DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
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2019
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IF 2.367
Jing Zhou,Yuanyuan Chen,Mengmeng Luo,Fen Deng,Sen Lin,Wencan Wu,Guqiang Li,Kaihui Nan
Objective: This study was aimed to develop sustained drug release from levofloxacin (LF)-loaded chitosan (CS) microspheres for treating ophthalmic infections.Significance: Dual cross-linked CS microspheres developed by the spray-drying technique displays significantly higher level of sustained drug release compared with non-cross-linked CS microspheres.Methods: LF-loaded CS microspheres were prepared using the spray-drying technique, and then solidified with tripolyphosphate and glutaraldehyde as dual cross-linking agents. The microspheres were characterized by surface morphology, size distribution, zeta potential, encapsulation efficiency, and drug release profiles in vitro. The drug quantification was verified and analyzed by high-performance liquid chromatography (HPLC). The structural interactions of the CS with LF were studied with Fourier transform infrared spectroscopy. The effect of various influencing excipients in the formulation of the dual cross-linked CS microspheres on drug encapsulation efficiency and the drug release profiles were extensively investigated.Result: The microspheres demonstrated high encapsulation efficiency (72.4 ∼ 98.55%) and were uniformly spherical with wrinkled surface. The mean particle size was between 1020.7 ± 101.9 and 2381.2 ± 101.6 nm. All microspheres were positively charged (zeta potential ranged from 31.1 ± 1.32 to 42.81 ± 1.55 mV). The in vitro release profiles showed a sustained release of the drug and it was remarkably influenced by the cross-linking process.Conclusion: This novel spray-drying technique we have developed is suitable for manufacturing LF-loaded CS microspheres, and thus could serve as a potential platform for sustained drug release for effective therapeutic application in ocular infections.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
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2018
·
IF 3.909
Lin Wang,Yu Du,Yi Yuan,Ruo-Jun Mu,Jingni Gong,Yongsheng Ni,Jie Pang,Chunhua Wu
Intelligent hydrogels are attractive biomaterials for various applications, however, fabricating a hydrogel with both adequate self-healing ability and mechanical properties remains a challenge. Herein, a series of novel intelligent konjac glucomannan (KGM)/microcrystalline cellulose (MCC) hydrogels were prepared vis the mussel-inspired chemistry. MCC was firstly functionalized by the oxidative polymerization of dopamine, and the intelligent hydrogels were obtained by mixing aqueous solutions of KGM and functionalized MCC (PDMCC). By introducing PDMCC, a more compact interconnected porous structure formed for the resulting hydrogels. The self-healing ability and mechanical properties of intelligent hydrogels were dependence on the PDMCC content. Compared with KGM hydrogels, KGM/PDMCC hydrogels exhibited a more distinct pH sensitivity and a lower initial burst release, which was attributed to the compact structure and strong intermolecular hydrogen bond interaction between PDMCC and KGM. These results suggest that the KGM/PDMCC intelligent hydrogels may be promising carriers for controlled drug delivery.
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JOURNAL OF FOOD PROCESSING AND PRESERVATION
·
2018
·Vol. 42
·期 8
·e13696
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IF 1.51
Xingzhong Zhang,Xia Wu,Wei Li,Xiaogang Luo,Yan Li,Bin Li,Shilin Liu
In order to increase the solubility, stability, and availability of cinnamaldehyde which was widely used in food industry, ethyl cellulose aqueous dispersions encapsulated cinnamaldehyde had been prepared by using an anti-solvent induced method. The particles size of the obtained aqueous dispersions was in the range of 150–200 nm, and it increased slightly with the increasing concentrations of the precursor solution. The prepared dispersions after being dried at ambient conditions had the ability to form a free-standing film, and the film had denser structure and smooth surface. Moreover, the ethyl cellulose dispersions had powerful encapsulation ability to cinnamaldehyde, and the encapsulated cinnamaldehyde could be sustained released, it could prolong the storage time of fresh pork samples for more than 6 days, and an excellent antimicrobial property for food spoilage was observed. It indicated that the prepared dispersions could be a fascinating supporter for increasing the stability and sustained-release of cinnamaldehyde. Practical applications In this work, the ethyl cellulose aqueous dispersions encapsulating with cinnamaldehyde had good stability, and the sustained released of cinnamaldehyde could effectively inhibit the growth of spoilage organism for a long time, which indicated that aqueous dispersions system had potential applications for food preservation.
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Bioactive Materials
·
2022
·
IF 16.874
Ruofei Wang,Xia-Xiao Wu,Zhenming Tian,Tian Hu,Chaoyang Cai,Guan-Ping Wu,Gang-Biao Jiang,Bin Liu
Spinal cord injury (SCI) results in massive neuronal death, axonal disruption, and cascading inflammatory response, which causes further damage to impaired neurons. The survived neurons with damaged function fail to form effective neuronal circuits. It is mainly caused by the neuroinflammatory microenvironment at injury sites and regenerated axons without guidance. To address this challenge, a ferrofluid hydrogel (FFH) was prepared with Ferric tetrasulfide (Fe 3 S 4 ), carboxymethyl chitosan, and gold. Its internal structural particles can be oriented in a magnetic field to acquire anisotropy. Moreover, Fe 3 S 4 can release hydrogen sulfide (H 2 S) with anti-inflammatory effects under acidic conditions. Regarding in vitro experiments, 0.01g/ml Fe 3 S 4 FFH significantly reduced the inflammatory factors produced by LPS-induced BV2 cells. Oriented and longer axons of the induced neural stem cells loaded on anisotropic FFH were observed. In vivo experiments showed that FFH reduced the activated microglia/macrophage and the expression of pro-inflammatory factors in SCI rats through the NF-κB pathway. Moreover, it significantly promoted directional axonal regrowth and functional recovery after SCI. Given the critical role of inhibition of neuroinflammation and directional axonal growth, anisotropic Fe 3 S 4 FFH is a promising alternative for the treatment of SCI.
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CHEMISTRY-A EUROPEAN JOURNAL
·
2023
·Vol. 29
·期 21
·e202203458
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IF 4.3
Peng Wang,Guangyu Wang,Hongwen Tang,Siwen Feng,Lichuan Tan,Pu Zhang,Guihua Wei,Cuijuan Wang
Graphical A ropivacaine microspheres encapsulated by zeolite imidazole framework (RVC@ZIF-8) as sustained-release system was prepared for the first time. This novel material exhibits a high drug loading rate and superior biological safety, with a continuously release in vitro for at least 96 h, and the sensory block time was more than 72 h in vivo pharmacodynamic. The management of persistent postoperative pain still remains a clinical challenge currently. Although ropivacaine (RVC) is widely used for postoperative analgesia as a local anesthetic, the short half-life makes it difficult to achieve the desired duration of analgesia. Herein, a RVC sustained-release microspheres encapsulated by zeolite imidazole framework-8 (RVC@ZIF-8) was synthesized for the first time, which prolonged the sustained-release of RVC and decreased the resulting drug toxicity. RVC can continuously release in vitro for at least 96 h with high drug loading of 30.6 % and RVC@ZIF-8 had excellent biocompatibility and low cytotoxicity. In sciatic nerve block model, the sensory block time of RVC@ZIF-8 was significantly prolonged compared with RVC, achieving more than 72 h post injection and no inflammation or lesion were found. Based on high drug loading, ideal sustained-release and superior biological safety, RVC@ZIF-8 will be a novel delivery material for local anesthetic with potential application.
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CRYSTAL GROWTH & DESIGN
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2022
·
IF 4.01
Chenxin Duan,Yanming Chen,Yuxin Zhang,Feifei Liang,Wenwen Liu,Xinyi Xiao,Cangcang Xu,Tao Zhuang,Chao Hao,Yin Chen
As the first FDA-approved PARP1/2 inhibitor, olaparib (OLA) is a blockbuster anticancer drug, but its use has been limited by the dose-limiting toxicity and short half life of commercially available immediate-release preparations. To realize the sustained release of OLA, the cocrystal of OLA with kaempferol (KAE) and the cocrystal solvate of OLA with quercetin (QUE) were screened and obtained in this study. The cocrystals were characterized by X-ray diffraction, Hirshfeld surface, thermal analysis, and spectroscopic analysis. Intrinsic dissolution rate (IDR) experiments showed that the IDR values of both OLA–KAE and OLA–QUE were 0.40 times that of pure OLA. In dissolution experiments, the dissolution of OLA–KAE and OLA–QUE in pH 6.8 medium was reduced to 21.4% and 18.6% of the original drug, respectively. The stability test indicates that OLA–KAE has excellent physical stability under accelerated conditions for 3 months. Moreover, OLA–KAE and OLA–QUE showed significantly increased inhibiting effects on ovarian cancer cells compared to OLA in MTT assays. This work provides a promising approach for developing sustained-release formulations of OLA via cocrystallization with enhanced pharmacological activity.
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Bioactive Materials
·
2022
·
IF 16.874
Lang Chen,Chenyan Yu,Yuan Xiong,Kai Chen,Pei Liu,Adriana C. Panayi,Xiufeng Xiao,Qian Feng,Bobin Mi,Guohui Liu
Fracture nonunion remains a great challenge for orthopedic surgeons. Fracture repair comprises of three phases, the inflammatory, repair and remodeling stage. Extensive advancements have been made in the field of bone repair, including development of strategies to balance the M1/M2 macrophage populations, and to improve osteogenesis and angiogenesis. However, such developments focused on only one or the latter two phases, while ignoring the inflammatory phase during which cell recruitment occurs. In this study, we combined Stromal Cell-Derived Factor-1α (SDF-1α) and M2 macrophage derived exosomes (M2D-Exos) with a hyaluronic acid (HA)-based hydrogel precursor solution to synthesize an injectable, self-healing, adhesive [email protected] α/M2D-Exos hydrogel. The HA hydrogel demonstrated good biocompatibility and hemostatic ability, with the 4% HA hydrogels displaying great antibacterial activity against gram-negative E. coli and gram-positive S. aureus and Methicillin-resistant Staphylococcus aureus (MRSA). Synchronously and sustainably released SDF-1α and M2D-Exos from the [email protected] α/M2D-Exos hydrogel enhanced proliferation and migration of human bone marrow mesenchymal stem cell (HMSCs) and Human Umbilical Vein Endothelial Cells (HUVECs), promoting osteogenesis and angiogenesis both in vivo and in vitro. Overall, the developed [email protected] SDF-1α/M2D-Exos hydrogel was compatible with the natural healing process of fractures and provides a new modality for accelerating bone repair by coupling osteogenesis, angiogenesis, and resisting infection at all stages.
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GREEN CHEMISTRY
·
2022
·Vol. 24
·期 20
·8088-8099
·
IF 11.034
Yuntian Xiao,Chuanhua Wu,Ling Zhou,Qiuxiang Yin,Jingxiang Yang
Due to the poor efficacy and environmental contamination caused by the ease of leaching, highly water-soluble herbicides have received considerable attention. For example, metamitron (MET), a herbicide that is used for controlling grass and broadleaf weeds in sugar beet fields, has led to a great threat to aquatic invertebrates because of its great migratory capacity. As a result, it is critical to control the release rate of MET applied in the field. Cocrystallization has been proven to be an effective strategy for dissolution property manipulation of pharmaceuticals and agrochemicals. However, few cocrystals of herbicides were reported for the release rate control. Herein, cocrystals of MET with cinnamic acid (CA), naringenin (NA), and baicalein (BA) were developed. Compared to pure MET, the dissolution rate of cocrystals MET–NA and MET–BA were dramatically decreased by 98.30% and 96.28%, respectively; the solubility of MET–NA and MET–BA were decreased by 95.49% and 96.21%. Leaching experiments showed that the leaching amounts of MET–NA and MET–BA in the soil were significantly reduced to roughly one-fifth of pure MET. Under simulated rainfall, the MET–NA and MET–BA showed a longer duration of action than pure MET. Additionally, crystal structure analysis and molecular dynamics simulations were conducted to reveal the mechanism of the sustained release effect of cocrystals MET–NA and MET–BA at a molecular level. This work demonstrates that cocrystal engineering can offer a promising strategy to achieve sustained-release efficacy and reduce environmental damage for highly water-soluble herbicides.
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POLYMERS FOR ADVANCED TECHNOLOGIES
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2022
·Vol. 34
·期 1
·155-165
·
IF 3.348
Chengjun Peng,Guichun Wang,Yuxiao Wang,Maomao Tang,Xiaodong Ma,Xiangwei Chang,Jian Guo,Shuangying Gui
Periodontitis is a chronic inflammatory disease of tooth support tissues leading to progressive destruction of periodontal soft tissues as well as alveolar bone, and can be treated with anti-inflammatory and bone-protective agents to prevent disease progression. Caffeic acid phenethyl ester (CAPE) is a natural polyphenolic compound with anti-inflammation, anti-oxidation and bone tissue repair efficacy. In this work, we synthesized a thermosensitive hydrogel matrix of acetylated carboxymethyl chitosan (A-CC), and firstly applied for periodontal local drug delivery. The biocompatible CAPE-loaded A-CC hydrogel (CAPE-A-CC) has the advantages of forming a drug depot in situ, sustained release and precisely improving the drug concentration in the lesion sites compared with traditional systemic administration. In addition, CAPE-A-CC could significantly inhibit the expression of inflammatory cytokines of TNF-α, IL-1β, IL-6, and IL-17 in macrophages, and increased the expression of alkaline phosphatase (ALP) in human periodontal ligament stem cells (hPDLSC) related to osteogenesis. This study develops a novel in situ thermosensitive hydrogel delivery system to improve the therapeutic potential of natural active ingredient for periodontitis therapy.
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
·
2021
·
IF 6.953
Aiping Zhang,Yucheng Zou,Yuhang Xi,Peng Wang,Yue Zhang,Liangru Wu,Hui Zhang
The feasibility of using unmodified bamboo shoot cellulose (BSC) to produce composite aerogels with sodium alginate (SA) in a fast and green way for sustained release of curcumin was explored for the first time, in which calcium ion-induced SA cross-linking could effectively retain the structural stability of aerogel skeleton. The aerogels were characterized by scanning electron microscopy, Fourier transform infrared spectroscopy and differential scanning calorimetry . The encapsulation and release of curcumin from aerogels were studied while the antioxidant activity of encapsulated curcumin was investigated. Curcumin was evenly encapsulated in the composite aerogels and showed a sustained release behavior, followed the first-order rate expression. Interpenetrating network structures were built between BSC and SA mainly through hydrogen bonding, which could be further reinforced by the cross-linking of CaCO 3 on the SA matrix. The original characteristics of BSC in the composite aerogels were well retained. The thermal stability and mechanical properties of the composite aerogels were improved by Ca 2+ -induced cross-linking, while the uncross-linked composite aerogels exhibited better encapsulation efficiency and in vitro antioxidant activity. Overall, this study was the first to use cellulose from bamboo shoot to develop aerogels for drug delivery purposes. The cellulose/alginate composite aerogels were promising to be used as biocompatible carriers for drug and nutraceutical delivery.
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ACS Applied Bio Materials
·
2020
·
IF 0
Jinyu Hu,Yi Song,Cuiyun Zhang,Wen Huang,Anqi Chen,Huacheng He,Susu Zhang,Yanxin Chen,Chaodong Tu,Jianhui Liu,Xuan Xuan,Yung Chang,Jie Zheng,Jiang Wu
Development of biocompatible and bioactive drug-loaded sutures is considered as an effective but challenging strategy for the wound healing process by delivering biological drugs (e.g., antibiotics) or growth factors (e.g., bFGF) at the surgical wound sites. Conventional offline suture strategies often lead to fast and uncontrollable release of drugs at wound sites, rendering wound healing to become a longer and painful process for patients. Herein, we propose an online suture strategy to fabricate electrospun polycaprolactone (PCL) fibrous yarns, incorporated with both collagen (COL) and bFGF, to produce bFGF-COL@PCL sutures. Upon demonstrating the well-oriented and aligned fibrous microstructure, high mechanical properties, and controlled release of bFGF from bFGF-COL@PCL sutures in vitro, we then applied bFGF-COL@PCL sutures to an incision wound healing mouse model in vivo. Further in vivo study showed that as compared to the commercialized Vicryl suture, bFGF-COL@PCL sutures significantly promoted the wound healing at different stages by accelerating granulation tissue formation, collagen deposition, and re-epithelialization. The enhanced wound healing efficiency of bFGF-COL@PCL sutures is likely attributed to two synergistic factors: (i) the well-oriented nanofibrous structure reduces tissue drag to minimize their trauma and (ii) the presence of both collagen and bFGF enhances the basement membrane (BM) reconstruction, cell proliferation, and angiogenesis. This work demonstrates an effective suture strategy and system for surgical suture applications.
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JOURNAL OF PHARMACY AND PHARMACOLOGY
·
2020
·Vol. 72
·期 9
·1152-1164
·
IF 2.571
Wang Jinwu,Zhu Gaosheng,Wang Xingyu,Cai Jie,Xie Linzhen,Zheng Wenhao,Feng Yongzeng,Guo Qiang,Chen Hua,Cai Leyi
ObjectivesIcariin, extracted from Epimedium, is a kind of flavonoid and possesses osteogenesis and antioxidant. This study aimed to evaluate the therapeutic effects of icariin liposome on acute blunt skeletal muscle injury in rats.MethodsIcariin liposome was prepared by the thin-film dispersion method. After muscle injury, the corresponding treatment measures were given every day for two weeks. Recovery and mechanism of muscle injury were evaluated by QRT-PCR, HE, immunohistochemistry, malondialdehyde, superoxide dismutase and serological tests.Key findingsThe particle size, polydispersity index, zeta potential, encapsulation efficiency and drug loading of icariin liposomes were 171.37 ± 38.23 nm, 0.27 ± 0.01, −5.59 ± 1.36 mV, 78.15 ± 2.04% and 15.62%, respectively. The QRT-PCR showed that icariin liposome significantly promoted the expression of MHCIIB and vimentin. Through HE, immunohistochemistry, ELISA and serological tests, we found that icariin liposome effectively promoted desmin expression, reduced collagen I expression and inhibited the production of pro-inflammatory factors, including TNF-α and IL-6. Icariin liposome therapy significantly reduced the level of malondialdehyde and increased the activity of superoxide dismutase.ConclusionsIcariin liposome has excellent therapeutic effects on acute blunt muscle injury in rats by improving immunity, repairing cytoskeleton and cellular integrity, anti-inflammation, anti-fibrosis and antioxidant stress.
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