Improved drug targeting of cancer cells by utilizing actively targetable folic acid-conjugated albumin nanospheres.


:Folic acid-conjugated albumin nanospheres (FA-AN) have been developed to provide an actively targetable drug delivery system for improved drug targeting of cancer cells with reduced side effects. The nanospheres were prepared by conjugating folic acid onto the surface of albumin nanospheres using 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDAC) as a catalyst. To test the efficacy of these nanospheres as a potential delivery platform, doxorubicin-loaded albumin nanospheres (DOX-AN) and doxorubicin-loaded FA-AN (FA-DOX-AN) were prepared by entrapping DOX (an anthracycline, antibiotic drug widely used in cancer chemotherapy that works by intercalating DNA) into AN and FA-AN nanoparticles. Cell uptake of the DOX was then measured. The results show that FA-AN was incorporated into HeLa cells (tumor cells) only after 2.0h incubation, whereas HeLa cells failed to incorporate albumin nanospheres without conjugated folic acid after 4.0h incubation. When HeLa cells were treated with the DOX-AN, FA-DOX-AN nanoparticles or free DOX, cell viability decreased with increasing culture time (i.e. cell death increases with time) over a 70h period. Cell viability was always the lowest for free DOX followed by FA-DOX-AN4 and then DOX-AN. In a second set of experiments, HeLa cells washed to remove excess DOX after an initial incubation for 2h were incubated for 70h. The corresponding cell viability was slightly higher when the cells were treated with FA-DOX-AN or free DOX whilst cells treated with DOX-AN nanoparticles remained viable. The above experiments were repeated for non-cancerous, aortic smooth muscle cells (AoSMC). As expected, cell viability of the HeLa cells (with FA receptor alpha, FRα) and AoSMC cells (without FRα) decreased rapidly with time in the presence of free DOX, but treatment with FA-DOX-AN resulted in selective killing of the tumor cells. These results indicated that FA-AN may be used as a promising actively targetable drug delivery system to improve drug targeting to cancer cells.


Pharmacol Res


Pharmacological research


Shen Z,Li Y,Kohama K,Oneill B,Bi J




Has Abstract


2011-01-01 00:00:00














  • Effect of tempol on altered angiotensin II and acetylcholine-mediated vascular responses in thoracic aorta isolated from rats with insulin resistance.

    abstract::The altered vascular responses to various vasopressors and relaxants have been well reported in various animal models of hypertension, insulin resistance and diabetes. Though the role of oxidative stress (increased superoxide levels) associated with these altered vascular responses in hyperglycemic/diabetic state is w...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Viswanad B,Srinivasan K,Kaul CL,Ramarao P

    更新日期:2006-03-01 00:00:00

  • Modulation of inflammatory paw oedema by cysteamine in the rat.

    abstract::Cysteamine, a potent somatostatin depletor, was used in the present study to investigate the role of endogenous somatostatin in acute peripheral inflammation. The acute inflammation was induced by intraplantar injection of carrageenan (1%), histamine (5 micromol), or formalin (2.5%) in the rat hind paw. The induced in...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Salam OM

    更新日期:2002-04-01 00:00:00

  • Ozone treatment reduces markers of oxidative and endothelial damage in an experimental diabetes model in rats.

    abstract::Ozone has been used as a therapeutical agent and beneficial effects have been observed. However so far only a few biochemical and pharmacodynamic mechanisms have been elucidated. We demonstrate that controlled ozone administration may promote an oxidative preconditioning or adaptation to oxidative stress, preventing t...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Al-Dalain SM,Martínez G,Candelario-Jalil E,Menéndez S,Re L,Giuliani A,León OS

    更新日期:2001-11-01 00:00:00

  • Biosimilars in rheumatology.

    abstract::Biotechnologicals are an invaluable resource in the treatment of patients with inflammatory rheumatic diseases (IRD) non-responsive or intolerant to conventional therapies. However, they are the main driver for increase in direct costs and represent a significant economic burden to healthcare systems worldwide. Since ...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Araújo FC,Gonçalves J,Fonseca JE

    更新日期:2019-11-01 00:00:00

  • Gastrointestinal effects of single and repeated doses of ferrous sulphate in rats.

    abstract::The gastrointestinal effects of single and repeated administration of ferrous sulphate was evaluated measuring faecal flora modifications and histology of stomach and duodenum of the rat. The acute experiments showed reversible histopathological lesions of stomach and duodenum with iron deposition and increase in faec...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Benoni G,Cuzzolin L,Zambreri D,Donini M,Del Soldato P,Caramazza I

    更新日期:1993-01-01 00:00:00


    abstract::A bovine dopamine transporter (bDAT) cDNA was transfected into CV-1 cells, a cell line that lacks vesicular storage and release mechanisms. Using this cell line, the effects of neuroleptic drugs on DAT-mediated uptake and release of dopamine (DA) were examined. All of the neuroleptic drugs tested, inhibited DA uptakes...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Lee Sh,Oh Dy,Jung Sc,Kim Ym,Cho Hk,Koh Jk,Lee Ys

    更新日期:1997-05-01 00:00:00

  • Ligand autoradiographical quantification of histamine H3 receptor in human dementia with Lewy bodies.

    abstract::Dementia with Lewy bodies (DLB) is a serious age-dependent human neurodegenerative disease, with multiple debilitating symptoms, including dementia, psychosis and significant motor deficits, but with little or no effective treatments. This comparative ligand autoradiographical study has quantified histamine H3 recepto...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Lethbridge NL,Chazot PL

    更新日期:2016-11-01 00:00:00

  • Radiation protective effects of baclofen predicted by a computational drug repurposing strategy.

    abstract::Exposure to ionizing radiation causes damage to living tissues; however, only a small number of agents have been approved for use in radiation injuries. Radioprotector is the primary countermeasure to radiation injury and none radioprotector has indeed reached the drug development stage. Repurposing the long list of a...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Ren L,Xie D,Li P,Qu X,Zhang X,Xing Y,Zhou P,Bo X,Zhou Z,Wang S

    更新日期:2016-11-01 00:00:00

  • Vasoactive eicosanoids in the rat heart: clues to a contributory role of cardiac thromboxane to post-ischaemic hyperaemia.

    abstract::To assess the potential role of vasoactive cardiac eicosanoids in the modulation of coronary flow, we measure thromboxane(TX)B2, 6-keto-prostaglandin(PG)F1 alpha, PGE2 and sulphido-peptide leukotrienes (LTC4, D4, E4) in the coronary effluent of isolated perfused rat heart in both baseline and post-ischaemic conditions...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Giannessi D,Lazzerini G,Sicari R,DeCaterina R

    更新日期:1992-12-01 00:00:00

  • Fish as model in pharmacological and biological research.

    abstract::Fish represent the oldest and most diverse classes of vertebrates, comprising around the 48% of the known member species in the subphylum Vertebrata. There are many scientific fields that use fish as models in research, including respiratory and cardiovascular research, cell culture, ecotoxicology, ageing, pharmacolog...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Bolis CL,Piccolella M,Dalla Valle AZ,Rankin JC

    更新日期:2001-10-01 00:00:00

  • Properties of solubilized and reconstituted A1 adenosine receptors from bovine brain.

    abstract::A simple method for solubilization and reconstitution of the A1 adenosine receptor from bovine brain is presented. Solubilization with CHAPS-phosphatidylcholine (CHAPS/PC) mixture did not alter the binding properties of the A1 adenosine receptor antagonist [3H]-DPCPX. The solubilized receptors were chromatographed on ...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Ragazzi E,Shryock J,Palczewski K

    更新日期:1991-07-01 00:00:00

  • Carnosol-mediated Sirtuin 1 activation inhibits Enhancer of Zeste Homolog 2 to attenuate liver fibrosis.

    abstract::Quiescent hepatic stellate cell (HSC) activation and subsequent conversion into myofibroblasts is the central event in hepatic fibrosis pathogenesis. Epithelial-mesenchymal transition (EMT), another vital participant in liver fibrosis, has the potential to initiate HSC activation, which promotes abundant myofibroblast...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Zhao H,Wang Z,Tang F,Zhao Y,Feng D,Li Y,Hu Y,Wang C,Zhou J,Tian X,Yao J

    更新日期:2018-02-01 00:00:00

  • Meta-analysis on outcome-worsening comorbidities of COVID-19 and related potential drug-drug interactions.

    abstract::Drug-drug interactions (DDI) potentially occurring between medications used in the course of COVID-19 infection and medications prescribed for the management of underlying comorbidities may cause adverse drug reactions (ADRs) contributing to worsening of the clinical outcome in affected patients. First, we conducted a...

    journal_title:Pharmacological research

    pub_type: 杂志文章,meta分析


    authors: Awortwe C,Cascorbi I

    更新日期:2020-11-01 00:00:00

  • ATB-346, a novel hydrogen sulfide-releasing anti-inflammatory drug, induces apoptosis of human melanoma cells and inhibits melanoma development in vivo.

    abstract::Inflammation plays a key role in tumor promotion and development. Indeed, cyclooxygenase-2 (COX-2) expression is strongly associated with different types of cancer. An emerging class of compounds with significant anti-inflammatory properties is the hydrogen sulfide-releasing non-steroidal anti-inflammatory drugs (H2S-...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: De Cicco P,Panza E,Ercolano G,Armogida C,Sessa G,Pirozzi G,Cirino G,Wallace JL,Ianaro A

    更新日期:2016-12-01 00:00:00

  • Vigabatrin does not affect the intestinal absorption of phenytoin in rat duodeno-jejunal loops in situ.

    abstract::The antiepileptic drug vigabatrin (GVG) is known to decrease significantly the serum concentration of concurrently administered phenytoin (PHT) in epileptic patients. To assess a possible mechanism for this interaction, the effect of GVG on the intestinal absorption of PHT was investigated by means of circulation expe...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Tonini M,Gatti G,Manzo L,Olibet G,Coccini T,Perucca E

    更新日期:1992-09-01 00:00:00

  • Dementia of Alzheimer's disease and other neurodegenerative disorders--memantine, a new hope.

    abstract::Alzheimer's disease is the fourth largest cause of death for people over 65 years of age. Dementia of Alzheimer's type is the commonest form of dementia, the other two forms being vascular dementia and mixed dementia. At present, the therapy of Alzheimer's disease is aimed at improving both, cognitive and behavioural ...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Sonkusare SK,Kaul CL,Ramarao P

    更新日期:2005-01-01 00:00:00

  • Evidence of melatonin synthesis and release by mast cells. Possible modulatory role on inflammation.

    abstract::Mast cells take part of armamentarium immunologic for host defense against parasitic and bacterial infections. They are derived from bone marrow progenitors and can be activated by immunological and chemical stimuli in order to get its degranulation. The activation of mast cells generates a signalling cascade leaded t...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Maldonado MD,Mora-Santos M,Naji L,Carrascosa-Salmoral MP,Naranjo MC,Calvo JR

    更新日期:2010-09-01 00:00:00

  • The effects of Kctd12, an auxiliary subunit of GABAB receptor in dentate gyrus on behavioral response to chronic social defeat stress in mice.

    abstract::Adaptive responses to stress are critical to enhance physical and mental well-being, but excessive or prolonged stress may cause inadaptability and increase the risks of psychiatric disorders, such as depression. GABABR signaling is fundamental to brain function and has been identified in neuropsychiatric disorders. K...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Deng SL,Hu ZL,Mao L,Gao B,Yang Q,Wang F,Chen JG

    更新日期:2021-01-01 00:00:00

  • Modulation of intestinal barrier by intestinal microbiota: pathological and therapeutic implications.

    abstract::Mammals and their intestinal microbiota peacefully coexist in a mutualistic relationship. Commensal bacteria play an active role in shaping and modulating physiological processes in the host, which include, but are not restricted to, the immune system and the intestinal barrier. Both play a crucial role in containing ...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Natividad JM,Verdu EF

    更新日期:2013-03-01 00:00:00

  • Effect of Sinpo-Tang on the mast cell-mediated anaphylactic reactions.

    abstract::The herbal formulation Sinpo-Tang (SPT) has long been used for various allergic diseases. We investigated the effect of SPT on the mast cell-mediated anaphylactic reactions in vivo and in vitro murine models. SPT dose dependently inhibited compound 48/80-induced ear swelling response and histamine release. SPT (0.001-...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Jeong HJ,Yi JM,Hong SH,Kong JY,Kim KS,Won JH,Cho KH,Shin TY,Kim HS,Kim HM

    更新日期:2002-11-01 00:00:00

  • TRAIL in oncology: From recombinant TRAIL to nano- and self-targeted TRAIL-based therapies.

    abstract::TNF-related apoptosis-inducing ligand (TRAIL) selectively induces the apoptosis pathway in tumor cells leading to tumor cell death. Because TRAIL induction can kill tumor cells, cancer researchers have developed many agents to target TRAIL and some of these agents have entered clinical trials in oncology. Unfortunatel...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Dianat-Moghadam H,Heidarifard M,Mahari A,Shahgolzari M,Keshavarz M,Nouri M,Amoozgar Z

    更新日期:2020-05-01 00:00:00

  • Mechanopharmacology of Rho-kinase antagonism in airway smooth muscle and potential new therapy for asthma.

    abstract::The principle of mechanopharmacology of airway smooth muscle (ASM) is based on the premise that physical agitation, such as pressure oscillation applied to an airway, is able to induce bronchodilation by reducing contractility and softening the cytoskeleton of ASM. Although the underlying mechanism is not entirely cle...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Wang L,Chitano P,Seow CY

    更新日期:2020-09-01 00:00:00

  • Nadolol-glibenclamide interaction: relevance to carbohydrate metabolism in hyperglycaemic rats.

    abstract::In the present study, hyperglycaemia was induced by intraperitoneal injection of streptozotocin (65 mg/kg). Treatment with glibenclamide (GB) in a dose of 0.45 or 0.9 mg/kg significantly decreased plasma glucose level in a dose-related manner. Administration of nadolol (ND) in a dose of 5 or 10 mg/kg did not affect pl...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Abdel Aziz AH,Moustafa AM,Abd Ellah MF,el-Mazar MA

    更新日期:1996-07-01 00:00:00

  • Effect of nimodipine on systemic, renal, and cerebral haemodynamics after a mild hypoxic-ischaemic insult in newborn piglets.

    abstract::Because many Ca2+ channel blocking agents are known to cause adverse systemic effects, in this study we tested the haemodynamic side effects of nimodipine with and without a mild hypoxic-ischaemic (HI) insult in a newborn piglet model. Fifteen min after completing a brief period of asphyxia we gave i.v. nimodipine as ...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Raju TN,John E,Shankararao R,Fornell L,Vasa R,Abu-Harb M

    更新日期:1996-01-01 00:00:00

  • Dehydroevodiamine and hortiamine, alkaloids from the traditional Chinese herbal drug Evodia rutaecarpa, are IKr blockers with proarrhythmic effects in vitro and in vivo.

    abstract::Evodiae fructus is a widely used herbal drug in traditional Chinese medicine. Evodia extract was found to inhibit hERG channels. The aim of the current study was to identify hERG inhibitors in Evodia extract and to investigate their potential proarrhythmic effects. Dehydroevodiamine (DHE) and hortiamine were identifie...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Baburin I,Varkevisser R,Schramm A,Saxena P,Beyl S,Szkokan P,Linder T,Stary-Weinzinger A,van der Heyden MAG,Houtman M,Takanari H,Jonsson M,Beekman JHD,Hamburger M,Vos MA,Hering S

    更新日期:2018-05-01 00:00:00

  • Influence of a 3-day regimen of azithromycin on the disposition kinetics of cyclosporine A in stable renal transplant patients.

    abstract::Some macrolide antibiotics have been shown to produce significant drug-drug interactions through the inhibition of cytochrome P450 (CYP) enzymes. In renal transplant patients these interactions pose potentially serious problems for the safe administration of cyclosporine A (CSA), a substrate of CYP3A4. The effects of ...

    journal_title:Pharmacological research

    pub_type: 临床试验,杂志文章


    authors: Bachmann K,Jauregui L,Chandra R,Thakker K

    更新日期:2003-06-01 00:00:00

  • Biological characterization of PM226, a chromenoisoxazole, as a selective CB2 receptor agonist with neuroprotective profile.

    abstract::Cannabinoids have emerged as promising neuroprotective agents due to their capability to activate specific targets, which are involved in the control of neuronal homeostasis and survival. Specifically, those ligands that selectively target and activate the CB2 receptor may be useful for their anti-inflammatory and neu...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Gómez-Cañas M,Morales P,García-Toscano L,Navarrete C,Muñoz E,Jagerovic N,Fernández-Ruiz J,García-Arencibia M,Pazos MR

    更新日期:2016-08-01 00:00:00

  • Association between early treatment with Qingfei Paidu decoction and favorable clinical outcomes in patients with COVID-19: A retrospective multicenter cohort study.

    abstract::The coronavirus disease 2019 (COVID-19) epidemic has been almost controlled in China under a series of policies, including "early diagnosis and early treatment". This study aimed to explore the association between early treatment with Qingfei Paidu decoction (QFPDD) and favorable clinical outcomes. In this retrospecti...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Shi N,Liu B,Liang N,Ma Y,Ge Y,Yi H,Wo H,Gu H,Kuang Y,Tang S,Zhao Y,Tong L,Liu S,Zhao C,Chen R,Bai W,Fan Y,Shi Z,Li L,Liu J,Gu H,Zhi Y,Wang Z,Li Y,Li H,Wang J,Jiao L,Tian Y,Xiong Y,Huo R,Zhang X

    更新日期:2020-11-01 00:00:00

  • Lipocalin-2 and iron trafficking in the tumor microenvironment.

    abstract::Iron is an essential element for virtually all organisms. It facilitates cell proliferation and growth but also contributes to major hallmarks of cancer such as tumor initiation, growth, and metastasis. Often, iron handling of tumor cells is disturbed, with altered iron acquisition, efflux, and storage. Targeting pert...

    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


    authors: Jung M,Mertens C,Bauer R,Rehwald C,Brüne B

    更新日期:2017-06-01 00:00:00

  • Allergic contact dermatitis: From pathophysiology to development of new preventive strategies.

    abstract::As the body's first line of defense, the skin is the organ most frequently exposed to chemicals present in personal hygiene products, household products, or materials used in the work environment. In this context, skin disorders account for more than 40 % of all occupational and work-related diseases, constituting a s...

    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Brites GS,Ferreira I,Sebastião AI,Silva A,Carrascal M,Neves BM,Cruz MT

    更新日期:2020-12-01 00:00:00