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In this study, we developed an optimized formulation of a breviscapine lipid emulsion (BLE) and evaluated the physicochemical properties and in vivo pharmacokinetics of BLE in rats. For the preparation of the lipid emulsion, soybean oil and oleic acid were used as the oil phase, lecithin and poloxamer 188 as surfactants and glycerol as co-surfactant. An optimized formulation consisting of soybean oil (10.0%), oleic acid (0.9%), lecithin (1.5%), poloxamer 188 (0.4%), and glycerol (2.25%) was selected. The results showed that the average particle size, polydispersity index, and zeta potential of the optimized formulation were 183.5 ± 5.5 nm, 0.098 ± 0.046, and -35.0 ± 2.5 mV, respectively. The BLE was stable for at least three month at room temperature. After a single intravenous dose of 4 mg/kg to rats, the AUC of scutellarin from the lipid emulsion was about 1.5-fold higher than that of the commercial product (breviscapine injection). In conclusion, the optimized formulation of BLE showed positive results over the commercial product in terms of the physicochemical properties and pharmacokinetics of BLE in rats.

To formulate a self-nanoemulsifying drug delivery system (SNEDDS) for the oral administration of docetaxel as an alternative to commercial docetaxel-loaded injectable products, it was prepared by spray-drying an aqueous solution containing liquid SNEDDS and colloidal silica. Its physicochemical properties and oral bioavailability were investigated compared to a clear docetaxel solution administered intravenously or orally to rats. In the docetaxel-loaded solid SNEDDS prepared with colloidal silica, the liquid SNEDDS composed of Capryol 90, Cremophore EL and Transcutol HP (45/35/20, volume ratio) was absorbed inside the pores of carriers, and docetaxel was present in a changed amorphous state. The solid SNEDDS with 3.3% (w/v) docetaxel produced nanoemulsions, and showed about 12.5% absolute bioavailability in rats. Thus, this solid SNEDDS may be a potential candidate for oral pharmaceutical product with improved oral bioavailability of docetaxel.

The main purpose of our study is to optimize the formulation for Ginkgolide B (GB) solid dispersion in order to improve its dissolution in water. For the preparation of GB solid dispersion, we use a solvent method. The optimized formulation consists of GB : PVPK30 = 1:10, PVPK30 as the carrier, and ethanol : dichloromethane = 1:1 as the solvent. They were treated ultrasonically for 10 min at 60°C. The results from scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and particle size analysis show that the morphological appearance of GB changed significantly in solid dispersion. The original crystal form of GB no longer existed, but it was uniformly dispersed within PVPK30 in a non-crystalline form. It is probably because the -C=O in GB forms hydrogen bonds with the -OH of PVPK30 or urea; this produces a nice solid dispersion and significantly improves the dissolution of GB in water. When GB is in a solid dispersion system, GB’s dissolution in water could be enhanced from 30% to 80%. Furthermore, it may even be produced as a solid agent.