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pegylation in anti-cancer therapy: An overview

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Asian Journal of Pharmaceutical Sciences 2016年第3期11卷 337-348页

作者： Prajna Mishra Bismita Nayak R.K.Dey Centre for Applied Chemistry Central University of Jharkhand Department of Life Science National Institute of Technology

Advanced drug delivery systems using poly(ethylene glycol)(PEG) is an important development in anti-cancer therapy. pegylation has the ability to enhance the retention time of the therapeutics like proteins, enzymes small molecular drugs, liposomes and nanoparticles by protecting them against various degrading mechanisms active inside a tissue or cell, which consequently improves their therapeutic potential. pegylation effectively alters the pharmacokinetics(PK) of a variety of drugs and dramatically improves the pharmaceutical values;recent development of which includes fabrication of stimuli-sensitive polymers/smart polymers and polymeric micelles to cope of with the pathophysiological environment of targeted site with less toxic effects and more effectiveness. This overview discusses pegylation involving proteins, enzymes, low molecular weight drugs, liposomes and nanoparticles that has been developed, clinically tried for anti-cancer therapy during the last decade.

关键词： PEG pegylation Targeted drug delivery Polymers

Dynamic micelles with detachable pegylation at tumoral extracellular pH for enhanced chemotherapy

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Asian Journal of Pharmaceutical Sciences 2020年第6期15卷 728-738页

作者： Guoqing Yan Panpan Zhang Jun Wang Xin Wang Rupei Tang Engineering Research Centerfor Biomedical Materials School of Life ScienceAnhui UniversityHefei 230601China

Although surface pegylation of nanomedicines can decrease serum protein adsorption in vivo,it also blocks uptake by tumor cells.This dilemma could be overcome by employing detachably PEGylated strategy at tumoral extracellular microenvironment to achieve improved cellular uptake while prolonged circulation times.Herein,the amphiphilic graft copolymers with p H-sensitive ortho ester-linked m PEG in side chains and polyurethanes in backbone,can self-assemble into the free and doxorubicin(DOX)-loaded micelles.The p H-sensitive micelles could undergo several characteristics as follows:(i)PEGylated shells for stability in sodium dodecyl sulfonate(SDS)solution;(ii)De pegylation via degradation of ortho ester linkages at tumoral extracellular pH(6.5)for gradually dynamic size changes and effective release of DOX;and(iii)enhanced cellular uptake and cytotoxicity via positive DOX.Moreover,the dynamic micelles with detachable pegylation could quickly penetrate the centers of SH-SY5 Y multicellular spheroids(MCs)and strongly inhibit tumor growth in vitro and in vivo,and might be considered as promising and effective drug carriers in tumor therapy.

关键词： Micelles Ortho ester pegylation Size transition Antitumor

Site-specific pegylation of Human Growth Hormone by Mutated Sortase A

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Chemical Research in Chinese Universities 2018年第3期34卷 428-433页

作者： SHI Hui SHI Qingyang James T. OSWALD GAO Ying LI Leijiao LI Yunhui School of Chemistry & Environmental Engineering Changchun University of Science & Technology Changchun 130022 P R. China Key Laboratory of Regenerative Biology of the Chinese Academy of Sciences Guangdong Provincial Key Laboratory of Stem Cells and Regenerative Medicine Guangzhou Institutes of Biomedicine and Health Chinese Academy of Sciences Guangzhou 510530 P. R. China University of Chinese Academy of Sciences Beijing P. R. China 100049 Centre for Reproductive Medicine Centre for Prenatal Diagnosis the First Hospital of Jilin Universi(y. Changchun 130021 P. R. China School of Nanoteehnology & Chemical Engineering University of Waterloo Waterloo ON Canada

Human growth hormone（hGH）, a classic therapeutic protein, which promotes growth and wound healing, is released from the pituitary gland. As a protein drug, its short half-life is its main barrier to therapeutic efficacy. Various strategies have been designed to prolong its serum half-life, the most conunon of which is the conjugation with polyethylene glycol（PEG）, as this has been shown to significantly extend protein＇s serum half-life. However, pegylation often results in random conjugation, which can lead to impaired protein function and hinder purification, characterization and evaluation of the PEGylated protein. Therefore, site specific pegylation is a promising direction for PEG-protein conjugation. Here we took advantages of the mutated sortase A（7M） enzyme, which can enzymati- cally ligate the universal a-amino acids to a C-terminal tagged protein. This then allows specific modification of the C-terminal of hGH with PEG. This site-specific bound PEG-hGH has similar efficacy, receptor binding and cell proliferation as wild-type hGH; however, pharmacokinetic analysis demonstrates that its serum half-life is almost 24 times that of wild-type hGH. Herein, we provided a promising advancement in the development of site specific PEGylated therapeutic proteins.

关键词： Human growth hormone pegylation Site specific modification

Circumvent pegylation dilemma by implementing matrix metalloproteinase-responsive chemistry for promoted tumor gene therapy

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Chinese Chemical Letters 2020年第12期31卷 3143-3148页

作者： Jingyun Wang Hao Wang Hongyan Cui Peng Sun Xi Yang Qixian Chen State Key Laboratory of Fine Chemicals Dalian University of TechnologyDalian 116024China School of Bioengineering Dalian University of TechnologyDalian 116024China Department of Neurosurgery Renji HospitalSchool of MedicineShanghai Jiao Tong UniversityShanghai 200127China

Surface modification by poly(ethylene glycol)(pegylation)has been acknowledged as a powerful strategy in minimizing non-specific reactions for biomedical devices.Once applied into manufacture of drug/gene delivery systems,pegylation has demonstrated to significantly improve their biocompatibility and stealthiness in physiological environment.Nonetheless,reluctant cell membrane affinities thus cellular uptake efficiencies owing to pegylation brought up further issues that are imperative to be resolved.Pertain to this pegylation dilemma,we attempted to introduce peptide(GPLGVRG)linkage between block copolymer of PEG-poly{N’-[N-(2-aminoethyl)-2-aminoethyl]aspartamide}PAsp(DET),wherein the cationic PAsp(DET)could self-assemble with pDNA into nanoscaled complex core.Noteworthy was the peptide linkage whose amino acids sequence could be specifically recognized and degraded by matrix metalloproteinases(MMPs)(overexpressed in extracellular milieu of tumors).Therefore,our subsequent studies validated facile detachment of pegylation from the aforementioned polyplex micelles upon treatment of MMPs,which elicited improved cytomembrane affinities and cellular uptake efficiencies.In addition,promoted escape from endosome entrapment was also confirmed through direct endosome membrane destabilization by PAsp(DET),which was further elucidated to be attributable to depegylation as well as elevated charged density of PAsp(DET)in acidic endosomes.These benefits from depegylation eventually contributed to promoted gene expression at the affected cells and potent tumor growth suppression based on anti-angiogenic approach.Therefore,our developed strategy has provided a facile approach in overcoming the dilemma of pegylation,which could be informative in design of drug/gene delivery systems.

关键词： pegylation Tumor Polyplex micelle Gene delivery system Matrix metalloproteinase

Surface pegylation of hollow mesoporous silica nanoparticles via aminated intermediate

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Progress in Natural Science:Materials International 2019年第6期29卷 612-616页

作者： Thi Ngoc Tram Nguyen Diem-Huong Nguyen-Tran Long Giang Bach Tran Hoang Du Truong Ngoc Thuy Trang Le Dai Hai Nguyen Tra Vinh University Institute of Applied Materials Science Vietnam Academy of Science and Technology Graduate University of Science and Technology Vietnam Academy of Science and Technology Nguyen Tat Thanh University 5. Institute of Research and Development Duy Tan University

A hybrid of organic/inorganic system, hollow mesoporous silica nanoparticles functionalized with poly(ethylene glycol), was synthesized in the presence of coupling agent and aminated ends. Doxorubicin(DOX) was used as a model drug to evaluate the effect of pegylation on the loading capacity and release pattern of the system.Characterization with transmission electron microscopy(TEM) and scanning electron microscopy(SEM), X-ray diffraction(XRD), nitrogen adsorption-desorption, thermogravimetric analysis(TGA) and Fourier transformed infrared(FTIR) confirmed the PEG conjugation, as well as the amorphous mesoporous nature of the synthesized particles. Due to the capping effect of PEG molecules over the pores in the silica structure, the synthesized system was able to retain higher amount of cargo and establish a controlled manner when releasing.

关键词： Hollow mesoporous silica nanoparticles mPEG pegylation Surface modification

Accurate construction of cell membrane biomimetic graphene nanodecoys via purposeful surface engineering to improve screening efficiency of active components of traditional Chinese medicine

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Acta Pharmaceutica Sinica B 2022年第1期12卷 394-405页

作者： Qi Hu Lanlan Jia Xiaolin Zhang Aihong Zhu Sicen Wang Xiaoyu Xie School of Pharmacy Health Science CenterXi’an Jiaotong UniversityXi'an 710061China Shaanxi Engineering Research Center of Cardiovascular Drugs Screening&Analysis Xi'an 710061China

Biomimetic nanoengineering presents great potential in biomedical research by integrating cell membrane(CM) with functional nanoparticles. However, preparation of CM biomimetic nanomaterials for custom applications that can avoid the aggregation of nanocarriers while maintaining the biological activity of CM remains a challenge. Herein, a high-performance CM biomimetic graphene nanodecoy was fabricated via purposeful surface engineering, where polyethylene glycol(PEG) was used to modifying magnetic graphene oxide(MGO) to improve its stability in physiological solution, so as to improve the screening efficiency to active components of traditional Chinese medicine(TCM). With this strategy, the constructed PEGylated MGO(PMGO) could keep stable at least 10 days, thus improving the CM coating efficiency. Meanwhile, by taking advantage of the inherent ability of He La cell membrane(HM) to interact with specific ligands, HM-camouflaged PMGO showed satisfied adsorption capacity(116.2 mg/g) and selectivity. Finally, three potential active components, byakangelicol, imperatorin,and isoimperatorin, were screened from Angelica dahurica, whose potential antiproliferative activity were further validated by pharmacological studies. These results demonstrated that the purposeful surfaceengineering is a promising strategy for the design of efficient CM biomimetic nanomaterials, which will promote the development of active components screening in TCM.

关键词： Cell membrane Biomimetic nanoengineering Purposeful surface engineering Graphene oxide Dispersity Active components screening Traditional Chinese medicine pegylation

Liposome based drug delivery as a potential treatment option for Alzheimer’s disease

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Neural Regeneration Research 2022年第6期17卷 1190-1198页

作者： Carely Hernandez Surabhi Shukla Department of Pharmaceutical Sciences College of PharmacyLarkin UniversityMiamiFLUSA

Alzheimer’s disease is a neurodegenerative condition leading to atrophy of the brain and robbing nearly 5.8 million individuals in the United States age 65 and older of their cognitive functions.Alzheimer’s disease is associated with dementia and a progressive decline in memory,thinking,and social skills,eventually leading to a point that the individual can no longer perform daily activities independently.Currently available drugs on the market temporarily alleviate the symptoms,however,they are not successful in slowing down the progression of Alzheimer’s disease.Treatment and cures have been constricted due to the difficulty of drug delivery to the blood-brain barrier.Several studies have led to identification of vesicles to transport the necessary drugs through the blood-brain barrier that would typically not achieve the targeted area through systemic delivered medications.Recently,liposomes have emerged as a viable drug delivery agent to transport drugs that are not able to cross the blood-brain barrier.Liposomes are being used as a component of nanoparticle drug delivery;due to their biocompatible nature;and possessing the capability to carry both lipophilic and hydrophilic therapeutic agents across the blood brain barrier into the brain cells.Studies indicate the importance of liposomal based drug delivery in treatment of neurodegenerative disorders.The idea is to encapsulate the drugs inside the properly engineered liposome to generate a response of treatment.Liposomes are engineered to target specific diseased moieties and also several surface modifications of liposomes are under research to create a clinical path to the management of Alzheimer’s disease.This review deals with Alzheimer’s disease and emphasize on challenges associated with drug delivery to the brain,and how liposomal drug delivery can play an important role as a drug delivery method for the treatment of Alzheimer’s disease.This review also sheds some light on variation of liposomes.Additionally,it emphasizes on the liposomal formulations

关键词： Alzheimer’s disease beta-amyloid blood-brain barrier brain delivery drug delivery systems encapsulated drugs liposomes nanoparticles neurodegenerative diseases pegylation targeted delivery tau

Development of a novel multi-functional integrated bioconjugate effectively targeting K-Ras mutant pancreatic cancer

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Journal of Pharmaceutical Analysis 2022年第2期12卷 232-242页

作者： Yang-Yang Wang Liang Li Xiu-Jun Liu Qing-Fang Miao Yi Li Meng-Ran Zhang Yong-Su Zhen Department of Pediatric Oncology Tianjin Medical University Cancer Institute and HospitalTianjin300060China NHC Key Laboratory of Biotechnology of Antibiotics Department of OncologyInstitute of Medicinal BiotechnologyChinese Academy of Medical Sciences&Peking Union Medical CollegeBeijing100050China

Folate receptor(FR)overexpression occurs in a variety of cancers,including pancreatic cancer.In addition,enhanced macropinocytosis exists in K-Ras mutant pancreatic cancer.Furthermore,the occurrence of intensive desmoplasia causes a hypoxic microenvironment in pancreatic cancer.In this study,a novel FR-directed,macropinocytosis-enhanced,and highly cytotoxic bioconjugate folate(F)-human serum albumin(HSA)-apoprotein of lidamycin(LDP)-active enediyne(AE)derived from lidamycin was designed and prepared.F-HSA-LDP-AE consisted of four moieties:F,HSA,LDP,and AE.F-HSA-LDP presented high binding efficiency with the FR and pancreatic cancer cells.Its uptake in wild-type cells was more extensive than in K-Ras mutant-type cells.By in vivo optical imaging,F-HSA-LDP displayed prominent tumor-specific biodistribution in pancreatic cancer xenograft-bearing mice,showing clear and lasting tumor localization for 360 h.In the MTT assay,F-HSA-LDP-AE demonstrated potent cytotoxicity in three types of pancreatic cancer cell lines.It also induced apoptosis and caused G2/M cell cycle arrest.F-HSALDP-AE markedly suppressed the tumor growth of AsPc-1 pancreatic cancer xenografts in athymic mice.At well-tolerated doses of 0.5 and 1 mg/kg,(i.v.,twice),the inhibition rates were 91.2%and 94.8%,respectively(P<0.01).The results of this study indicate that the F-HSA-LDP multi-functional bioconjugate might be effective for treating K-Ras mutant pancreatic cancer.

关键词： Pancreatic cancer Folate receptor Multi-functional Macropinocytosis-enhanced Bioconjugate K-Ras pegylation

Impact of the amount of PEG on prodrug nanoassemblies for efficient cancer therapy

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Asian Journal of Pharmaceutical Sciences 2022年第2期17卷 241-252页

作者： Yaqiao Li Lingxiao Li Qianhui Jin Tian Liu Jin Sun Yongjun Wang Zhijun Yang Zhonggui He Bingjun Sun Wuya College of Innovation Shenyang Pharmaceutical UniversityShenyang 110016China School of Chinese Medicine Hong Kong Baptist UniversityHong Kong 999077China

pegylation has been widely used to improve the pharmacokinetic properties of prodrug self-assembled nanoparticles(prodrug-SANPs).However,the impacts of the amount of PEG on the self-assemble stability,cellular uptake,pharmacokinetics,and antitumor efficacy of prodrug-SANPs are still unknown.Herein,selenoether bond bridged docetaxel dimeric prodrug was synthesized as the model prodrug.Five prodrug-SANPs were designed by using different mass ratios of prodrugs to PEG(W_(prodrug)/W_(DSPE-mPEG2000)=10:0,9:1,8:2,7:3 and 6:4),and defined as Pure drug NPs,9:1NPs,8:2NPs,7:3 NPs and 6:4 NPs,respectively.Interestingly,8:2 NPs formed the most compact nanostructure,thus improving the self-assemble stability and pharmacokinetics behavior.In addition,the difference of these prodrug-SANPs in cellular uptake was investigated,and the influence of PEG on cytotoxicity and antitumor efficacy was also clarified in details.The 8:2 NPs exhibited much better antitumor efficacy than other prodrug-SANPs and even commercial product.Our findings demonstrated the pivotal role of the amount of PEG on prodrug-SANPs.

关键词： pegylation Prodrug Self-assembly nanoparticles Docetaxel Oxidation responsive