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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 417-426页

作者： Longmei Wang Ruihua Feng Jinhua Gao Yanwei Xi Guihua Huang The School of Pharmaceutical Science Shandong University

The aim of the current work was to develop generic sustained-release tablets containing35 mg trimetazidine dihydrochloride and to establish an in vitro–in vivo correlation that could predict the bioavailability. The marketed sustained release tablet(Vastarel MR) used as reference, a sustained-release matrix tablet was prepared using hydroxypropyl methylcellulose(HPMC) as matrix by wet granulation and the in vitro dissolution profiles of the self-made tablets were determined in four different dissolution media(0.1 M HCl, pH 4.5 PBS, pH 6.8 PBS and water). A higher similarity between prepared tablets and Vastarel MR was established, with similarity factor(f2) ranging from 60 to 75 in the four media. The in vivo pharmacokinetics was studied in six healthy beagles. Compared with Vastarel MR, the Cmax of self-made tablets was slightly decreased, while the Tmax and MRT0–t were slightly prolonged, but with no significant difference(P > 0.05). The average of relative bioavailability(F) was 102.52% based on AUC0–t. For log-transformed AUC0–t and Cmax, the upper confidence limit on the appropriate criterion is release rate and extent of absorption, and a good in vivo–in vitro correlation was established for the self-made tablets that indicated in vitro dissolution tests could be used as a surrogate for bioavailability studies.

关键词： Bioequivalence studies Generic tablets In vitro-in vivo correlation sustained release

Polydopamine-modified collagen sponge scaffold as a novel dermal regeneration template with sustained release of platelet-rich plasma to accelerate skin repair:A one-step strategy

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Bioactive Materials 2021年第8期6卷 2613-2628页

作者： Zijun Zheng Minxiong Li Pengwei Shi Yanbin Gao Jun Ma Yuchen Li Lei Huang Zhangfeifan Yang Lei Yang Department of Burns Nanfang HospitalSouthern Medical UniversityJingxi StreetBaiyun DistrictGuangzhou510515PR China Department of Emergency Nanfang HospitalSouthern Medical UniversityJingxi StreetBaiyun DistrictGuangzhou510515PR China Department of Statistics University of British Columbia2329 West MallVancouverV6T 1Z4BCCanada

Although employed to release growth factors(GFs)for regenerative medicine,platelet-rich plasma(PRP)has been hindered by issues like burst *** on collagen sponge scaffolds(CSSs)modified with polydopamine(pDA),a novel dermal regeneration template(DRT)was ***,whether it could efficiently deliver PRP and even foster wound healing remained *** this work,after PRP was prepared and pDA-modified CSSs(pDA-CSSs)were fabricated,microscopic observation,GFs release assay and in-vitro biological evaluations of pDA-CSSs with PRP(pDA-CSS@PRP)were performed,followed by BALA-C/nu mice full-thickness skin defects implanted with pDA-CSS@PRP covered by grafted skins(termed as a One-step strategy).As a result,scanning electron microscope demonstrated more immobilized platelets on pDA-CSS′surface with GFs’controlled release via enzyme-linked immunosorbent assay,compared with *** line with enhanced in-vitro proliferation,adhesion and migration of keratinocytes&endothelial cells,pDA-CSS@PRP were histologically revealed to accelerate wound healing with less scar via rapid angiogenesis,arrangement of more mature collagen,guiding cells to spread,*** conclusion,pDA-CSSs have potential to serve as a novel DRT capable of delivering PRP,which may foster full-thickness skin defect healing by means of a One-step strategy.

关键词： Polydopamine sustained release Platelet-rich plasma Dermal regeneration template Full-thickness skin defect

Formation of composite hydrogel of carboxymethyl konjac glucomannan/gelatin for sustained release of EGCG

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Food Science and Human Wellness 2022年第5期11卷 1373-1383页

作者： Lin Wang Ning zhou Shengxuan Zheng Jie Pang Department of Engineering Mechanics Tsinghua UniversityBeijing 100084China Institute of Superlubricity Technology Research Institute of Tsinghua University in ShenzhenShenzhen 518057China College of Food Science Fujian Agriculture and Forestry UniversityFuzhou 350002China

Development of functional bioinspired hydrogels that have good releases control character is necessary for the application of these materials in biomedical ***,we report a composite hydrogel prepared from several biocompatible carboxymethyl konjac glucomannan(CKGM)/gelatin(G)/tannic acid(TA)functional nano-hydroxyapatite(TA@n-HA),which has good biodegradability and pH *** mechanism of interaction between hydrogels was confirmed by Fourier transform infrared spectroscopy,X-ray diffraction,Scanning electron microscopy and Thermogravimetric *** physico-chemical properties of CKGM/G hydrogels have been significantly improved through the incorporation of TA@n-HA within the *** in the sustained release of epigallocatechin gallate(EGCG)demonstrated that the TA@n-HA/CKGM/G hydrogels exhibit not only better pH sensitive properties,but also enhanced biocompatibility and encapsulation in comparison to the matrix devoid of TA@***,TA@n-HA/CKGM/G hydrogels using EGCG as a drug release model show the potential for drug delivery.

关键词： Hydrogel Carboxymethyl konjac glucomannan Gelatin Tannic acid Biodegradation sustained release

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Enhanced delivery efficiency and sustained release of biopharmaceuticals by complexation-based gel encapsulated coated microneedles:rhIFNα-1b example

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Asian Journal of Pharmaceutical Sciences 2021年第5期16卷 612-622页

作者： Zequan Zhou Suohui Zhang Guozhong Yang Yunhua Gao Key Laboratory of Photochemical Conversion and Optoelectronic Materials Technical Institute of Physics and ChemistryChinese Academy of SciencesBeijing 100190China University of Chinese Academy of Sciences Beijing 100049China Beijing CAS Microneedle Technology Ltd Beijing 102609China

Coated microneedles(MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs(GEC-MNs) was developed. The water-soluble drug coating was encapsulated with sodium alginate(SA) in situ complexation gel. The manufacturing process of GEC-MNs was optimized for mass production. Compared to the water-soluble coated MNs(72.02% ± 11.49%), the drug delivery efficiency of the optimized GEC-MNs(88.42% ± 6.72%) was steadily increased, and this improvement was investigated through in vitro drug release. The sustained-release of BSA was observed in vitro permeation through the skin. The rhIFN α-1 b GEC-MNs was confirmed to achieve biosafety and 6-month storage stability. Pharmacokinetics of rhIFN α-1 b in GEC-MNs showed a linearly dosedependent relationship. The AUC of rhIFN α-1 b in GEC-MNs(4.51 ng/ml ·h) was bioequivalent to the intradermal(ID) injection(5.36 ng/ml ·h) and significantly higher than water-soluble coated MNs(3.12 ng/ml ·h). The rhIFN α-1 b elimination half-life of GEC-MNs, soluble coated MNs, and ID injection was 18.16, 1.44, and 2.53 h, respectively. The complexation-based GECMNs have proved to be more efficient, stable, and achieve the sustained-release of watersoluble drug in coating MNs, constituting a high value to biopharmaceutical.

关键词： Coated microneedle Drug delivery system sustained release Interferon alpha 1b Sodium alginate

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Characterization of physiochemical and biological properties of spherical protein crystals for sustained release

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Asian Journal of Pharmaceutical Sciences 2013年第1期8卷 58-63页

作者： Kai Shi Hongshu Bi Yanbo Jiang Shenyang Pharmaceutical University No.103Wenhua RoadShenyang 110016China Liaoning Satellite Biotechnology Products Research Institute No.51-3Dongzhan StreetShenyang 110044China

This study presents an exploration on extending the action of therapeutic proteins by crystallization strategy without new molecular entities *** human interferon a-2b(rhIFN),a model protein drug in this case,was crystallized using a hanging drop vapor diffusion method.A novel chelating technique with metal ions was employed to promote crystals *** physico-chemical characterization of the protein crystals,including morphology,particle size,X-ray diffraction,circular dichroism and biological potency evaluations were *** addition,the in vitro release behavior of rhIFN from crystal lattice suggested an exciting possibility of protein crystals as a longacting *** work described here demonstrates the possibility of spherical crystals of biomacromolecules for controllable delivery application of therapeutic proteins.

关键词： Protein Spherical crystal Characterization sustained release

Size-dependent cellular uptake and sustained drug release of PLGA particles

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Particuology 2023年第2期73卷 1-7页

作者： Rui Sun Xia Liu Yu Zhang Qian Li Ying Zhu Chunhai Fan Division of Physical Biology CAS Key Laboratory of Interfacial Physics and TechnologyShanghai Institute of Applied PhysicsChinese Academy of SciencesShanghai 201800China The Interdisciplinary Research Center Shanghai Synchrotron Radiation FacilityZhangjiang LaboratoryShanghai Advanced Research InstituteChinese Academy of SciencesShanghai 201210China University of Chinese Academy of Sciences Beijing 100049China School of Chemistry and Chemical Engineering Frontiers Science Center for Transformative Molecules and National Center for Translational MedicineShanghai Jiao Tong UniversityShanghai 200240China

Poly(lactic-co-glycolic)acid(PLGA)particles have become a commonly used drug delivery strategy in the pharmaceutical *** this work,we aim to investigate the size-dependent cellular internalization of PLGA particles and its effects on sustained drug *** prepared three different-sized particles using PLGA(200,500 and 2000 nm)ranging from submicrometer to ***(DEX)with excellent anti-inflammatory properties was used as a model drug to prepare DEX-loaded PLGA particles(DPs).We comprehensively investigated the encapsulation efficiency,cellular uptake and in vitro drug release *** assessment revealed that,in the lipopolysaccharide(LPS)-induced RAW 264.7 cells model,500 nm DPs showed sustained anti-inflammatory *** work provides important information for designing PLGA-based drug delivery systems for biomedical applications.

关键词： DEX-loaded PLGA particles(DPs) sustained release Anti-inflammatory efficacy

Polymeric Hydrogel Nanocapsules: A Thermo and pH Dual-responsive Carrier for sustained Drug release

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Nano-Micro Letters 2014年第3期6卷 200-208页

作者： Jingya Nan Ying Chen Rutian Li Jifu Wang Meihong Liu Chunpeng Wang Fuxiang Chu Institute of Chemical Industry of Forest Products Chinese Academy of Forestry Key Laboratory of Biomass Energy and Material Jiangsu Province National Engineering Laboratory for Biomass Chemical Utilization Key and Open Laboratory on Forest ChemicalEngineering SFA Institute of New Technology Chinese Academy of Forestry The Comprehensive Cancer Center Drum-Tower Hospital of Nanjing University Clinical Cancer Institute of Nanjing University Chinese Academy of Forestry

Hydrogel capsules show attractive prospects in drug delivery recently because of high drug loading and sustained release behavior. In this study we reported a simple and convenient route to fabricate poly(acrylic acid)-poly(N-isopropylacrylamide)(PAA-PNIPAm) hydrogel capsules by using hydroxypropylcellulose-poly(acrylic acid)(HPC-PAA) complexes as the templates. The capsules showed a high drug loading(～280% to the weight of capsules) for Doxorubicin hydrochloride. The release of drug from the capsules was responsive to the temperature and p H of the surroundings, showing a low-rate but sustained release behavior favorable for low-toxic and long-term therapy. Together with the convenient preparation, high drug loading, dual responsivity as well as the sustained release feature, it is implied that this polymeric hydrogel capsule might be a promising candidate for new drug carriers.

关键词： Hydrogel capsules sustained release High drug loading Dual responsivity

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Study on sustained-release Pesticides Blended with Fosthiazate-Stearic Acid/Expanded Perlite

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Journal of Renewable Materials 2023年第1期11卷 257-272页

作者： Huimin Huang Zijun Wu Zhijian Zhou Qiulin Xu Jie Yan Qiaoguang Li College of Chemistry and Chemical Engineering Zhongkai University of Agriculture and EngineeringGuangzhou510225China College of Light Industry and Food Science Zhongkai University of Agriculture and EngineeringGuangzhou510225China

The low utilization rate of pesticides makes the migration of pesticides in water and soil,which brings great harm to the *** development of pesticide carriers with good drug loading capacity and release control abil-ity is an effective method to realize effective utilization of pesticides and reduce pesticide *** this work,fosthiazate-stearic acid/expanded perlite sustained-release particles were successfully prepared by vacuum impregnation using expanded perlite(EP)as carrier,fosthiazate(FOS)as model pesticide and stearic acid(SA)as hydrophobic *** structure and morphology of the samples were studied by BET,FT-IR,TGA,XRD,DSC and *** effects of different mass ratios of FOS to SA on loading capacity and release rate at 24 h were *** sustained release behavior of FOS-SA/EP at different temperatures and pH values was investigated by static dialysis bag *** results showed that FOS and SA were adsorbed in EP pores by physical *** the mass ratios of FOS to SA decreasing from 7:3 to 3:7,the 24 h release rate of FOS-SA/EP decreased from 18.77%to 8.05%,and the drug loading decreased from 461.32 to 130.99 mg/***-SA/EP showed obvious temperature response at 25℃,30℃ and 35℃,the cumulative release rate(CRR)of 200 h were 33.38%,41.50%and 51.17%,*** pH=5,the CRR of FOS was higher than that of pH=7,and the CRR of FOS for 200 h were 49.01%and 30.12%,*** different temperatures and pH=5,the release mechanism of FOS-SA/EP belongs to the Fickian diffusion mechanism;When pH=7,the diffusion mechanism is dominant,and the dissolution mechanism is complementary.

关键词： Expanded perlite fosthiazate stearic acid sustained release release kinetics

sustained-release drug delivery systems for the treatment of glaucoma

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International Journal of Ophthalmology(English edition) 2021年第1期14卷 148-159页

作者： Natasha P.Kesav Cara E.Capitena Young Monica K.Ertel Leonard K.Seibold Malik Y.Kahook Department of Ophthalmology University Hospitals Cleveland Medical CenterClevelandOH 44106USA Department of Ophthalmology University of Colorado School of MedicineCO 80045USA

Glaucoma,a leading cause of irreversible blindness,affects more than 64 million people worldwide and is expected to grow in number due to the aging global population and enhanced methods of *** topical therapies are often effective when used as prescribed,the drawbacks of current medical management methods include poor patient adherence,local and systemic side effects,and in some cases,limited therapeutic *** ocular drug delivery platforms promise to deliver differentiated drug formulations with targeted delivery leveraging patient-independent *** platforms are in various stages of development with promising pre-clinical and clinical *** Bimatoprost sustained release (SR) intracameral implant was approved in the United States in March of 2020,making it the first long-term injectable therapy available for the treatment of *** review aims to provide an update on novel sustained release drug delivery systems that are available today as well as those that might be commercialized in coming years.

关键词： glaucoma drug delivery sustained release

The preparation and the in-vitro pharmacodynamics study of the intracapsular sustained-release preparations for the prevention of posterior capsule opacification

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Asian Journal of Pharmaceutical Sciences 2013年第4期8卷 252-260页

作者： Qian Dong Shaoling Yi Zihang Peng Chunshun Zhao Sun Yat-sen University Guangzhou 510006China Guangdong Food and Drug Vocational College Guangzhou 510520China

Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and *** influence factors and mechanism of drug release were studied in the ***-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release *** of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also *** results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymeriza*** the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the *** mechanism of docetaxel fitted the Higuchi model *** results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous *** elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’*** docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing *** results also lay a theoretical and experimental foundation for the future.

关键词： Docetaxel sustained-release preparations sustained release PCO