Development of intravenous lipid emulsion of tanshinone IIA and evaluation of its anti-hepatoma activity in vitro

Chu, Ting; Zhang, Qing; Li, Hui; Ma, Wei-Cong; Zhang, Na; Jin, Hui; Mao, Shengjun

doi:10.1016/j.ijpharm.2011.12.049

Cited by 40 publications

(17 citation statements)

References 44 publications

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“…However, the clinical application of TAN for anticancer therapy is hindered by its low water-solubility, poor cellular uptake , short half-life, and first pass metabolism (Zhang et al, 2012b;Yu et al, 2007). Many colloidal carriers including polymeric micelles (Wang et al, 2014), emulsions (Chu et al, 2012), micro-emulsions (Ma et al, 2013), and nanoparticles have been used to improve the solubility of TAN. However, the cytotoxicity and bioavailability of TAN still need to be improved.…”

Section: Introductionmentioning

confidence: 99%

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Zhang

Fang

et al. 2014

International Journal of Pharmaceutics

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Section: Introductionmentioning

confidence: 99%

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Zhang

Fang

et al. 2014

International Journal of Pharmaceutics

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“…Uniform droplet size and high drug encapsulation efficiency have been obtained by permeating a dispersed phase into a continuous phase through an SPG membrane at an adequate pressure [10][11][12][13][14]. …”

Section: Research Articlementioning

confidence: 99%

Optimization and Evaluation of Monodispersed Tetrandrine- Loaded PLA Microspheres Prepared With A SPG Membrane Emulsification Technique

Jin¹,

Yin²,

Zhang³

et al. 2017

SOJPPS

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Research articlewidely in vivo without a targeting effect, thus tetrandrine in this formulation does not concentrate highly in diseased organs or tissues [6][7] and usually causes pain or phlebitis. To improve pulmonary drug concentration to maximize its effectiveness and minimize the adverse side effects, tetrandrine polylactic acid microspheres with diameters of 7-15 μm were injected intravenously to achieve lung targeting [8]. This mechanism of lung targeting by injecting more than 7 μm microspheres occurs through mechanical filtration by the pulmonary capillaries, which can damage the lung permanently. Microspheres with diameters between 0.5-5 μm used for pulmonary inhalation could overcome this shortcoming. However, the controllability and uniformity of the microsphere size are closely related to the effects of pulmonary inhalation. The particle size is difficult to control for microspheres prepared by conventional methods, such as emulsification, ultrasonic emulsifying preparation and distribution [9].Recently, a novel method, the Shirasu Porous Glass (SPG) membrane emulsification technique, has been widely applied to the preparation of uniform-sized emulsions. Uniform droplet size and high drug encapsulation efficiency have been obtained by permeating a dispersed phase into a continuous phase through an SPG membrane at an adequate pressure [10][11][12][13][14]. Optimization and Evaluation of Monodispersed AbstractTo improve pulmonary drug concentrations and to maximize the effectiveness and minimize the adverse side effects, uniformsized tetrandrine-loaded polylactide (PLA) microspheres with a suitable particle size for pulmonary inhalation were prepared by the Shirasu Porous Glass (SPG) membrane emulsification technique. The main parameters influencing PLA microsphere properties were investigated: transmembrane pressure, circulation speed, high hydrophilic-lipophilic balance (HLB value), PLA concentration and oil-water volume ratio. Narrowly size-distributed tetrandrine-loaded PLA microspheres were obtained with a high drug encapsulation efficiency of 81.0% and an average diameter of 3.16 μm under optimized conditions. The results of Fourier transform infrared, differential scanning calorimetry and powder X-ray diffraction revealed that tetrandrine would be either molecularly dispersed in the polymer or distributed in an amorphous form. Further, the in vitro drug release experiment confirmed that the uniform-sized tetrandrine-loaded PLA microspheres showed suppressed burst release. These studies provide a basis for the use of uniformly sized 3.16 μm tetrandrine-loaded PLA microspheres for pulmonary inhalation.

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“…Emulsions are a class of formulation consisting of two immiscible phases stabilized by a surfactant 86 and are widely used to enhance the stability of active constituents, thereby maintaining their effectiveness. 87 In previous studies, lipid emulsions, 88 microemulsions, 89 and nanoemulsions 90 of soybean phospholipid, pluronic F68 (F68), glycerol, oleic acid, lecithin, and so on were used to produce TNIIA formulations with long-term stability and obvious anticancer activity.…”

Section: Emulsionsmentioning

confidence: 99%

Recent insights into the biological activities and drug delivery systems of tanshinones

Cai¹,

Zhang²,

Chen³

et al. 2016

IJN

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Tanshinones, the major lipid-soluble pharmacological constituents of the Chinese medicinal herb Tanshen ( Salvia miltiorrhiza ), have attracted growing scientific attention because of the prospective biomedical applications of these compounds. Numerous pharmacological activities, including anti-inflammatory, anticancer, and cardio-cerebrovascular protection activities, are exhibited by the three primary bioactive constituents among the tanshinones, ie, tanshinone I (TNI), tanshinone IIA (TNIIA), and cryptotanshinone (CPT). However, due to their poor solubility and low dissolution rate, the clinical applications of TNI, TNIIA, and CPT are limited. To solve these problems, many studies have focused on loading tanshinones into liposomes, nanoparticles, microemulsions, cyclodextrin inclusions, solid dispersions, and so on. In this review, we aim to offer an updated summary of the biological activities and drug delivery systems of tanshinones to provide a reference for these constituents in clinical applications.

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Development of intravenous lipid emulsion of tanshinone IIA and evaluation of its anti-hepatoma activity in vitro

Cited by 40 publications

References 44 publications

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Optimization and Evaluation of Monodispersed Tetrandrine- Loaded PLA Microspheres Prepared With A SPG Membrane Emulsification Technique

Recent insights into the biological activities and drug delivery systems of tanshinones

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Development of intravenous lipid emulsion of tanshinone IIA and evaluation of its anti-hepatoma activity in vitro

Cited by 40 publications

References 44 publications

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

TPGS-g-PLGA/Pluronic F68 mixed micelles for tanshinone IIA delivery in cancer therapy

Optimization and Evaluation of Monodispersed Tetrandrine- Loaded PLA Microspheres Prepared With A SPG Membrane Emulsification Technique

Recent insights into the biological activities and&nbsp;drug delivery systems of tanshinones

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Recent insights into the biological activities and drug delivery systems of tanshinones