LIVIVO - Search results -

Search results

Result 1 - 10 of total 19

Search options

Article ; Online: Current status of the development of intravesical drug delivery systems for the treatment of bladder cancer.

Yoon, Ho Yub / Yang, Hee Mang / Kim, Chang Hyun / Goo, Yoon Tae / Kang, Myung Joo / Lee, Sangkil / Choi, Young Wook

2020 Volume 17, Issue 11, Page(s) 1555–1572

Abstract: Introduction: Intravesical instillation is preferred over the systemic route of administration, as an efficient route of drug administration to treat bladder cancer. However, the periodic voiding of urine washes out the instilled drugs, eventually ... ...

Abstract	Introduction: Intravesical instillation is preferred over the systemic route of administration, as an efficient route of drug administration to treat bladder cancer. However, the periodic voiding of urine washes out the instilled drugs, eventually resulting in reduced drug exposure. Moreover, the presence of the bladder permeability barrier limits drug permeation into tumor tissues. It is therefore important to develop a novel delivery system that not only promotes prolonged retention of drugs in the bladder but also enables drugs to penetrate the barrier. Areas covered: This review addresses the limitations of conventional therapeutic regimens and reports the use of polymeric hydrogels and nano/microcarriers for enhanced intravesical drug delivery in bladder cancer. Strategies to prolong residence time in the bladder and enhance cell penetration and target-cell specificity are discussed. Expert opinion: Although promising results have been obtained in the field of intravesical drug delivery, numerous questions remain unanswered in terms of therapeutic efficacy. Specialized function covering extended drug exposure and/or enhanced drug uptake should be considered. Assessment protocols that adequately mimic the human bladder environment in vitro and in vivo experiments are needed to expedite formulation development.
MeSH term(s)	Administration, Intravesical ; Animals ; Drug Delivery Systems ; Humans ; Hydrogels ; Permeability ; Polymers/chemistry ; Urinary Bladder Neoplasms/drug therapy
Chemical Substances	Hydrogels ; Polymers
Language	English
Publishing date	2020-09-04
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2167286-6
ISSN	1744-7593 ; 1742-5247
ISSN (online)	1744-7593
ISSN	1742-5247
DOI	10.1080/17425247.2020.1810016
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 6012: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

Details ▾

Article ; Online: Optimization of solid self-dispersing micelle for enhancing dissolution and oral bioavailability of valsartan using Box-Behnken design.

Goo, Yoon Tae / Park, Sun Young / Chae, Bo Ram / Yoon, Ho Yub / Kim, Chang Hyun / Choi, Ji Yeh / Song, Seh Hyon / Choi, Young Wook

International journal of pharmaceutics

2020 Volume 585, Page(s) 119483

Abstract: A novel solid self-dispersing micelle (S-SDM) was developed to enhance the oral bioavailability of valsartan (VST) and to reduce the total mass of solidified supersaturable self-microemulsifying drug delivery system (S-SuSMEDDS), composed of Capmul MCM, ... ...

Abstract	A novel solid self-dispersing micelle (S-SDM) was developed to enhance the oral bioavailability of valsartan (VST) and to reduce the total mass of solidified supersaturable self-microemulsifying drug delivery system (S-SuSMEDDS), composed of Capmul MCM, Tween 80 (T80), Gelucire 44/14 (G44), Poloxamer 407, Florite PS-10 (FLO), and low-substituted hydroxypropyl cellulose B1 (HPC). Excluding oil component from S-SuSMEDDS, S-SDM was optimized using a Box-Behnken design with three independent variables: X
MeSH term(s)	Administration, Oral ; Animals ; Antihypertensive Agents/administration & dosage ; Antihypertensive Agents/blood ; Antihypertensive Agents/chemical synthesis ; Biological Availability ; Chemistry, Pharmaceutical/methods ; Drug Design ; Male ; Micelles ; Rats ; Rats, Sprague-Dawley ; Solubility ; Valsartan/administration & dosage ; Valsartan/blood ; Valsartan/chemical synthesis
Chemical Substances	Antihypertensive Agents ; Micelles ; Valsartan (80M03YXJ7I)
Language	English
Publishing date	2020-05-30
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2020.119483
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 1409: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾

Article: Enhanced Intracellular Delivery of BCG Cell Wall Skeleton into Bladder Cancer Cells Using Liposomes Functionalized with Folic Acid and Pep-1 Peptide.

Yoon, Ho Yub / Yang, Hee Mang / Kim, Chang Hyun / Goo, Yoon Tae / Hwang, Gwang Yong / Chang, In Ho / Whang, Young Mi / Choi, Young Wook

Pharmaceutics

2019 Volume 11, Issue 12

Abstract: Although bacillus Calmette-Guérin cell wall skeleton (BCG-CWS) might function as a potential substitute for live BCG, its use in the treatment of bladder cancer remains limited owing to issues such as insolubility and micrometer-size following exposure ... ...

Abstract	Although bacillus Calmette-Guérin cell wall skeleton (BCG-CWS) might function as a potential substitute for live BCG, its use in the treatment of bladder cancer remains limited owing to issues such as insolubility and micrometer-size following exposure to an aqueous environment. Thus, to develop a novel nanoparticulate system for efficient BCG-CWS delivery, liposomal encapsulation was carried out using a modified emulsification-solvent evaporation method (targets: Size, <200 nm; encapsulation efficiency, ~60%). Further, the liposomal surface was functionalized with specific ligands, folic acid (FA), and Pep-1 peptide (Pep1), as targeting and cell-penetrating moieties, respectively. Functionalized liposomes greatly increased the intracellular uptake of BCG-CWS in the bladder cancer cell lines, 5637 and MBT2. The immunoactivity was verified through elevated cytokine production and a THP-1 migration assay. In vivo antitumor efficacy revealed that the BCG-CWS-loaded liposomes effectively inhibited tumor growth in mice bearing MBT2 tumors. Dual ligand-functionalized liposome was also superior to single ligand-functionalized liposomes. Immunohistochemistry supported the enhanced antitumor effect of BCG-CWS, with IL-6 production and CD4 infiltration. Thus, we conclude that FA- and Pep1-modified liposomes encapsulating BCG-CWS might be a good candidate for bladder cancer treatment with high target selectivity.
Language	English
Publishing date	2019-12-04
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics11120652
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article: Surface-Modification of RIPL Peptide-Conjugated Liposomes to Achieve Steric Stabilization and pH Sensitivity.

Kwon, Yie Hyuk / Shin, Taek Hwan / Jang, Moon Ho / Yoon, Ho Yub / Kang, Min Hyung / Kang, Myung Joo / Choi, Young Wook

Journal of nanoscience and nanotechnology

2018 Volume 17, Issue 2, Page(s) 1008–1017

Abstract: We have previously demonstrated that RIPL peptide-conjugated liposomes (RIPL-L) exhibited high hepsin (HPN) selectivity and enhanced intracellular drug delivery. In this study, surface modification of RIPL-L was performed to reduce plasma protein ... ...

Abstract	We have previously demonstrated that RIPL peptide-conjugated liposomes (RIPL-L) exhibited high hepsin (HPN) selectivity and enhanced intracellular drug delivery. In this study, surface modification of RIPL-L was performed to reduce plasma protein adsorption and off-target effects. For steric stabilization, distearoyl phosphatidylethanolamine (DSPE)-polyethylene glycol (PEG)2000 was used (5% molar ratio to total lipid) to prepare PEG-RIPL-L. Further, pH-sensitive oligopeptides [(HD)4 or (HE)4] were coupled to shield the RIPL polyarginine moiety, yielding (HD)4/PEG-RIPL-L and (HE)4/PEG-RIPL-L. All liposomal vesicles had a narrow and homogenous size distribution of approximately 140–150 nm, with zeta potentials varying from −15 to 36 mV. Increased plasma stability was observed upon quantifying the protein adsorbed onto liposomes by using a micro bicinchoninic acid assay. The (HD)4- and (HE)4-coupling capacity of PEG-RIPL-L was investigated by measuring the amount of oligopeptide involved in transient ionic complexation (TIC-oligopep) and zeta potential changes. As the molar ratio of (HD)4 and (HE)4 increased, TIC-oligopep increased and zeta potential decreased. (HE)4/PEG-RIPL-L were pH-sensitive, producing 1.6-fold greater cellular uptake of FITC-dextran by LNCaP cells at pH 6.8 than at pH 7.4. This result suggested that (HE)4/PEG-RIPL-L might provide a sterically stabilized, pH-sensitive drug carrier for HPN-specific cancer targeting.
MeSH term(s)	Adsorption ; Cell Line, Tumor ; Drug Delivery Systems/methods ; Humans ; Hydrogen-Ion Concentration ; Liposomes/chemistry ; Peptides/chemistry ; Phosphatidylethanolamines/chemistry ; Polyethylene Glycols/chemistry ; Protein Stability ; Surface Properties
Chemical Substances	Liposomes ; Peptides ; Phosphatidylethanolamines ; polyethylene glycol-distearoylphosphatidylethanolamine ; Polyethylene Glycols (3WJQ0SDW1A)
Language	English
Publishing date	2018-04-19
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ISSN	1533-4880
ISSN	1533-4880
DOI	10.1166/jnn.2017.12670
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Inter-library loan at ZB MED

Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

Article ; Online: Tablet Formulation of a Polymeric Solid Dispersion Containing Amorphous Alkalinized Telmisartan.

Chae, Jun Soo / Chae, Bo Ram / Shin, Dong Jun / Goo, Yoon Tae / Lee, Eun Seok / Yoon, Ho Yub / Kim, Chang Hyun / Choi, Young Wook

AAPS PharmSciTech

2018 Volume 19, Issue 7, Page(s) 2990–2999

Abstract: To overcome the poor dissolution of telmisartan (TMS) at weak acidic pH, amorphous alkalinized TMS (AAT) was prepared by introducing sodium hydroxide as a selective alkalizer. AAT-containing polymeric solid dispersions were prepared by a solvent ... ...

Abstract	To overcome the poor dissolution of telmisartan (TMS) at weak acidic pH, amorphous alkalinized TMS (AAT) was prepared by introducing sodium hydroxide as a selective alkalizer. AAT-containing polymeric solid dispersions were prepared by a solvent evaporation method; these solid dispersions were AAT-PEG, AAT-PVP, AAT-POL, and AAT-SOL for the polymers of PEG 6000, PVP K30, Poloxamer 407, and Soluplus, respectively. The characteristics of the different formulations were observed by differential scanning calorimetry, powder X-ray diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy. To compare the supersaturation behavior, a dissolution test was performed at 37 ± 0.5 °C either in 900 ml (plain condition) or 500 ml (limited condition) of pH 6.8-simulated intestinal fluid used as a medium. AAT-SOL exhibited enhanced dissolution, indicating the probability of extended supersaturation in the limited condition. AAT-SOL was further formulated into a tablet by introducing other excipients, Vivapur 105 and Croscarmellose, as a binder and superdisintegrant, respectively, using a direct compression method. The selected AAT-SOL tablet was superior to Micardis (the reference product) in the aspect of supersaturation maintenance during dissolution in the limited condition, suggesting that it is a promising candidate for practical development that can replace the commercial product in the future.
MeSH term(s)	Antacids/chemistry ; Antacids/metabolism ; Antihypertensive Agents/chemistry ; Antihypertensive Agents/metabolism ; Calorimetry, Differential Scanning/methods ; Drug Compounding/methods ; Excipients/chemistry ; Excipients/metabolism ; Microscopy, Electron, Scanning/methods ; Polymers/chemistry ; Polymers/metabolism ; Solvents/chemistry ; Solvents/metabolism ; Spectroscopy, Fourier Transform Infrared/methods ; Tablets ; Telmisartan/chemistry ; Telmisartan/metabolism ; X-Ray Diffraction/methods
Chemical Substances	Antacids ; Antihypertensive Agents ; Excipients ; Polymers ; Solvents ; Tablets ; Telmisartan (U5SYW473RQ)
Language	English
Publishing date	2018-07-24
Publishing country	United States
Document type	Journal Article
ISSN	1530-9932
ISSN (online)	1530-9932
DOI	10.1208/s12249-018-1124-y
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

Order via subito

Inter-library loan at ZB MED

Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

Details ▾
- Full text online
- Order with fees

Article ; Online: Supersaturable self-microemulsifying drug delivery system enhances dissolution and bioavailability of telmisartan.

Park, Sun Young / Jin, Chang Hwa / Goo, Yoon Tae / Chae, Bo Ram / Yoon, Ho Yub / Kim, Chang Hyun / Song, Seh Hyon / Han, Sang Beom / Choi, Young Wook

Pharmaceutical development and technology

2020 Volume 26, Issue 1, Page(s) 60–68

Abstract: To enhance the dissolution and oral bioavailability of telmisartan (TMS), a poorly water-soluble anti-hypertensive drug, a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) was developed. Amorphous alkalinized TMS (AAT) was formulated ... ...

Abstract	To enhance the dissolution and oral bioavailability of telmisartan (TMS), a poorly water-soluble anti-hypertensive drug, a supersaturable self-microemulsifying drug delivery system (SuSMEDDS) was developed. Amorphous alkalinized TMS (AAT) was formulated into a SMEDDS, composed of Capmul® MCM (oil), Cremophor
MeSH term(s)	Administration, Oral ; Animals ; Antihypertensive Agents/administration & dosage ; Antihypertensive Agents/blood ; Antihypertensive Agents/chemical synthesis ; Biological Availability ; Drug Delivery Systems/methods ; Emulsifying Agents/administration & dosage ; Emulsifying Agents/blood ; Emulsifying Agents/chemical synthesis ; Male ; Rats ; Rats, Sprague-Dawley ; Solubility ; Telmisartan/administration & dosage ; Telmisartan/blood ; Telmisartan/chemical synthesis
Chemical Substances	Antihypertensive Agents ; Emulsifying Agents ; Telmisartan (U5SYW473RQ)
Language	English
Publishing date	2020-10-18
Publishing country	England
Document type	Journal Article
ZDB-ID	1331774-x
ISSN	1097-9867 ; 1083-7450
ISSN (online)	1097-9867
ISSN	1083-7450
DOI	10.1080/10837450.2020.1834580
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 5043: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Enhanced docetaxel delivery using sterically stabilized RIPL peptide-conjugated nanostructured lipid carriers: In vitro and in vivo antitumor efficacy against SKOV3 ovarian cancer cells.

Kim, Chang Hyun / Kang, Tae Hoon / Kim, Byoung Deok / Lee, Tae Hwa / Yoon, Ho Yub / Goo, Yoon Tae / Choi, Yong Seok / Kang, Myung Joo / Choi, Young Wook

International journal of pharmaceutics

2020 Volume 583, Page(s) 119393

Abstract: Docetaxel (DTX) has poor solubility, low specificity, and severe side effects. For efficient targeting of DTX to hepsin-overexpressing SKOV3 ovarian cancer cells, PEGylated and RIPL peptide (IPLVVPLRRRRRRRRC)-conjugated nanostructured lipid carriers (PEG- ...

Abstract	Docetaxel (DTX) has poor solubility, low specificity, and severe side effects. For efficient targeting of DTX to hepsin-overexpressing SKOV3 ovarian cancer cells, PEGylated and RIPL peptide (IPLVVPLRRRRRRRRC)-conjugated nanostructured lipid carriers (PEG-RIPL-NLCs) were examined for in vitro and in vivo antitumor efficacy. DTX-loaded plain NLCs (DTX-pNLCs), RIPL-NLCs (DTX-RIPL-NLCs), and PEG-RIPL-NLCs (DTX-PEG-RIPL-NLCs) were prepared using a solvent emulsification-evaporation technique. DTX was successfully loaded with high encapsulation efficiency (>93%), and all NLCs showed homogeneous dispersion with zeta potentials varying from -17 to 15 mV. Drug release was biphasic: initial rapid release, then gradual release. In vitro cytotoxicity was time- and dose-dependent: DTX-RIPL-NLCs and DTX-PEG-RIPL-NLCs exhibited greater cytotoxicity, enhanced cell apoptosis owing to the cell cycle arrest in the G2/M phase, and increased activation of the mitochondria-related intrinsic apoptosis pathway compared to DTX-pNLCs. Pharmacokinetic experiments in male Sprague-Dawley rats revealed that DTX-PEG-RIPL-NLCs increased the mean residence time of DTX but reduced total body clearance and volume of distribution. In a SKOV3-bearing xenograft Balb/c athymic mouse model, DTX-PEG-RIPL-NLCs suppressed tumors, evidenced by tumor volume change and histopathological examination. Thus, we conclude that PEG-RIPL-NLCs have an advantage of high payload of poorly water-soluble drugs and are a good candidate for drug targeting to SKOV3-derived ovarian cancer.
MeSH term(s)	Animals ; Antineoplastic Agents/administration & dosage ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacokinetics ; Apoptosis/drug effects ; Cell Line, Tumor ; Cell-Penetrating Peptides/chemistry ; Cell-Penetrating Peptides/metabolism ; Docetaxel/administration & dosage ; Docetaxel/chemistry ; Docetaxel/pharmacokinetics ; Drug Carriers ; Drug Compounding ; Drug Liberation ; Female ; G2 Phase Cell Cycle Checkpoints/drug effects ; Humans ; Injections, Intravenous ; Lipids/chemistry ; Male ; Mice, Inbred BALB C ; Mice, Nude ; Nanoparticles ; Ovarian Neoplasms/drug therapy ; Ovarian Neoplasms/metabolism ; Ovarian Neoplasms/pathology ; Rats, Sprague-Dawley ; Tumor Burden/drug effects ; Xenograft Model Antitumor Assays
Chemical Substances	Antineoplastic Agents ; Cell-Penetrating Peptides ; Drug Carriers ; Lipids ; RIPL peptide ; Docetaxel (15H5577CQD)
Language	English
Publishing date	2020-05-04
Publishing country	Netherlands
Document type	Comparative Study ; Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2020.119393
Database	MEDical Literature Analysis and Retrieval System OnLINE

Full text online

Accessible to users with ZB MED library card

In stock of ZB MED Cologne/Königswinter

Zs.A 1409: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (1.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾

Article: Improved Dissolution and Oral Bioavailability of Valsartan Using a Solidified Supersaturable Self-Microemulsifying Drug Delivery System Containing Gelucire

Shin, Dong Jun / Chae, Bo Ram / Goo, Yoon Tae / Yoon, Ho Yub / Kim, Chang Hyun / Sohn, Se Il / Oh, Dongho / Lee, Ahram / Song, Seh Hyon / Choi, Young Wook

Pharmaceutics

2019 Volume 11, Issue 2

Abstract: To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of ... ...

Abstract	To improve the dissolution and oral bioavailability of valsartan (VST), we previously formulated a supersaturable self-microemulsifying drug delivery system (SuSMED) composed of Capmul
Language	English
Publishing date	2019-01-31
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics11020058
Database	MEDical Literature Analysis and Retrieval System OnLINE

Order via subito

Article ; Online: Enhanced oral bioavailability of valsartan in rats using a supersaturable self-microemulsifying drug delivery system with P-glycoprotein inhibitors.

Goo, Yoon Tae / Song, Seh Hyon / Yeom, Dong Woo / Chae, Bo Ram / Yoon, Ho Yub / Kim, Chang Hyun / Park, Sun Young / Kang, Tae Hoon / Lee, Sangkil / Choi, Young Wook

Pharmaceutical development and technology

2019 Volume 25, Issue 2, Page(s) 178–186

Abstract: Valsartan (VST) is a poorly water-soluble drug and a P-glycoprotein (P-gp) substrate. To enhance the dissolution and oral absorption of VST, a novel supersaturable self-microemulsifying drug delivery system (Su-SMEDDS) was formulated. Based on the ... ...

Abstract	Valsartan (VST) is a poorly water-soluble drug and a P-glycoprotein (P-gp) substrate. To enhance the dissolution and oral absorption of VST, a novel supersaturable self-microemulsifying drug delivery system (Su-SMEDDS) was formulated. Based on the previously reported Su-SMEDDS composed of Capmul
MeSH term(s)	ATP Binding Cassette Transporter, Subfamily B, Member 1/antagonists & inhibitors ; Administration, Oral ; Animals ; Biological Availability ; Chemistry, Pharmaceutical/methods ; Drug Delivery Systems/methods ; Emulsions/chemistry ; Male ; Particle Size ; Rats ; Rats, Sprague-Dawley ; Solubility/drug effects ; Surface-Active Agents/chemistry ; Valsartan/chemistry ; Valsartan/pharmacology
Chemical Substances	ATP Binding Cassette Transporter, Subfamily B, Member 1 ; Emulsions ; Surface-Active Agents ; Valsartan (80M03YXJ7I)
Language	English
Publishing date	2019-11-18
Publishing country	England
Document type	Journal Article
ZDB-ID	1331774-x
ISSN	1097-9867 ; 1083-7450
ISSN (online)	1097-9867
ISSN	1083-7450
DOI	10.1080/10837450.2019.1683749
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 5043: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
Jg. 1995 - 2021: Lesesall (2.OG)
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

Article ; Online: Intravesical delivery of rapamycin via folate-modified liposomes dispersed in thermo-reversible hydrogel.

Yoon, Ho Yub / Chang, In Ho / Goo, Yoon Tae / Kim, Chang Hyun / Kang, Tae Hoon / Kim, Soo-Yeon / Lee, Sang Jin / Song, Seh Hyon / Whang, Young Mi / Choi, Young Wook

International journal of nanomedicine

2019 Volume 14, Page(s) 6249–6268

Abstract: Purpose: To develop an intravesical instillation system for the treatment of bladder cancer, rapamycin (Rap) was encapsulated into liposomes and then homogeneously dispersed throughout a poloxamer 407 (P407)-based hydrogel.: Methods: Rap-loaded ... ...

Abstract	Purpose: To develop an intravesical instillation system for the treatment of bladder cancer, rapamycin (Rap) was encapsulated into liposomes and then homogeneously dispersed throughout a poloxamer 407 (P407)-based hydrogel. Methods: Rap-loaded conventional liposomes (R-CL) and folate-modified liposomes (R-FL) were prepared using a film hydration method and pre-loading technique, and characterized by particle size, drug entrapment efficiency, and drug loading. The cellular uptake behavior in folate receptor-expressing bladder cancer cells was observed by flow cytometry and confocal laser scanning microscopy using a fluorescent probe. In vitro cytotoxic effects were evaluated using MTT assay, colony forming assay, and Western blot. For in vivo intravesical instillation, Rap-loaded liposomes were dispersed in P407-gel, generating R-CL/P407 and R-FL/P407. Gel-forming capacities and drug release were evaluated. Using the MBT2/Luc orthotopic bladder cancer mouse model, in vivo antitumor efficacy was evaluated according to regions of interest (ROI) measurement. Results: R-CL and R-FL were successfully prepared, at approximately <160 nm, 42% entrapment efficiency, and 57 μg/mg drug loading. FL cellular uptake was enhanced over 2-fold than that of CL; folate receptor-mediated endocytosis was confirmed using a competitive assay with folic acid pretreatment. In vitro cytotoxic effects increased dose-dependently. Rap-loaded liposomes inhibited mTOR signaling and induced autophagy in urothelial carcinoma cells. With gelation time of <30 seconds and gel duration of >12 hrs, both R-CL/P407 and R-FL/P407 preparations transformed into gel immediately after instillation into the mouse bladder. Drug release from the liposomal gel was erosion controlled. In orthotopic bladder cancer mouse model, statistically significant differences in ROI values were found between R-CL/P407 and R-FL/P407 groups at day 11 ( Conclusion: Intravesical instillation of R-FL/P407 might represent a good candidate for bladder cancer treatment, owing to its enhanced retention and FR-targeting.
MeSH term(s)	Administration, Intravesical ; Animals ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Autophagy/drug effects ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Colloids ; Disease Models, Animal ; Drug Liberation ; Female ; Folate Receptors, GPI-Anchored/metabolism ; Folic Acid/chemistry ; Humans ; Hydrogels/chemistry ; Liposomes ; Mice ; Particle Size ; Sirolimus/administration & dosage ; Sirolimus/pharmacology ; Sirolimus/therapeutic use ; TOR Serine-Threonine Kinases/metabolism ; Temperature ; Urinary Bladder Neoplasms/drug therapy
Chemical Substances	Antineoplastic Agents ; Colloids ; Folate Receptors, GPI-Anchored ; Hydrogels ; Liposomes ; Folic Acid (935E97BOY8) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; Sirolimus (W36ZG6FT64)
Language	English
Publishing date	2019-08-05
Publishing country	New Zealand
Document type	Journal Article
ZDB-ID	2364941-0
ISSN	1178-2013 ; 1176-9114
ISSN (online)	1178-2013
ISSN	1176-9114
DOI	10.2147/IJN.S216432
Database	MEDical Literature Analysis and Retrieval System OnLINE

In stock of ZB MED Cologne/Königswinter

Zs.A 6606: Show issues

Location:
Je nach Verfügbarkeit (siehe Angabe bei Bestand)
bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
ab Jg. 2022: Lesesaal (EG)

Order via subito

Details ▾
- See ZB MED holdings
- Order with fees

To top

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

Order via subito

Inter-library loan at ZB MED

Full text online

More links

Kategorien

Order via subito

Inter-library loan at ZB MED

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

Full text online

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito

More links

Kategorien

In stock of ZB MED Cologne/Königswinter

Order via subito