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JOURNAL OF THE CHINESE CHEMICAL SOCIETY · 2017 ·Vol. 64 ·期 2 ·231-238 · IF 0.935

Effect of Sodium Alginate on the Properties of Thermosensitive Hydrogels

Jie Wu,Zongmei Wu,Xuejiao Sun,Shichao Yuan,Ruling Zhang,Qingliang Lu,Yueqin Yu

Sodium alginate (SA) was combined with poly( N -isopropylacrylamide) (PNIPAAm) to prepare thermosensitive hydrogels through semi-interpenetrating polymer network (semi-IPN) and fully interpenetrating polymer network (full-IPN). The thermosensitive, swelling, mechanical, and thermal properties of pure PNIPAAm, SA/PNIPAAm semi-IPN, and Ca-alginate/PNIPAAm full-IPN hydrogels were investigated. The formation of semi-IPN and full-IPN significantly improved the hydrogels’ swelling capability and mechanical properties without altering their thermosensitivity. 5-Fluorouracil (5-Fu) was selected as a model drug to study the release behaviors of the hydrogels. It was found that in vitro controlled drug release from semi-IPN hydrogels showed an initial release burst, followed by a slower and sustained release, before reaching equilibrium. Full-IPN hydrogels showed slow and sustained release during the whole process. Temperature and pH were found to affect the rate of drug release. Ca-alginate/PNIPAAm full-IPN hydrogels have potential application as drug delivery matrices in controlled drug release.

研究领域: 生物材料 · 药剂学 · 高分子科学 · 组织工程 · 药物递送系统
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INTERNATIONAL JOURNAL OF PHARMACEUTICS · 2013 · IF 3.458

A novel pulsatile drug delivery system based on the physiochemical reaction between acrylic copolymer and organic acid: In vitro and in vivo evaluation

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 · 制剂工程 · 药动学
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Small · 2017 ·Vol. 14 ·期 7 ·1702288 · IF 8.643

Bioadhesive Polymersome for Localized and Sustained Drug Delivery at Pathological Sites with Harsh Enzymatic and Fluidic Environment via Supramolecular Host–Guest Complexation

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 · 关节生物学 · 转化医学
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Materials Science & Engineering C-Materials for Biological Applications · 2016 · IF 3.42

Bioactive apatite incorporated alginate microspheres with sustained drug-delivery for bone regeneration application

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
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