Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

Shi-lin, MA; Chen, Fen; Ye, Xiaohui; Dong, Yifei; Xue, Yingna; Xu, Heming; Zhang, Wenji; Song, Shuangshuang; Ai, Li; Naixian, Zhang; Pan, Wei-San

doi:10.2147/ijn.s47956

Cited by 23 publications

(16 citation statements)

References 35 publications

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“…OA has also attracted much attention in the “Mediterranean diet”, characterized by a high olive oil (rich in OA) consumption 7 . BJO or OA has shown anticancer effects in many types of cancers, such as prostate, breast and colorectal cancer, and OA is commonly administered in combination with chemotherapy 6 , 8 – 11 .…”

Section: Introductionmentioning

confidence: 99%

Oleic acid induces apoptosis and autophagy in the treatment of Tongue Squamous cell carcinomas

Jiang

Wang

et al. 2017

Sci Rep

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Oleic acid (OA), a main ingredient of Brucea javanica oil (BJO), is widely known to have anticancer effects in many tumors. In this study, we investigated the anticancer effect of OA and its mechanism in tongue squamous cell carcinoma (TSCC). We found that OA effectively inhibited TSCC cell proliferation in a dose- and time-dependent manner. OA treatment in TSCC significantly induced cell cycle G0/G1 arrest, increased the proportion of apoptotic cells, decreased the expression of CyclinD1 and Bcl-2, and increased the expression of p53 and cleaved caspase-3. OA also obviously induced the formation of autolysosomes and decreased the expression of p62 and the ratio of LC3 I/LC3 II. The expression of p-Akt, p-mTOR, p-S6K, p-4E-BP1 and p-ERK1/2 was significantly decreased in TSCC cells after treatment with OA. Moreover, tumor growth was significantly inhibited after OA treatment in a xenograft mouse model. The above results indicate that OA has a potent anticancer effect in TSCC by inducing apoptosis and autophagy via blocking the Akt/mTOR pathway. Thus, OA is a potential TSCC drug that is worthy of further research and development.

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Section: Introductionmentioning

confidence: 99%

Oleic acid induces apoptosis and autophagy in the treatment of Tongue Squamous cell carcinomas

Jiang

Wang

et al. 2017

Sci Rep

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“…Measurement of zeta potential is important to predict the long term stability of formulations as well as to understand the state of the surface of the nanoparticles [ 37 ]. This parameter is not only responsible for the stability of colloidal dispersions but it provides an indication of the degree of repulsion between particles with identical charge in the dispersion [ 38 ].…”

Section: Resultsmentioning

confidence: 99%

An Artificial Neural Network Based Analysis of Factors Controlling Particle Size in a Virgin Coconut Oil-Based Nanoemulsion System Containing Copper Peptide

et al. 2016

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A predictive model of a virgin coconut oil (VCO) nanoemulsion system for the topical delivery of copper peptide (an anti-aging compound) was developed using an artificial neural network (ANN) to investigate the factors that influence particle size. Four independent variables including the amount of VCO, Tween 80: Pluronic F68 (T80:PF68), xanthan gum and water were the inputs whereas particle size was taken as the response for the trained network. Genetic algorithms (GA) were used to model the data which were divided into training sets, testing sets and validation sets. The model obtained indicated the high quality performance of the neural network and its capability to identify the critical composition factors for the VCO nanoemulsion. The main factor controlling the particle size was found out to be xanthan gum (28.56%) followed by T80:PF68 (26.9%), VCO (22.8%) and water (21.74%). The formulation containing copper peptide was then successfully prepared using optimum conditions and particle sizes of 120.7 nm were obtained. The final formulation exhibited a zeta potential lower than -25 mV and showed good physical stability towards centrifugation test, freeze-thaw cycle test and storage at temperature 25°C and 45°C.

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“…Particle size, zeta potential and encapsulation efficiency are the properties that influence the biopharmaceutical characteristics and stability of a liposomes. The smaller liposomes can more easily evade the reticuloendothelial system (RES) and prolong the time in circulation [7, 32, 33]. It has been reported that particle size of the drug carrier should be bigger than 10 nm to escape the first-pass elimination by the kidney [34–36], while with particle size less than 200 nm could increase drug accumulation in the tumor via “enhanced permeability and retention (EPR)” effect [25, 37–40].…”

Section: Discussionmentioning

confidence: 99%

“…The treatment of ovarian cancer usually involves debulking surgery and chemotherapy [5, 6]. Seed oil of Brucea javanica (BJO), a traditional herbal medicine, is extracted from the seeds of Brucea javanica [7], and has been used clinically to treat various tumors, including ovarian cancer [7–9]. The mechanisms of antitumor activity of BJO include inducing tumor apoptosis and reversing multidrug resistance [10, 11].…”

Section: Introductionmentioning

confidence: 99%

Enhanced therapeutic efficacy of LHRHa-targeted brucea javanica oil liposomes for ovarian cancer

Liu

Sun

et al. 2016

BMC Cancer

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BackgroundAlthough brucea javanica oil liposomes (BJOLs) have been used clinically to treat ovarian cancer, its clinical efficacy is often limited by systemic side effects due to non-specific distribution. Luteinizing hormone releasing hormone receptor (LHRHR) is overexpressed in most ovarian cancers but negligibly expressed in most of the other visceral organs. In this study, we aimed to develop a novel LHRHa targeted and BJO-loaded liposomes (LHRHa-BJOLs), and investigate its characteristics, targeting ability and anti-ovarian cancer efficiency both in vitro and in vivo.MethodsThe LHRHa-BJOLs were prepared by film-dispersion and biotin-streptavidin linkage methods, and characterized in terms of its morphology, particle size, zeta potential, ligand conjugation, encapsulation efficiency and stability. The targeting nature and antitumor effects of the liposomes were evaluated in vitro using cultured human ovarian cancer A2780/DDP cells, and in vivo using ovarian cancer-bearing nude mice.ResultsThe LHRHa-BJOLs were successfully synthesized, with a uniformly spherical shape, appropriate particle size and zeta potential, as well as a high encapsulation efficiency. Compared to non-targeted liposomes and BJO emulsion, the LHRHa-BJOLs could significantly increase specific intracellular uptaking rate, enhance cell inhibitory effect and induce cell apoptosis in A2780/DDP cells in vitro. Meanwhile, LHRHa-BJOLs also had a significantly stronger activity of targeting tumor tissue, inhibiting tumor growth, inducing tumor apoptosis and prolonging survival time in ovarian cancer-bearing mice in vivo.ConclusionsOur experiment suggests that LHRHa-BJOLs may be a useful targeted drug for the treatment of ovarian cancer.

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Intravenous microemulsion of docetaxel containing an anti-tumor synergistic ingredient (Brucea javanica oil): formulation and pharmacokinetics

Cited by 23 publications

References 35 publications

Oleic acid induces apoptosis and autophagy in the treatment of Tongue Squamous cell carcinomas

Oleic acid induces apoptosis and autophagy in the treatment of Tongue Squamous cell carcinomas

An Artificial Neural Network Based Analysis of Factors Controlling Particle Size in a Virgin Coconut Oil-Based Nanoemulsion System Containing Copper Peptide

Enhanced therapeutic efficacy of LHRHa-targeted brucea javanica oil liposomes for ovarian cancer

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