Moussab/ORKG-training-evaluation-set huggingface dataset:
Research field: Medicinal Chemistry and Pharmaceutics
Title: Oral Drug Delivery Systems for Ulcerative Colitis Therapy: A Comparative Study with Microparticles and Nanoparticles
Abstract: <jats:sec>
<jats:title>Background:</jats:title>
<jats:p> Oral administrations of microparticles (MPs) and nanoparticles (NPs) have
been widely employed as therapeutic approaches for the treatment of ulcerative colitis (UC). However,
no previous study has comparatively investigated the therapeutic efficacies of MPs and NPs.
</jats:p></jats:sec>
<jats:sec>
<jats:title>Methods:</jats:title>
<jats:p> In this study, curcumin (CUR)-loaded MPs (CUR-MPs) and CUR-loaded NPs (CUR-NPs)
were prepared using a single water-in-oil emulsion solvent evaporation technique. Their therapeutic
outcomes against UC were further comparatively studied.
</jats:p></jats:sec>
<jats:sec>
<jats:title>Results:</jats:title>
<jats:p> The resultant spherical MPs and NPs exhibited slightly negative zeta-potential with average
particle diameters of approximately 1.7 &amp;#181;m and 270 nm, respectively. It was found that NPs exhibited
a much higher CUR release rate than MPs within the same period of investigation. In vivo experiments
demonstrated that oral administration of CUR-MPs and CUR-NPs reduced the symptoms
of inflammation in a UC mouse model induced by dextran sulfate sodium. Importantly, CUR-NPs
showed much better therapeutic outcomes in alleviating UC compared with CUR-MPs.
</jats:p></jats:sec>
<jats:sec>
<jats:title>Conclusion:</jats:title>
<jats:p> NPs can improve the anti-inflammatory activity of CUR by enhancing the drug release
and cellular uptake efficiency, in comparison with MPs. Thus, they could be exploited as a promising
oral drug delivery system for effective UC treatment.</jats:p>
</jats:sec>
Extracted statement — Uses drug: Curcumin
Research field: Medicinal Chemistry and Pharmaceutics
Title: PLGA nanoparticles modified with a BBB-penetrating peptide co-delivering Aβ generation inhibitor and curcumin attenuate memory deficits and neuropathology in Alzheimer's disease mice
Abstract: Alzheimer's disease (AD) is the most common form of dementia, characterized by the formation of extracellular senile plaques and neuronal loss caused by amyloid β (Aβ) aggregates in the brains of AD patients. Conventional strategies failed to treat AD in clinical trials, partly due to the poor solubility, low bioavailability and ineffectiveness of the tested drugs to cross the blood-brain barrier (BBB). Moreover, AD is a complex, multifactorial neurodegenerative disease; one-target strategies may be insufficient to prevent the processes of AD. Here, we designed novel kind of poly(lactide-co-glycolic acid) (PLGA) nanoparticles by loading with Aβ generation inhibitor S1 (PQVGHL peptide) and curcumin to target the detrimental factors in AD development and by conjugating with brain targeting peptide CRT (cyclic CRTIGPSVC peptide), an iron-mimic peptide that targets transferrin receptor (TfR), to improve BBB penetration. The average particle size of drug-loaded PLGA nanoparticles and CRT-conjugated PLGA nanoparticles were 128.6 nm and 139.8 nm, respectively. The results of Y-maze and new object recognition test demonstrated that our PLGA nanoparticles significantly improved the spatial memory and recognition in transgenic AD mice. Moreover, PLGA nanoparticles remarkably decreased the level of Aβ, reactive oxygen species (ROS), TNF-α and IL-6, and enhanced the activities of super oxide dismutase (SOD) and synapse numbers in the AD mouse brains. Compared with other PLGA nanoparticles, CRT peptide modified-PLGA nanoparticles co-delivering S1 and curcumin exhibited most beneficial effect on the treatment of AD mice, suggesting that conjugated CRT peptide, and encapsulated S1 and curcumin exerted their corresponding functions for the treatment.
Extracted statement — Uses drug: Curcumin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Curcumin Loaded-PLGA Nanoparticles Conjugated with Tet-1 Peptide for Potential Use in Alzheimer's Disease
Abstract: Alzheimer's disease is a growing concern in the modern world. As the currently available medications are not very promising, there is an increased need for the fabrication of newer drugs. Curcumin is a plant derived compound which has potential activities beneficial for the treatment of Alzheimer's disease. Anti-amyloid activity and anti-oxidant activity of curcumin is highly beneficial for the treatment of Alzheimer's disease. The insolubility of curcumin in water restricts its use to a great extend, which can be overcome by the synthesis of curcumin nanoparticles. In our work, we have successfully synthesized water-soluble PLGA coated- curcumin nanoparticles and characterized it using different techniques. As drug targeting to diseases of cerebral origin are difficult due to the stringency of blood-brain barrier, we have coupled the nanoparticle with Tet-1 peptide, which has the affinity to neurons and possess retrograde transportation properties. Our results suggest that curcumin encapsulated-PLGA nanoparticles are able to destroy amyloid aggregates, exhibit anti-oxidative property and are non-cytotoxic. The encapsulation of the curcumin in PLGA does not destroy its inherent properties and so, the PLGA-curcumin nanoparticles can be used as a drug with multiple functions in treating Alzheimer's disease proving it to be a potential therapeutic tool against this dreaded disease.
Extracted statement — Uses drug: Curcumin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Cyclodextrins in eye drop formulations: enhanced topical delivery of corticosteroids to the eye: Acta
 Ophthalmologica
 Scandinavica
 2002
Abstract: Cyclodextrins are cylindrical oligosaccharides with a lipophilic central cavity and hydrophilic outer surface. They can form water-soluble complexes with lipophilic drugs, which 'hide' in the cavity. Cyclodextrins can be used to form aqueous eye drop solutions with lipophilic drugs, such as steroids and some carbonic anhydrase inhibitors. The cyclodextrins increase the water solubility of the drug, enhance drug absorption into the eye, improve aqueous stability and reduce local irritation. Cyclodextrins are useful excipients in eye drop formulations of various drugs, including steroids of any kind, carbonic anhydrase inhibitors, pilocarpine, cyclosporins, etc. Their use in ophthalmology has already begun and is likely to expand the selection of drugs available as eye drops. In this paper we review the properties of cyclodextrins and their application in eye drop formulations, of which their use in the formulation of dexamethasone eye drops is an example. Cyclodextrins have been used to formulate eye drops containing corticosteroids, such as dexamethasone, with levels of concentration and ocular absorption which, according to human and animal studies, are many times those seen with presently available formulations. Cyclodextrin-based dexamethasone eye drops are well tolerated in the eye and seem to provide a higher degree of bioavailability and clinical efficiency than the steroid eye drop formulations presently available. Such formulations offer the possibility of once per day application of corticosteroid eye drops after eye surgery, and more intensive topical steroid treatment in severe inflammation. While cyclodextrins have been known for more than a century, their use in ophthalmology is just starting. Cyclodextrins are useful excipients in eye drop formulations for a variety of lipophilic drugs. They will facilitate eye drop formulations for drugs that otherwise might not be available for topical use, while improving absorption and stability and decreasing local irritation.
Extracted statement — Uses drug: Dexamethasone
Research field: Medicinal Chemistry and Pharmaceutics
Title: Topical and systemic absorption in delivery of dexamethasone to the anterior and posterior segments of the eye
Abstract: PURPOSE This study aimed to: (1) determine the relative efficiencies of topical and systemic absorption of drugs delivered by eyedrops to the anterior and posterior segments of the eye; (2) establish whether dexamethasone-cyclodextrin eyedrops deliver significant levels of drug to the retina and vitreous in the rabbit eye, and (3) compare systemic absorption following topical application to the eye versus intranasal or intravenous delivery. METHODS In order to distinguish between topical and systemic absorption in the eye, we applied 0.5% dexamethasone-cyclodextrin eyedrops to one (study) eye of rabbits and not to the contralateral (control) eye. Drug levels were measured in each eye. The study eye showed the result of the combination of topical and systemic absorption, whereas the control eye showed the result of systemic absorption only. Systemic absorption was also examined after intranasal and intravenous administration of the same dose of dexamethasone. RESULTS In the aqueous humour dexamethasone levels were 170 +/- 76 ng/g (mean +/- standard deviation) in the study eye and 6 +/- 2 ng/g in the control eye. Similar ratios were seen in the iris and ciliary body. In the retina the dexamethasone level was 33 +/- 7 ng/g in the study eye and 14 +/- 3 ng/g in the control eye. Similar ratios were seen in the vitreous humour. Systemic absorption was similar from ocular, intranasal and intravenous administration. CONCLUSIONS Absorption after topical application dominates in the anterior segment. Topical absorption also plays a significant role in delivering dexamethasone to the posterior segment of the rabbit eye. In medication administered to the retina, 40% of the drug reaches the retina via the systemic route and 60% via topical penetration. Dexamethasone-cyclodextrin eyedrops deliver a significant amount of drug to the rabbit retina.
Extracted statement — Uses drug: Dexamethasone
Research field: Medicinal Chemistry and Pharmaceutics
Title: Superparamagnetic Iron Oxide–enhanced MR Imaging of Head and Neck Lymph Nodes
Abstract: PURPOSE To compare findings on superparamagnetic iron oxide (SPIO)-enhanced magnetic resonance (MR) images of the head and neck with those from resected lymph node specimens and to determine the effect of such imaging on surgical planning in patients with histopathologically proved squamous cell carcinoma of the head and neck. MATERIALS AND METHODS Thirty patients underwent MR imaging with nonenhanced and SPIO-enhanced (2.6 mg Fe/kg intravenously) T1-weighted (500/15 [repetition time msec/echo time msec]) and T2-weighted (1,900/80) spin-echo and T2-weighted gradient-echo (GRE) (500/15, 15 degrees flip angle) sequences. Signal intensity decrease was measured, and visual analysis was performed. Surgical plans were modified, if necessary, according to MR findings. Histopathologic and MR findings were compared. RESULTS Histopathologic evaluation of 1,029 lymph nodes revealed 69 were metastatic. MR imaging enabled detection of 59 metastases. Regarding lymph node levels, MR diagnosis was correct in 26 of 27 patients who underwent surgery: Only one metastasis was localized in level II with MR imaging, whereas histopathologic evaluation placed it at level III. Extent of surgery was changed in seven patients. SPIO-enhanced T2-weighted GRE was the best sequence for differentiating between benign and malignant lymph nodes. CONCLUSION SPIO-enhanced MR imaging has an important effect on planning the extent of surgery. On a patient basis, SPIO-enhanced MR images compared well with resected specimens.
Extracted statement — Field of application: Diagnosis
Research field: Medicinal Chemistry and Pharmaceutics
Title: Lactoferrin bioconjugated solid lipid nanoparticles: a new drug delivery system for potential brain targeting
Abstract: Abstract Background: Delivery of drugs to brain is a subtle task in the therapy of many severe neurological disorders. Solid lipid nanoparticles (SLN) easily diffuse the blood–brain barrier (BBB) due to their lipophilic nature. Furthermore, ligand conjugation on SLN surface enhances the targeting efficiency. Lactoferin (Lf) conjugated SLN system is first time attempted for effective brain targeting in this study. Purpose: Preparation of Lf-modified docetaxel (DTX)-loaded SLN for proficient delivery of DTX to brain. Methods: DTX-loaded SLN were prepared using emulsification and solvent evaporation method and conjugation of Lf on SLN surface (C-SLN) was attained through carbodiimide chemistry. These lipidic nanoparticles were evaluated by DLS, AFM, FTIR, XRD techniques and in vitro release studies. Colloidal stability study was performed in biologically simulated environment (normal saline and serum). These lipidic nanoparticles were further evaluated for its targeting mechanism for uptake in brain tumour cells and brain via receptor saturation studies and distribution studies in brain, respectively. Results: Particle size of lipidic nanoparticles was found to be optimum. Surface morphology (zeta potential, AFM) and surface chemistry (FTIR) confirmed conjugation of Lf on SLN surface. Cytotoxicity studies revealed augmented apoptotic activity of C-SLN than SLN and DTX. Enhanced cytotoxicity was demonstrated by receptor saturation and uptake studies. Brain concentration of DTX was elevated significantly with C-SLN than marketed formulation. Conclusions: It is evident from the cytotoxicity, uptake that SLN has potential to deliver drug to brain than marketed formulation but conjugating Lf on SLN surface (C-SLN) further increased the targeting potential for brain tumour. Moreover, brain distribution studies corroborated the use of C-SLN as a viable vehicle to target drug to brain. Hence, C-SLN was demonstrated to be a promising DTX delivery system to brain as it possessed remarkable biocompatibility, stability and efficacy than other reported delivery systems.
Extracted statement — Uses drug: Docetaxel
Research field: Medicinal Chemistry and Pharmaceutics
Title: Comparison, synthesis and evaluation of anticancer drug-loaded polymeric nanoparticles on breast cancer cell lines
Abstract: Breast cancer is a major form of cancer, with a high mortality rate in women. It is crucial to achieve more efficient and safe anticancer drugs. Recent developments in medical nanotechnology have resulted in novel advances in cancer drug delivery. Cisplatin, doxorubicin, and 5-fluorouracil are three important anti-cancer drugs which have poor water-solubility. In this study, we used cisplatin, doxorubicin, and 5-fluorouracil-loaded polycaprolactone-polyethylene glycol (PCL-PEG) nanoparticles to improve the stability and solubility of molecules in drug delivery systems. The nanoparticles were prepared by a double emulsion method and characterized with Fourier Transform Infrared (FTIR) spectroscopy and Hydrogen-1 nuclear magnetic resonance (1HNMR). Cells were treated with equal concentrations of cisplatin, doxorubicin and 5-fluorouracil-loaded PCL-PEG nanoparticles, and free cisplatin, doxorubicin and 5-fluorouracil. The 3-[4,5-dimethylthiazol-2yl]-2,5-diphenyl tetrazolium bromide (MTT) assay confirmed that cisplatin, doxorubicin, and 5-fluorouracil-loaded PCL-PEG nanoparticles enhanced cytotoxicity and drug delivery in T47D and MCF7 breast cancer cells. However, the IC50 value of doxorubicin was lower than the IC50 values of both cisplatin and 5-fluorouracil, where the difference was statistically considered significant (p˂0.05). However, the IC50 value of all drugs on T47D were lower than those on MCF7.
Extracted statement — keywords: Doxorubicin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Comparison, synthesis and evaluation of anticancer drug-loaded polymeric nanoparticles on breast cancer cell lines
Abstract: Breast cancer is a major form of cancer, with a high mortality rate in women. It is crucial to achieve more efficient and safe anticancer drugs. Recent developments in medical nanotechnology have resulted in novel advances in cancer drug delivery. Cisplatin, doxorubicin, and 5-fluorouracil are three important anti-cancer drugs which have poor water-solubility. In this study, we used cisplatin, doxorubicin, and 5-fluorouracil-loaded polycaprolactone-polyethylene glycol (PCL-PEG) nanoparticles to improve the stability and solubility of molecules in drug delivery systems. The nanoparticles were prepared by a double emulsion method and characterized with Fourier Transform Infrared (FTIR) spectroscopy and Hydrogen-1 nuclear magnetic resonance (1HNMR). Cells were treated with equal concentrations of cisplatin, doxorubicin and 5-fluorouracil-loaded PCL-PEG nanoparticles, and free cisplatin, doxorubicin and 5-fluorouracil. The 3-[4,5-dimethylthiazol-2yl]-2,5-diphenyl tetrazolium bromide (MTT) assay confirmed that cisplatin, doxorubicin, and 5-fluorouracil-loaded PCL-PEG nanoparticles enhanced cytotoxicity and drug delivery in T47D and MCF7 breast cancer cells. However, the IC50 value of doxorubicin was lower than the IC50 values of both cisplatin and 5-fluorouracil, where the difference was statistically considered significant (p˂0.05). However, the IC50 value of all drugs on T47D were lower than those on MCF7.
Extracted statement — Uses drug: Doxorubicin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Co-delivery of doxorubicin and siRNA for glioma therapy by a brain targeting system: angiopep-2-modified poly(lactic-co-glycolic acid) nanoparticles
Abstract: Abstract It is very challenging to treat brain cancer because of the blood–brain barrier (BBB) restricting therapeutic drug or gene to access the brain. In this research project, angiopep-2 (ANG) was used as a brain-targeted peptide for preparing multifunctional ANG-modified poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs), which encapsulated both doxorubicin (DOX) and epidermal growth factor receptor (EGFR) siRNA, designated as ANG/PLGA/DOX/siRNA. This system could efficiently deliver DOX and siRNA into U87MG cells leading to significant cell inhibition, apoptosis and EGFR silencing in vitro. It demonstrated that this drug system was capable of penetrating the BBB in vivo, resulting in more drugs accumulation in the brain. The animal study using the brain orthotopic U87MG glioma xenograft model indicated that the ANG-targeted co-delivery of DOX and EGFR siRNA resulted in not only the prolongation of the life span of the glioma-bearing mice but also an obvious cell apoptosis in glioma tissue.
Extracted statement — Uses drug: Doxorubicin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Enhanced Intracellular Delivery and Chemotherapy for Glioma Rats by Transferrin-Conjugated Biodegradable Polymersomes Loaded with Doxorubicin
Abstract: A brain drug delivery system for glioma chemotherapy based on transferrin-conjugated biodegradable polymersomes, Tf-PO-DOX, was made and evaluated with doxorubicin (DOX) as a model drug. Biodegradable polymersomes (PO) loaded with doxorubicin (DOX) were prepared by the nanoprecipitation method (PO-DOX) and then conjugated with transferrin (Tf) to yield Tf-PO-DOX with an average diameter of 107 nm and surface Tf molecule number per polymersome of approximately 35. Compared with PO-DOX and free DOX, Tf-PO-DOX demonstrated the strongest cytotoxicity against C6 glioma cells and the greatest intracellular delivery. It was shown in pharmacokinetic and brain distribution experiments that Tf-PO significantly enhanced brain delivery of DOX, especially the delivery of DOX into brain tumor cells. Pharmacodynamics results revealed a significant reduction of tumor volume and a significant increase of median survival time in the group of Tf-PO-DOX compared with those in saline control animals, animals treated with PO-DOX, and free DOX solution. By terminal deoxynucleotidyl transferase-mediated dUTP nick-end-labeling, Tf-PO-DOX could extensively make tumor cell apoptosis. These results indicated that Tf-PO-DOX could significantly enhance the intracellular delivery of DOX in glioma and the chemotherapeutic effect of DOX for glioma rats.
Extracted statement — Uses drug: Doxorubicin
Research field: Medicinal Chemistry and Pharmaceutics
Title: Evaluation of psoralen ethosomes for topical delivery in rats by using in vivo microdialysis
Abstract: This study aimed to improve skin permeation and deposition of psoralen by using ethosomes and to investigate real-time drug release in the deep skin in rats. We used a uniform design method to evaluate the effects of different ethosome formulations on entrapment efficiency and drug skin deposition. Using in vitro and in vivo methods, we investigated skin penetration and release from psoralen-loaded ethosomes in comparison with an ethanol tincture. In in vitro studies, the use of ethosomes was associated with a 6.56-fold greater skin deposition of psoralen than that achieved with the use of the tincture. In vivo skin microdialysis showed that the peak concentration and area under the curve of psoralen from ethosomes were approximately 3.37 and 2.34 times higher, respectively, than those of psoralen from the tincture. Moreover, it revealed that the percutaneous permeability of ethosomes was greater when applied to the abdomen than when applied to the chest or scapulas. Enhanced permeation and skin deposition of psoralen delivered by ethosomes may help reduce toxicity and improve the efficacy of long-term psoralen treatment.
Extracted statement — Type of Lipid-based nanoparticle: Ethosomes
Research field: Medicinal Chemistry and Pharmaceutics
Title: Enhanced delivery of etoposide across the blood–brain barrier to restrain brain tumor growth using melanotransferrin antibody- and tamoxifen-conjugated solid lipid nanoparticles
Abstract: Abstract Melanotransferrin antibody (MA) and tamoxifen (TX) were conjugated on etoposide (ETP)-entrapped solid lipid nanoparticles (ETP-SLNs) to target the blood–brain barrier (BBB) and glioblastom multiforme (GBM). MA- and TX-conjugated ETP-SLNs (MA–TX–ETP–SLNs) were used to infiltrate the BBB comprising a monolayer of human astrocyte-regulated human brain-microvascular endothelial cells (HBMECs) and to restrain the proliferation of malignant U87MG cells. TX-grafted ETP-SLNs (TX–ETP–SLNs) significantly enhanced the BBB permeability coefficient for ETP and raised the fluorescent intensity of calcein-AM when compared with ETP-SLNs. In addition, surface MA could increase the BBB permeability coefficient for ETP about twofold. The viability of HBMECs was higher than 86%, suggesting a high biocompatibility of MA–TX–ETP-SLNs. Moreover, the efficiency in antiproliferation against U87MG cells was in the order of MA–TX–ETP-SLNs > TX–ETP-SLNs > ETP-SLNs > SLNs. The capability of MA–TX–ETP-SLNs to target HBMECs and U87MG cells during internalization was verified by immunochemical staining of expressed melanotransferrin. MA–TX–ETP-SLNs can be a potent pharmacotherapy to deliver ETP across the BBB to GBM.
Extracted statement — Uses drug: Etoposide
Research field: Medicinal Chemistry and Pharmaceutics
Title: Solid-state characterization of Felodipine–Soluplus amorphous solid dispersions
Abstract: Abstract The aim of the current study is to develop amorphous solid dispersion (SD) via hot melt extrusion technology to improve the solubility of a water-insoluble compound, felodipine (FEL). The solubility was dramatically increased by preparation of amorphous SDs via hot-melt extrusion with an amphiphilic polymer, Soluplus® (SOL). FEL was found to be miscible with SOL by calculating the solubility parameters. The solubility of FEL within SOL was determined to be in the range of 6.2–9.9% (w/w). Various techniques were applied to characterize the solid-state properties of the amorphous SDs. These included Fourier Transform Infrared Spectrometry spectroscopy and Raman spectroscopy to detect the formation of hydrogen bonding between the drug and the polymer. Scanning electron microscopy was performed to study the morphology of the SDs. Among all the hot-melt extrudates, FEL was found to be molecularly dispersed within the polymer matrix for the extrudates containing 10% drug, while few small crystals were detected in the 30 and 50% extrudates. In conclusion, solubility of FEL was enhanced while a homogeneous SD was achieved for 10% drug loading.
Extracted statement — Uses drug: Felodipine