YuJun Wang

Sichuan University, Chengdu, Sichuan Sheng, China

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Publications (23)

  • YuJun Wang · LiJuan Chen · LiWei Tan · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: In this study, a composite drug delivery system was developed and evaluated for oral delivery of docetaxel: docetaxel-loaded micelles in pH-responsive hydrogel (DTX-micelle-hydrogel). Docetaxel was successfully loaded in micelles with small particle size of 20 nm and high drug loading of 7.76%, which contributed to the drug absorption in the intestinal tract. The experiments of cytotoxicity on 4T1 cells demonstrated the effective antitumor activity of DTX micelles. Meanwhile, a pH-responsive hydrogel was synthesized and optimized for incorporating the docetaxel micelles. The pH-responsiveness and reversibility of the hydrogel were investigated under the pH conditions of the gastrointestinal tract. Furthermore, the DTX-micelle-hydrogel system showed much quicker diffusion of micelles in simulated intestinal fluid than in simulated gastric fluid, which was mainly caused by the change of pH value. The docetaxel released from the micelle-hydrogel system quite slowly, so it had little influence on the absorption of DTX micelles in small intestine. More important, the pharmacokinetic study revealed that the DTX-micelle-hydrogel significantly improved the oral bioavailability of docetaxel (75.6%) about 10 times compared to DTX micelles, and this increase in bioavailability was probably due to the small intestine targeting release of the pH-responsive hydrogel. Consequently, the oral DTX-micelle-hydrogel system was effective in inhibiting tumor growth in subcutaneous 4T1 breast cancer model, and decreased systemic toxicity compared with intravenous treatment. The apoptosis cells in the immunofluorescent studies and the proliferation-positive cells in the immunohistochemical studies were also consistent with the results. Therefore, the DTX-micelle-hydrogel system might be a promising candidate oral drug for breast cancer therapy.
    Article · May 2014 · Biomaterials
  • YuJun Wang · MaLing Gou · ChangYang Gong · [...] · Bartsev S.I.
    Article · Aug 2013
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    Changyang Gong · Qinjie Wu · Yujun Wang · [...] · Zhiyong Qian
    [Show abstract] [Hide abstract] ABSTRACT: A biodegradable in situ gel-forming controlled drug delivery system composed of curcumin loaded micelles and thermosensitive hydrogel was prepared and applied for cutaneous wound repair. Curcumin is believed to be a potent antioxidant and anti-inflammatory agent. Due to its high hydrophobicity, curcumin was encapsulated in polymeric micelles (Cur-M) with high drug loading and encapsulation efficiency. Cur-M loaded thermosensitive hydrogel (Cur-M-H) was prepared and applied as wound dressing to enhance the cutaneous wound healing. Cur-M-H was a free-flowing sol at ambient temperature and instantly converted into a non-flowing gel at body temperature. In vitro studies suggested that Cur-M-H exhibited well tissue adhesiveness and could release curcumin in an extended period. Furthermore, linear incision and full-thickness excision wound models were employed to evaluate the in vivo wound healing activity of Cur-M-H. In incision model, Cur-M-H-treated group showed higher tensile strength and thicker epidermis. In excision model, Cur-M-H group exhibited enhancement of wound closure. Besides, in both models, Cur-M-H-treated groups showed higher collagen content, better granulation, higher wound maturity, dramatic decrease in superoxide dismutase, and slight increase in catalase. Histopathologic examination also implied that Cur-M-H could enhance cutaneous wound repair. In conclusion, biodegradable Cur-M-H composite might have great application for wound healing.
    Full-text Article · May 2013 · Biomaterials
  • [Show abstract] [Hide abstract] ABSTRACT: In this paper, we successfully synthesized amino-terminated poly(ethylene glycol)-block-poly (epsilon-caprolactone) (NH2-PEG-PCL) block copolymer from polyethylene glycol 2000, epsilon-caprolactone (epsilon-CL) and hydrazine hydrate. The obtained copolymer was characterized by nuclear magnetic resonance (1H-NMR), the molecular weight and distribution of NH2-PEG-PCL were characterized by Gel permeation chromatography (GPC). The NH2-PEG-PCL copolymer could self-assemble into micelles in water. Paclitaxel (PTX) loaded NH2-PEG-PCL (PNPP) micelles were prepared by solid dispersion technique without organic solvent. The micelles were characterized by XRD, TEM and Malvern laser particle size. The results of this work indicated that PNPP micelles were uniform and spherical shapes in solution. The average size and zeta potential of PNPP (DL = 8%) in water was about 97.1 +/- 1.2 nm, +13.9 +/- 0.6 mV, respectively. The in vitrodrug release profile of PNPP micelles showed a clear slow-release effect. The results suggested that NH2-PEG-PCL copolymer might be an excellent carrier for hydrophobic drugs such as PTX. In particular, the NH2-PEG-PCL polymer has potential value for modifying with ligands to work as active targeting drug delivery carriers, which has great significance for cancer therapeutics.
    Article · May 2013 · Journal of Nanoscience and Nanotechnology
  • [Show abstract] [Hide abstract] ABSTRACT: In this paper, two nanoscale preparations were described for docetaxel encapsulation using poly(epsilon-caprolactone)poly(ethylene glycol)-poly(epsilon-caprolactone) (PCEC) copolymer as carrier for treating malignant tumor. The first formulation was docetaxel-loaded PCEC micelle (D-M), which was characterized by XRD, TEM and Malvern laser particle size and drug release studies. The highest drug-loading of docetaxel in micelle was about 22.1 +/- 1.9%, optimized average diameter and polydispersity index was 25.2 +/- 1.1 nm, 0.13 +/- 0.12, respectively. Another formulation was docetaxel-loaded PCEC thermosensitive hydrogel (D-H), which displayed special gel-sol transition behavior with body temperature. We studied the cytotoxicity and in vitro hemolytic test of blank PCEC copolymer, the result was superiority. The data of relative body weight (RW), relative tumor volume (RV) and micrographs of hematoxylin and eosin (H&E)-stained histological sections showed D-M and D-H had significant antitumor effect and exhibited different characteristics of antitumor activity. Thus, the experiments signified that the combination therapy of intravenous (i.v.) and intratumoral administration using the two formulations maybe an effective way to treat malignant tumor.
    Article · Mar 2013 · Journal of Biomedical Nanotechnology
  • Yingjing Wang · Cheng Wang · Yujun Wang · [...] · Zhiyong Qian
    [Show abstract] [Hide abstract] ABSTRACT: As a traditional immunosuppressive drug, tacrolimus showed the potency in treating ulcerative colitis. In this study, a novel drug delivery vehicle achieved by self-assembly was applied to tacrolimus. During the preparation, amphiphilic copolymer MPEG-PCL was chosen to form the unique core-shell structure, and tacrolimus was loaded into the hydrophobic core due to its great hydrophobicity. After several relevant tests, MPEG-PCL (2000-2000) was selected to be the most suitable and safest copolymer for drug carrier. For the tacrolimus loaded MPEG-PCL (2000-2000) micelles, the mean particle size and drug entrapment efficiency were ca. 25 +/- 5 nm and 98.47 +/- 0.43% respectively. The micelles could be stored for quite a long time even at room temperature after freeze-drying, and the freeze-drying process didn't affect the monodispersity of micelles. Transmission electron microscope (TEM) image emerged the spherical shape of micelles. Both Differential Scanning Calorimetric (DSC) and X-ray Diffractometer (XRD) assays demonstrated that tacrolimus was relatively completely incorporated into the core-shell structure. In vitro release profiles showed the apparent sustained release behavior compared with tacrolimus solution. Above all, animal treatment showed the most satisfactory therapeutic effect of tacrolimus loaded micelles, which means the micelles possess the ability to treat ulcerative colitis induced by dextran sulfate sodium (DSS) in mice. Therefore, micelles of MPEG-PCL could be a very promising novel vehicle for tacrolimus.
    Article · Feb 2013 · Journal of Biomedical Nanotechnology
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    [Show abstract] [Hide abstract] ABSTRACT: Nanoscale polymeric micelles have promising applications as drug delivery systems (DDS). In this work, to improve the anti-tumor activity and eliminate toxicity of the commercial formulation (cremophor EL and ethanol) of paclitaxel (PTX), we developed biodegradable poly(ethylene glycol)-poly(ε-caprolactone) (MPEG-PCL) micelles entrapping PTX by a simple one-step solid dispersion method, which is without any surfactants or additives and is easy to scale up. In addition, the PTX micelles could be lyophilized into powder without any adjuvant and the re-dissolved PTX micelles are stable and homogeneous. The prepared PTX micelles have a mean particle size of 38.06 ± 2.30 nm, a polydispersity index of 0.168 ± 0.014, a drug loading of 14.89 ± 0.06% and an encapsulation efficiency of 99.25 ± 0.38%. A molecular modeling study implied that PTX interacted with PCL as a core, which was embraced by PEG as a shell. The encapsulation of PTX in polymeric micelles enhanced its cytotoxicity by increasing the uptake by LL/2 cells. A sustained in vitro release behavior and slow extravasation behavior from blood vessels in a transgenic zebrafish model were observed in the PTX micelles. Furthermore, compared with Taxol®, the PTX micelles were more effective in suppressing tumor growth in the subcutaneous LL/2 tumor model. The PTX micelles also inhibited metastases in the pulmonary metastatic LL/2 tumor model and prolonged survival in both mouse models. Pharmacokinetic and tissue distribution studies showed that after PTX was encapsulated in polymeric micelles, the biodistribution pattern of PTX was altered and the PTX concentration in tumors was increased compared with Taxol® after intravenous injection. In conclusion, we have developed a polymeric micelles entrapping PTX that enhanced cytotoxicity in vitro and improved anti-tumor activity in vivo with low systemic toxicity on pulmonary carcinoma. The biodegradable MPEG-PCL micelles entrapping PTX may have promising applications in pulmonary carcinoma therapy.
    Full-text Article · Aug 2012 · Nanoscale
  • JinFeng Liao · Cheng Wang · YuJun Wang · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: Polymersomes are self-assembled spherical vesicles based on amphiphilic block copolymers. This review presents a summary of the achievements in the field of polymersome researches to date. Polymersomes have been applied as versatile drug carriers. Some polymersomes, which have well-known stimuli-responsibility, can release drugs in a controlled manner at the target site when they are given a specific stimulation such as pH, temperature, light, magnetic field, hydrogen bond actions, electrostatic force or ultrasound. The preparation methods of polymersomes are similar to that of liposomes, including the thin film rehydration technique, solvent method, direct dissolution, double emulsion in microfluidic device, and electroformation. In addition, biologically active ligands, such as antibodies, can be readily conjugated onto the exterior brush surface of polymersomes to target the vesicles or to provide a therapeutic response. Polymersomes offer superior advantages for future clinical therapeutic and diagnostic imaging applications.
    Article · May 2012 · Current pharmaceutical design
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    Yujun Wang · Cheng Wang · ChangYang Gong · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: In this article, polysorbate 80 coated poly (ɛ-caprolactone)-poly (ethylene glycol)-poly (ɛ-caprolactone) (PCEC) micelles were successfully prepared for paclitaxel (PTX) delivery. The particle size distribution, morphology, drug loading, encapsulation efficiency and sustained release profile of the micelles were studied in detail. The safety of the micelle formulation was evaluated by MTT assay on HEK293 cells. And the encapsulated PTX in the micelles remained potent antitumor effect on C6 glioma cells. The pharmacokinetic study showed that the PCEC micelles coated with polysorbate 80 altered the biodistribution pattern and increased PTX concentration in the brain significantly compared to the uncoated micelles and the free drug after intravenous injection. The results indicated that polysorbate 80 coated PCEC micelles might be a candidate for PTX delivery for brain tumor chemotherapy.
    Full-text Article · May 2012 · International Journal of Pharmaceutics
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    Changyang Gong · Cheng Wang · Yujun Wang · [...] · Zhiyong Qian
    [Show abstract] [Hide abstract] ABSTRACT: In this work, we aim to develop a dual drug delivery system (DDDS) of self-assembled micelles in thermosensitive hydrogel composite to deliver hydrophilic and hydrophobic drugs simultaneously for colorectal peritoneal carcinomatosis (CRPC) therapy. In our previous studies, we found that poly(ε-caprolactone)-poly(ethylene glycol)-poly(ε-caprolactone) (PCEC) copolymers with different molecular weight and PEG/PCL ratio could be administered to form micelles or thermosensitive hydrogels, respectively. Therefore, the DDDS was constructed from paclitaxel (PTX) encapsulated PCEC micelles (PTX-micelles) and a fluorouracil (Fu) loaded thermosensitive PCEC hydrogel (Fu-hydrogel). PTX-micelles were prepared by self-assembly of biodegradable PCEC copolymer (M(n) = 3700) and PTX without using any surfactants or excipients. Meanwhile, biodegradable and injectable thermosensitive Fu-hydrogel (M(n) = 3000) with a lower sol-gel transition temperature at around physiological temperature was also prepared. The obtained PTX-micelles in thermosensitive Fu-hydrogel (PTX-micelles-Fu-hydrogel) composite is a free-flowing sol at ambient temperature and rapidly turned into a non-flowing gel at physiological temperature. In addition, the results of cytotoxicity, hemolytic study, and acute toxicity evaluation suggested that the PTX-micelles-Fu-hydrogel was non-toxic and biocompatible. In vitro release behaviors of PTX-micelles-Fu-hydrogel indicated that both PTX and Fu have a sustained release behavior. Furthermore, intraperitoneal application of PTX-micelles-Fu-hydrogel effectively inhibited growth and metastasis of CT26 peritoneal carcinomatosis in vivo (p < 0.001), and induced a stronger antitumor effect than that of Taxol® plus Fu (p < 0.001). The pharmacokinetic study indicated that PTX-micelles-Fu-hydrogel significantly increased PTX and Fu concentration and residence time in peritoneal fluids compared with Taxol® plus Fu group. Thus, the results suggested the micelles-hydrogel DDDS may have great potential clinical applications.
    Full-text Article · Apr 2012 · Nanoscale
  • YuJun Wang · MaLing Gou · ChangYang Gong · [...] · Feng Luo
    [Show abstract] [Hide abstract] ABSTRACT: Micelles assembled from amphiphilic poly(ethylene glycol)/poly(-caprolactone) (PEG/PCL) copolymers are promised as safe and effective drug delivery systems. They offer the potential to achieve high solubility of hydrophobic drugs, long blood circulation time and effective delivery to target organs. These advantages contribute to their application as vehicles of a broad variation of therapeutic compounds. In this review, we discussed the safety of the copolymers, release behavior of PEG/PCL micelles in vitro, and pharmacokinetic profiles referring to the optimized fate in vascular system and targeting biodistribution.
    Article · Mar 2012 · Current Drug Metabolism
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    [Show abstract] [Hide abstract] ABSTRACT: The great potential of oridonin (ORI) for clinical application in cancer therapy is greatly limited due to its poor water-solubility. The purpose of this study was to increase the water solubility of oridonin using monomethoxy poly(ethylene glycol)-poly(epsilon-caprolactone) (MPEG-PCL) as drug carrier. The ORI-loaded MPEG-PCL micelles were prepared by thin film hydration method. The obtained ORI-micelles could be lyophilized into powder form, which could be re-dissolved in water to form homogeneous solution. This study showed that ORI was successfully incorporated in the core-shell structure of MPEG-PCL micelles and maintained its anticancer activity. The average particle size was 25.55 +/- 0.10 nm and the mean zeta potential was -4.71 +/- 0.05 mV. The actual drug loading and encapsulation efficiency were 7.99 +/- 0.03% and 99.51 +/- 0.34%, respectively. ORI could be released from MPEG-PCL micelles in a sustained manner in vitro. The permeation profiles of ORI from ORI-micelles and ORI water saturated solution through excised mouse skin demonstrated that ORI-micelles showed much better transdermal penetration performance than ORI water saturated solution. The prepared ORI-micelles have great potential for both direct intravascular administration and being further developed as a transdermal drug delivery system in cancer chemotherapy.
    Full-text Article · Feb 2012 · Journal of Biomedical Nanotechnology
  • [Show abstract] [Hide abstract] ABSTRACT: The two major concerns after cytoreductive surgery of abdominal and pelvic malignancies are residual tumors and peritoneal adhesions, which are inevitable and have great impact on prognosis. Therefore, to improve the intraperitoneal chemotherapeutic effect and prevent postsurgical adhesions simultaneously after surgery, we developed a novel strategy that combines the controlled drug delivery system (CDDS) with an antiadhesion barrier. Biodegradable poly(ethylene glycol)-poly(ɛ-caprolactone)-poly(ethylene glycol) (PECE) copolymer formed micelles in water, which turned instantly into a nonflowing gel at body temperature as a result of micellar aggregation. Effectiveness of doxorubicin-loaded PECE micelles (Dox-M) in improving intraperitoneal chemotherapeutic effect and preventing adhesions was investigated. Subsequently, we established a novel mouse model for postsurgical residual tumors and peritoneal adhesions, in which Dox-M could improve intraperitoneal chemotherapeutic effect and prevent postsurgical peritoneal adhesions simultaneously. Thus, it is a promising strategy to combine the CDDS and barrier method to improve the intraperitoneal chemotherapeutic effect and prevent peritoneal adhesions simultaneously after surgery.
    Article · Nov 2011 · Nanomedicine: nanotechnology, biology, and medicine
  • Cheng Wang · Yingjing Wang · Yujun Wang · [...] · Zhiyong Qian
    [Show abstract] [Hide abstract] ABSTRACT: Polymeric nanoparticles (NPs) have great potential application in achieving targeted delivery of anticancer drugs. Paclitaxel (PTX) loaded NPs were developed using biodegradable methoxy poly (ethylene glycol)-poly (ε-caprolactone) (MPEG-PCL) diblock copolymer by solid dispersion technique without toxic organic solvent. The lyophilized powder has been stored at room temperature for more than six months and still unchanged. PTX-loaded MPEG-PCL nanoparticles (PTX-NPs) displayed that the highest drug loading of PTX was about 25.6% and entrapment efficiency was over 98%, and the optimized average diameter and polydispersity index (PDI) were about 27.6 ± 0.1 nm and 0.05, respectively. Moreover, experimental results shown PTX-NPs had sustained-release effects and its curve fitting followed the Higuchi model. The maximum tolerated dose (MTD) of PTX-NPs after single dose in Balb/c mice was above 80 mg PTX/kg body weight (b.w), which was 2.6-fold higher than that of Taxol(®) (30 mg PTX/kg b.w). The levels of PTX administrated PTX-NPs had obvious distinction to Taxol(®) in plasma, liver, spleen, kidneys, lungs, heart and tumor. Especially, the concentration of PTX in tumor administrated PTX-NPs was higher than administration of Taxol(®). All results suggested that we had contrived a simple, biodegradable, effective and controllable drug delivery system for paclitaxel.
    Article · May 2011 · International Journal of Pharmaceutics
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    ChangYang Gong · YuJun Wang · XiuHong Wang · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: Polymeric micelles, prepared by self-assembly of biodegradable poly(ethylene glycol)-poly(ε-caprolactone)-poly(ethylene glycol) (PEG–PCL–PEG, PECE) copolymer in aqueous solution, were proved to be a potential carrier for hydrophobic drug honokiol in our previous contribution. In this study, the safety of blank PECE micelles was evaluated in vitro and in vivo before its further application in biomedical field. The average particle size of obtained micelle was 83.47±0.44nm, and polydisperse index was 0.27±0.01. Also, the zeta potential of prepared micelles was about −0.41±0.02mV. Otherwise, cytotoxicity of PECE micelles was evaluated by cell viability assay using L929 cells, and in vitro hemolytic test was also performed. In vivo acute toxicity evaluation and histopathological study of PECE micelles were conducted in BALB/c mice by intravenous administration. Furthermore, serum chemistry profile and complete blood count test were performed. In acute toxicity test, the mice were observed continuously for 7days. For histopathological study, samples including heart, liver, spleen, lung, and kidneys were histochemical prepared and stained with hematoxylin-eosin (H&E). No mortality or significant signs of acute toxicity was observed during the whole observation period, and there is no significant lesion to be shown in histopathological study of major organs. The maximal tolerance dose of PECE micelles (100mg/mL) by intravenous administration was calculated to be higher than 10g/kg body weight (b.w.). The results indicated that the obtained PECE micelles was non-toxic after intravenous administration, and could be a safe candidate for hydrophobic drug delivery system. KeywordsBiodegradable–Self-assembly–Micelle–Hemolytic test–Acute toxicity evaluation–Nanomedicine–Health and safety
    Full-text Article · Feb 2011 · Journal of Nanoparticle Research
  • [Show abstract] [Hide abstract] ABSTRACT: In attempt to overcome the problem of low water solubility and severe toxicity of camptothecin (CPT) after intravenous administration, a novel drug carrier system based on chitosan (CS) and dibasic sodium phosphate (DSP) has been developed in this paper to encapsulate CPT intending for local administration. Nanocolloids of CPT with size about 500  nm were first prepared, followed by encapsulation in the chitosan/dibasic sodium phosphate (CS/DSP) formulation. The formulation was sol state below 37°C and transformed to nonflowing gel state at 37°C. Encapsulation of CPT nanocolloids had greatly effect on the gelling time as well as the micro-structure of hydrogel. In vitro and in vivo degradation studies revealed that the developed CS/DSP hydrogel was biodegradable and biocompatible. In vitro release study revealed that CPT released from CS/DSP hydrogel in an extended period with about 70% of total CPT released from hydrogel after 18 days. Furthermore, nearly 90% of CPT in the chitosan hydrogels could be preserved in the lactone form (active form) even after 7 days's storage at 37°C. Furthermore, in vitro cytotoxicity of CPT nanocolloids on SKOV3 human ovarian cancer cells suggested the well anti-tumor cell efficiency could be gained at a lower concentration.
    Article · Jan 2011 · Journal of Pharmaceutical Sciences
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    [Show abstract] [Hide abstract] ABSTRACT: In this study, we aimed to develop a novel mannan loaded in situ gel-forming controlled protein delivery system for vaccine to improve humoral immunity. Preparation and potential application of mannan loaded biodegradable and injectable thermosensitive poly(ε-caprolactone)-poly(ethylene glycol)-poly(ε-caprolactone) (PCL-PEG-PCL, PCEC) hydrogel (M-hydrogel) was investigated. The prepared M-hydrogel is a free flowing sol at low temperature, which can be mixed with basic fibroblast growth factor (bFGF) easily, and forms a non-flowing gel at body temperature acting as in situ sustained delivery depot. Moreover, the interior morphology of bFGF-M-hydrogel was studied, which showed porous three-dimension structure. In addition, in vitro release assay indicated that bFGF could be released from the M-hydrogel system in a controlled manner. Furthermore, in vivo experiments indicated that the immunogenicity of bFGF was improved significantly after encapsulated into M-hydrogel, which was significantly higher than that of normal saline (NS), blank hydrogel, pure bFGF, bFGF loaded hydrogel (bFGF-hydrogel), bFGF and mannan mixture (bFGF-M), and bFGF loaded Complete Freund's Adjuvant (bFGF-CFA) groups. Therefore, M-hydrogel is believed to be promising as an in situ gel-forming controlled protein delivery system for vaccine.
    Full-text Article · Jan 2011 · Soft Materials
  • Ke Wang · Xu Xu · YuJun Wang · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: In this work, pH-sensitive P(CE-MAA-MEG) hydrogel coated with alginate-Ca2+ layer was successfully developed, which might be potential application for oral protein/vaccine delivery system. Morphology, swelling behavior, and in vitro release behavior of the alginate/P(CE-MAA-MEG) composite hydrogel were studied in detail. The results confirmed that the alginate/P(CE-MAA-MEG) composite hydrogel showed great pH-sensitivity. The fact that Bovine Serum Albumin (BSA) was released slowly in acidic environment while it was released quickly in neutral medium suggested that the composite hydrogel might be a candidate for protein drugs via oral administration.
    Article · Oct 2010 · Soft Materials
  • XiuHong Wang · Bing Kan · YuJun Wang · [...] · ZhiYong Qian
    [Show abstract] [Hide abstract] ABSTRACT: In our previous work, we had prepared a biodegradable amphiphilic three-armed star-shaped copolymers (SPCE) based on poly(epsilon-caprolactone) (PCL) and poly(ethylene glycol) (PEG), which could form micelles by self-assembly method and it was a potential carrier for hydrophobic drug. For further application, the safety of SPCE micelles was evaluated in vitro and in vivo here. (13)C-NMR was used to confirm the formation of the micelles in aqueous solution, and the morphology was observed on transmission electron microscope (TEM). Also, thermostability of blank SPCE micelles was determined by Malvern Nano-ZS 90 laser particle size analyzer. In vitro toxicity evaluation included hemolytic test and cytotoxicity. In vivo acute toxicity tests and histopathological study of SPCE micelles were carried out on BALB/C mice which were administrated SPCE micelles (1 g/kg b.w.) intravenously. In acute toxicity test, the mice were observed continuously for 7 days, obtained their body weight every day, at last the mice was sacrificed for the following study: the blood of the mice was assigned for blood chemistry and routine analysis, the heart, liver, spleen, lung, and kidneys were used for histopathological study. All results indicated that the biodegradable self-assembled SPCE micelles were nontoxic; therefore, it might be used as a safe candidate for drug delivery system.
    Article · Jun 2010 · Journal of Pharmaceutical Sciences
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    [Show abstract] [Hide abstract] ABSTRACT: This study aims to develop self-assembled poly(ethylene glycol)-poly(epsilon-caprolactone)-poly(ethylene glycol) (PEG-PCL-PEG, PECE) micelles to encapsulate hydrophobic honokiol (HK) in order to overcome its poor water solubility and to meet the requirement of intravenous administration. Honokiol loaded micelles (HK-micelles) were prepared by self-assembly of PECE copolymer in aqueous solution, triggered by its amphiphilic characteristic assisted by ultrasonication without any organic solvents, surfactants and vigorous stirring. The particle size of the prepared HK-micelles measured by Malvern laser particle size analyzer were 58 nm, which is small enough to be a candidate for an intravenous drug delivery system. Furthermore, the HK-micelles could be lyophilized into powder without any adjuvant, and the re-dissolved HK-micelles are stable and homogeneous with particle size about 61 nm. Furthermore, the in vitro release profile showed a significant difference between the rapid release of free HK and the much slower and sustained release of HK-micelles. Moreover, the cytotoxicity results of blank micelles and HK-micelles showed that the PECE micelle was a safe carrier and the encapsulated HK retained its potent antitumor effect. In short, the HK-micelles were successfully prepared by an improved method and might be promising carriers for intravenous delivery of HK in cancer chemotherapy, being effective, stable, safe (organic solvent and surfactant free), and easy to produce and scale up.
    Full-text Article · May 2010 · Nanotechnology