioavailability of drugs with poor lipophilic and poor hydrophilic properties.

Manufacturing Different Types of Solid Dispersions of BCS Class IV Polyphenol (Daidzein) by Spray Drying: Formulation and Bioavailability

“…Several studies have shown the biological effects of DZ, making it a promising compound for the treatment of several diseases [21]. Nevertheless, DZ is a BCS class IV polyphenol, with low aqueous solubility and low permeability, thus limiting its oral bioavailability.…”

“…Considering this, solubility tests were carried out with several polymers, surfactants, and alkalizers. The aim was to study and select the excipients by using a simple and effective approach, which is based on individual capability of dissolving the drug to obtain different generations of SDs [13,21,23].…”

“…Many efforts have been made to manufacture solid dosage forms with high bioavailability by changing the solid state [31]. The obtained F10 formulations by spray-drying technique also provided a higher Cmax and lower Tmax compared with DZ-loaded phospholipid complex polymeric nanoparticles and DZ-loaded cyclodextrin inclusion complex polymeric nanoparticles at the same dose [21,22]. The in vivo pharmacokinetic data have shown that the accelerated initial DZ release that was achieved by the spray drying technique and incorporation of excipients into SDs dramatically improved the extent of oral DZ absorption.…”

Design and evaluation of a novel nanodrug delivery system for reducing the side effects of clomiphene citrate on endometrium

“…Foroughi et al showed the reduced side effects of tamoxifen on endometrium when tamoxifen was loaded in palm oil lipids (S154), and soy lecithin (S100) [36]. Saesoo et al showed the reduced side effects of cisplatin (cisdiamminedichloroplatinum) during a cervical usage when the cisplatin was loaded in palm oil lipids (S154), and soy lecithin (S100) [37,38]. These lipoids include increasing the targeted effects of drugs and reducing their negative effects in non-target tissues [39,40].…”

A sensitive, high‐throughput, and eco‐friendly analysis of daidzein and its valine carbamate prodrug in rat plasma by supercritical fluid chromatography with tandem mass spectrometry

“…Daidzein, 4,7‐dihydroxyl isoflavone (Figure A), mainly exists in leguminous plants . Currently, this drug is marketed as tablets and capsules and has been widely applied in clinical therapy for cardiovascular disease, hypertension, coronary heart disease, and women menopausal syndrome .…”