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Externally Triggered Novel Rapid-Release Sonosensitive Folate-Modified Liposomes for Gemcitabine: Development and Characteristics.
- Source :
-
International journal of nanomedicine [Int J Nanomedicine] 2021 Jan 28; Vol. 16, pp. 683-700. Date of Electronic Publication: 2021 Jan 28 (Print Publication: 2021). - Publication Year :
- 2021
-
Abstract
- Purpose: To develop an externally triggered rapid-release targeted system for treating ovarian cancer, gemcitabine (GMC) was entrapped into sonosensitive (SoS) folate (Fo)-modified liposomes (LPs).<br />Methods: GMC-loaded LPs (GMC LPs), GMC-loaded Fo-targeted LPs (GMC-Fo LPs), and GMC-loaded Fo-targeted SoS LPs (GMC-SoS Fo LPs) were prepared utilizing a film-hydration technique and evaluated based on particle size, ζ-potential, and percentage entrapped drug. Cellular uptake of the fluorescent delivery systems in Fo-expressing ovarian cancer cells was quantified using flow cytometry. Finally, tumor-targeting ability, in vivo evaluation, and pharmacokinetic studies were performed.<br />Results: GMC LPs, GMC-Fo LPs, and GMC-SoS Fo LPs were successfully prepared, with sizes of <120.3±2.4 nm, 39.7 mV ζ-potential, and 86.3%±1.84% entrapped drug. Cellular uptake of GMC-SoS Fo LPs improved 6.51-fold over GMC LPs (under ultrasonic irradiation - p <0.05). However, cellular uptake of GMC-Fo LPs improved just 1.24-fold over GMC LPs ( p >0.05). Biodistribution study showed that of GMC concentration in tumors treated with GMC-SoS-Fo LPs (with ultrasound) improved 2.89-fold that of free GMC ( p <0.05). In vivo, GMC-SoS Fo LPs showed the highest antiproliferative and antitumor action on ovarian cancer.<br />Conclusion: These findings showed that externally triggered rapid-release SoS Fo-modified LPs are a promising system for delivering rapid-release drugs into tumors.<br />Competing Interests: The authors report no conflicts of interest in this work.<br /> (© 2021 Omar et al.)
- Subjects :
- Animals
Antineoplastic Agents administration & dosage
Antineoplastic Agents blood
Antineoplastic Agents pharmacokinetics
Antineoplastic Agents therapeutic use
Cell Death drug effects
Cell Line, Tumor
Deoxycytidine administration & dosage
Deoxycytidine blood
Deoxycytidine pharmacokinetics
Deoxycytidine pharmacology
Drug Delivery Systems
Drug Liberation
Endocytosis drug effects
Female
Humans
Liposomes
Ovarian Neoplasms blood
Ovarian Neoplasms drug therapy
Ovarian Neoplasms pathology
Particle Size
Rats, Sprague-Dawley
Tissue Distribution drug effects
Gemcitabine
Rats
Deoxycytidine analogs & derivatives
Folic Acid chemistry
Ultrasonics
Subjects
Details
- Language :
- English
- ISSN :
- 1178-2013
- Volume :
- 16
- Database :
- MEDLINE
- Journal :
- International journal of nanomedicine
- Publication Type :
- Academic Journal
- Accession number :
- 33536754
- Full Text :
- https://doi.org/10.2147/IJN.S266676