Long-circulating nanoliposomes (LCNs) sustained delivery of baicalein (BAI) with desired oral bioavailabilityin vivo

Abstract

Long-circulating nanoliposomes (LCNs) containing Baicalein (BAI) were prepared by diethyl ether injection method in this paper. Using soybean phosphatidylcholine (SPC) and cholesterol (CHOL) as the carrier ingredients, BAI-loaded LCNs were formulated in optimized condition with encapsulation efficiency (EE) of 41.5 AE 4.77%. The average diameter of BAI-loaded LCNs was $709 nm determined by dynamic light scattering (PDI 0.43). Drug storage stability study showed that BAI-loaded LCNs were highly stable in phosphate-buffered saline (PBS, pH 7.4) at 4 C. Additionally, the pharmacokinetic behaviors of BAI-loaded LCNs were studied using Kunming mice as experimental animals. Parallelly, free BAI solution was studied as control. As expected, it is found that LCNs-encapsulated BAI yields greater BAI oral bioavailability with 4.52 times of free BAI. These results suggest the potential applications of LCNs for the delivery of BAI.

Effects of stabilizing agents on the development of myricetin nanosuspension and its characterization: An in vitro and in vivo evaluation

“…Gaur et al (2014) reported that a solid lipid nanoparticle formulation of efavirenz showed mean particle size of 124 AE 3.2 nm and exhibited 10.98-fold increase in area under the concentration-time curve (AUC) in comparison to efavirenz suspension. The plasma level of baicalein, when administering its long-circulating nanoliposomes with an approximately 700 nm particle size, was significantly improved, and the relative bioavailability of baicalein was 452% in mice (Liang et al, 2013). Similarly, the aqueous solubility of kaempferol was increased approximately 139-fold when it was developed into a nanoparticle system, which resulted in a significant improvement in antioxidant activity (p < 0.05) compared with the pure drug (Tzeng et al, 2011).…”

Anticancer properties of baicalein: a review

“…Its Cmax was much higher and half-life was much longer than free baicalein (Ts a i et al 2012; Zhang et al 2011a). Complexation with delivery systems could enhance the solubility and dissolution of baicalein (Huang et al 2014; Liang et al 2013; Liu et al. 2006; Liu et al 2012; Zhang et al 2014a).…”

Preparation and Characterization of Baicalein-Loaded Nanoliposomes for Antitumor Therapy

“…The results of DLS analysis were presented in Figure 2. method [14]. The PDI was determined to examine the level of uniformity of particle size.…”

“…BAI, a major constituent of Scutellaria baicalensis Georgi, has a variety of pharmacological effects such as antivirus, antibacterial, and anticancer [13]. According to previous studies, BAI is a very promising and attractive drug in treatment of bladder cancer [14]. Our research group has conducted years of researches on anticancer effects and mechanisms of BAI.…”