INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2020
·
IF 4.845
Kaipei Luo,Shaoping Yin,Ruixia Zhang,Hua Yu,Guangji Wang,Juan Li
The efficient delivery of chemotherapeutic drugs to the tumor tissues unavoidably encounters numerous obstacles, such as poor tumor targeting capability, slow intracellular drug release and massive accumulation in the liver. In this study, by self-assembling methoxy poly (ethylene glycol)-poly (lactide) block copolymer (mPEG-PLA) and hyaluronic acid-paclitaxel conjugate (HA-PTX), the composite nanoparticles (mPPHP NPs) were fabricated for efficient therapy of cancer. mPPHP NPs formed self-assembled nanoparticles (116 nm in diameter) with a narrow size distribution; and showed a rapid release of PTX in the presence of hyaluronidase and esterase . mPPHP NPs exhibited enhanced internalization by cells via CD44 receptors and selected cytotoxicity against A549 cells in vitro . More importantly, compared with other PTX formulations, mPPHP NPs were demonstrated to present the reduced liver accumulation, excellent tumor-targeting ability and superior antitumor efficacy in vivo , with a TIR of 75.9%. The multifunctional composite nanoparticles could be developed as a promising nano-carrier for improved therapeutic efficacy.
研究领域:
肿瘤学
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纳米医学
·
药剂学
·
分子靶向治疗
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药物递送系统
·
转化医学
✓ 已验证
DOI
高影响因子
JOURNAL OF SOLID STATE CHEMISTRY
·
2022
·
IF 3.656
Liang Qin,Yan Li,Deyun Ma,Fenglan Liang,Lidian Chen,Chenyang Xie,Jiayong Lin,Yani Pan,Guizhen Li,Fenrou Chen,Peiru Xu,Canlin Hong,Jiaxing Zhu
Two transition metal-based MOFs , {[Ni 2 (pip) 2 (bimb) 1.5 ]·2(H 2 O)} n ( 1 ), and {[Zn(pip)(bimb)]·DMF} n ( 2 ) (pip = 5-phenyl-isophthalate, bimb = 1,4-bis(imidazole-1-ylmethyl)benzene) have been successfully prepared. Complex 1 displays a three-dimensional structure with a 7-connected svk topology with a point symbol of (3 3 ∙4 14 ∙5 3 ∙6). Complex 2 performs a two-dimensional (4,4) sql net with channels of 7.0 × 5.5 Å 2 and 10.5 × 4.7 Å 2 along the b and c axis, respectively. The magnetic result of 1 shows an antiferromagnetic coupling between the two metal centers. Desolvated 2 adsorbs around 15.25 wt% 5-fluorouracil (5-FU). The 5-FU was slowly released without any burst release. The degradation of methyl orange caused by oxidizing sulfate radicals (SO 4− ) in a Fenton-like process has also been explored.
研究领域:
无机化学
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材料科学
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药物递送
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环境催化
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配位化学
✓ 已验证
DOI
高影响因子
RSC Advances
·
2016
·Vol. 6
·期 112
·111217-111225
·
IF 3.289
Sijie Zhao,Huiru Yang,Cai Zuo,Lu Sun,Liwei Ma,Hua Wei
Star-shaped polymers are attractive as drug carriers due to the integration of relatively easy synthesis compared to the preparation of hyper-branched dendrimers and their potential ability to form unimolecular nanoparticles with enhanced stability to survive the high dilution-associated deformation and subsequently premature drug release in the body fluids and blood during circulation. Clearly, the star structure exerts a significant effect on their bioproperties and potential applications. In this study, three star-shaped amphiphilic copolymers with the same polymer compositions but different star structures were synthesized to investigate the effect of star architecture on their properties as well as potential applications as drug carriers. Three different branched alcohols, 2-(hydroxymethyl) propane-1,3-diol, pentaerythritol and dipentaerythritol with 3, 4, and 6 respective hydroxyl groups were chosen as the starting core to generate the target star-shaped amphiphilic block copolymers composed of hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic poly(oligoethyleneglycol methacrylate) (POEGMA) with 3, 4, and 6 corresponding star arms by a combination of ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP). Dynamic light scattering (DLS) measurements and pyrene fluorescence probe technique confirmed the capability of the resultant star-shaped amphiphilic copolymers to form unimolecular micelles with average diameters smaller than 50 nm in an aqueous phase. A comparison of the drug loading capacity revealed that the micelles of 4-star-PCL–POEGMA (4s-PCL–POEGMA) exhibited the highest drug loading content (DLC) of all the three formulations. More importantly, in vitro doxorubicin (DOX) release study showed unique pH-mediated drug release behaviors, i.e., dramatically accelerated release at pH 6.0 but a much slower profile at pH 7.4, from these generally recognized “pH-insensitive” 4-arm star-shaped micelles. An acid-triggered degradation and an acid–base titration were performed to further reveal that such interesting pH-responsive drug release behaviors were attributed primarily to the hydrophilic corona of OEG brushes. This study is believed to provide a new insight into the structure–bioproperties relationship of star-shaped polymers, thus should be useful for the future design and development of novel star-shaped polymers for controlled drug delivery.
研究领域:
高分子药剂学
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纳米医学
·
药物控释
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生物材料
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药剂学
·
肿瘤治疗
·
纳米载体
✓ 已验证
DOI
高影响因子
INTERNATIONAL JOURNAL OF PHARMACEUTICS
·
2013
·
IF 3.458
Ziwei Zhang,Xiaole Qi,Xiangbo Li,Jiayu Xing,Xuehua Zhu,Zhenghong Wu
Multilayer-coating technology is the traditional method to achieve pulsatile drug release with the drawbacks of time consuming, more materials demanding and lack of efficiency. The purpose of this study was to design a novel pulsatile drug delivery system based on the physiochemical interaction between acrylic copolymer and organic acid with relatively simpler formulation and manufacturing process. The Enalapril Maleate (EM) pulsatile release pellets were prepared using extruding granulation, spheronization and fluid-bed coating technology. The ion-exchange experiment, hydration study and determination of glass transition temperature were conducted to explore the related drug release mechanism. Bioavailability experiment was carried out by administering the pulsatile release pellets to rats compared with marketed rapid release tablets Yisu ® . An obvious 4 h lag time period and rapid drug release was observed from in vitro dissolution profiles. The release mechanism was a combination of both disassociated and undisassociated forms of succinic acid physiochemically interacting with Eudragit ® RS. The AUC0-τ of the EM pulsatile pellets and the market tablets was 702.384 ± 96.891 h ng/mL and 810.817 ± 67.712 h ng/mL, while the relative bioavailability was 86.62%. These studies demonstrate this novel pulsatile release concept may be a promising strategy for oral pulsatile delivery system.
研究领域:
药剂学
·
药物递送
·
生物药剂学
·
药物代谢
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制剂工程
·
药动学
✓ 已验证
DOI
高影响因子
Small
·
2017
·Vol. 14
·期 7
·1702288
·
IF 8.643
Meiling Zhu,Kongchang Wei,Sien Lin,Xiaoyu Chen,Chia-Ching Wu,Gang Li,Liming Bian
Targeted and sustained delivery of drugs to diseased tissues/organs, where body fluid exchange and catabolic activity are substantial, is challenging due to the fast cleansing and degradation of the drugs by these harsh environmental factors. Herein, a multifunctional and bioadhesive polycaprolactone-β-cyclodextrin (PCL-CD) polymersome is developed for localized and sustained co-delivery of hydrophilic and hydrophobic drug molecules. This PCL-CD polymersome affords multivalent crosslinking action via surface CD-mediated host–guest interactions to generate a supramolecular hydrogel that exhibits evident shear thinning and efficient self-healing behavior. The co-delivery of small molecule and proteinaceous agents by the encapsulated PCL-CD polymersomes enhances the differentiation of stem cells seeded in the hydrogel. Furthermore, the PCL-CD polymersomes are capable of in situ grafting to biological tissues via host–guest complexation between surface CD and native guest groups in the tissue matrix both in vitro and in vivo, thereby effectively extending the retention of loaded cargo in the grafted tissue. It is further demonstrated that the co-delivery of small molecule and proteinaceous drugs via PCL-CD polymersomes averts cartilage degeneration in animal osteoarthritic (OA) knee joints, which are known for their biochemically harsh and fluidically dynamic environment.
研究领域:
药物递送
·
生物材料
·
组织工程
·
纳米医学
·
再生医学
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关节生物学
·
转化医学
✓ 已验证
DOI
高影响因子
Materials Science & Engineering C-Materials for Biological Applications
·
2016
·
IF 3.42
Haibin Li,Fei Jiang,Song Ye,Yingying Wu,Kaiping Zhu,Deping Wang
The strontium-substituted hydroxyapatite microspheres (SrHA) incorporated alginate composite microspheres (SrHA/Alginate) were prepared via adding SrHA/alginate suspension dropwise into calcium chloride solution, in which the gel beads were formed by means of crosslinking reaction. The structure, morphology and in vitro bioactivity of the composite microspheres were studied by using XRD, SEM and EDS methods. The biological behaviors were characterized and analyzed through inductively coupled plasma optical emission spectroscopy (ICP-OES), CCK-8, confocal laser microscope and ALP activity evaluations. The experimental results indicated that the synthetic SrHA/Alginate showed similar morphology to the well-known alginate microspheres (Alginate) and both of them possessed a great in vitro bioactivity. Compared with the control Alginate, the SrHA/Alginate enhanced MC3T3-E1 cell proliferation and ALP activity by releasing osteoinductive and osteogenic Sr ions. Furthermore, vancomycin was used as a model drug to investigate the drug release behaviors of the SrHA/Alginate, Alginate and SrHA. The results suggested that the SrHA/Alginate had a highest drug-loading efficiency and best controlled drug release properties. Additionally, the SrHA/Alginate was demonstrated to be pH-sensitive as well. The increase of the pH value in phosphate buffer solution (PBS) accelerated the vancomycin release. Accordingly, the multifunctional SrHA/Alginate can be applied in the field of bioactive drug carriers and bone filling materials.
研究领域:
生物材料学
·
骨组织工程
·
药物递送系统
·
生物医学工程
·
再生医学
·
生物无机化学
·
药剂学
✓ 已验证
DOI
高影响因子
AAPS PHARMSCITECH
·
2019
·Vol. 20
·期 1
·1-14
·
IF 2.608
Wang Xingqi,Zhang Yong,Huang Jie,Tian Chunling,Xia Mengqiu,Liu Liu,Li Zhengguang,Cao Jiaojiao,Gui Shuangying,Chu Xiaoqin
The purpose of this paper was to investigate the potential of liquid crystalline (LC) gels for ophthalmic delivery, so as to enhance the bioavailability of pilocarpine nitrate (PN). The gels were prepared by a vortex method using phytantriol and water (in the ratio of 73:27 w / w ). Their inner structures were confirmed by crossed polarized light microscopy, small-angle X-ray scattering, attenuated total reflectance-Fourier transform infrared spectrum, and rheology. The in vitro release studies revealed that PN could keep sustained release from the gels over a period of 12 h. The ex vivo apparent permeability coefficient of the gels demonstrated a 3.83-folds ( P < 0.05) increase compared with that of eye drops. The corneal hydration levels of the gel maintained in the normal range of 79.46 ± 2.82%, hinting that the gel could be considered non-damaging and safe to the eyes. Furthermore, in vivo residence time evaluation suggested that a better retention performance of LC gel was observed in rabbit’s eyes compared to eye drops. In vivo ocular irritation study indicated that LC gel was nonirritant and might be suitable for various eye applications. In conclusion, LC gels might represent a potential ophthalmic delivery strategy to overcome the limitations of eye drops.
研究领域:
药剂学
·
药物递送系统
·
眼科学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）