scholarly journals Improved drug loading and antibacterial activity of minocycline-loaded PLGA nanoparticles prepared by solid/oil/water ion pairing method

Author(s):  
Rassoul Dinarvand ◽  
TS Jafarzadeh Kashi ◽  
Eskandarion ◽  
Esfandyari-Manesh ◽  
Samadi ◽  
...  
2021 ◽  
Vol 17 (10) ◽  
pp. 1939-1950
Author(s):  
Beibei Lin ◽  
Xuegu Xu ◽  
Xiaobi Zhang ◽  
Yinfei Yu ◽  
Xiaoling Wang

We prepared poly(lactide-co-glycolide) (PLGA) encapsulated with chlorin e6 (Ce6) in an effort to increase the stability and efficiency of photosensitizers for photodynamic therapy (PDT). We determined that Ce6-loaded PLGA nanoparticles (PLGA-Ce6 NPs) had drug-loading efficiency of 5%. The efficiency of encapsulation was 82%, the zeta potential was- 25 mV, and the average diameter was 130 nm. The encapsulation of Ce6 in PLGA nanoparticles showed excellent stability. The nanoparticles exhibited sustained Ce6 release profiles with 50% released at the end of 3 days, whereas free Ce6 showed rapid release within 1 day. Ce6 release patterns were controlled by encapsulation into PLGA. The uptake of PLGA-Ce6 NPs was significantly enhanced by endocytosis in the first 8 hours in the HCT-116 cell line. An intracellular reactive oxygen species assay revealed the enhanced uptake of the nanoparticles. An in vitro anti-tumor activity assay showed that the PLGA-Ce6 NPs exhibited enhanced phototoxicity toward HCT-116 cells and a slightly lower IC50 value in HCT-116 cells than Ce6 solution alone. Exposure of HCT-116 cell spheroids to PLGA-Ce6 NPs penetrated more profoundly and had better phototoxicity than pure drugs. These findings suggest that PLGA-Ce6 NPs might serve as PDT for colorectal cancer.


2019 ◽  
Vol 14 (4) ◽  
pp. 1934578X1984270 ◽  
Author(s):  
Leniher Castan Chibas ◽  
Priscila Pavini Cintra ◽  
Monique Rodrigues Moreira ◽  
Mirian Oliveira Goulart ◽  
Sérgio Ricardo Ambrósio ◽  
...  

Polyalthic acid (PA) is a diterpene present in several trees of the Copaifera genus, with reported antitumor activity but poor water solubility. The aim of this work was the incorporation of PA in polymeric nanoparticles and the evaluation of the antiproliferative activity of this formulation in tumor (MCF-7) and normal (MCF-10A) breast cell lines. The nanoparticles were obtained by nanoprecipitation, using poly lactic-co-glycolic acid (PLGA) as the main material. Scanning electron microscopy showed nanoparticles with semispherical morphology, and dynamic light scattering measures revealed negative surface charge and average size of 98.64 ± 28 nm. The encapsulation efficiency was 98% and the drug loading was 15.6% ± 0.02%. Treatments with PA nanoparticles reduced cell proliferation more efficiently than free PA and the effect was selective on MCF-7 cells. Comet assay revealed a selective DNA damage induction by the nanoformulation on the tumor cells, which probably caused the antiproliferative effect. Our results show that PA incorporated in PLGA nanoparticles has potential as a selective cytostatic and genotoxic agent against MCF-7 cells.


2020 ◽  
Vol 10 (9) ◽  
pp. 1567-1572
Author(s):  
Yurong Liu ◽  
Xiaoyan Hou ◽  
Lianwei Lu ◽  
Ruixiang Wang

This study examined the effect of nanosized ferric oxide (Fe3O4) particles coated with different materials on the toxicity to HeLa cervical cancer cells. Magnetic Fe3O4 nanoparticles were prepared using a solventless thermal decomposition method and coated with either PLGA or CA-PLGA star copolymers. The uptake of nanoparticles by HeLa cells was observed by laser confocal microscopy. The toxicity to HeLa cells of Fe3O4 nanoparticles coated with these two materials was determined by the thiazole blue (MTT) method. The particle size of the single Fe3O4 nanoparticles was about 7 nm, and the PLGA and CA-PLGA nanoparticles loaded with Fe3O4 were spherical, with a particle size of about 200 mm and a theoretical drug loading of 10%. When the mass concentration of Fe3O4 nanoparticles is the same (25 pg/mL), the toxicity of Fe3O4-loaded CA-PLGA nanoparticles to HeLa cells is less than that of the corresponding PLGA nanoparticles. Thus, the CA-PLGA star copolymer can reduce the cytotoxicity of magnetic Fe3O4 nanoparticles and offers potential for broad application in vivo.


2021 ◽  
Vol 8 ◽  
Author(s):  
Qi Liu ◽  
Wen-Chong Ouyang ◽  
Xiu-Hong Zhou ◽  
Tao Jin ◽  
Zheng-Wei Wu

In this study, nanofibers with different ratios of poly(vinyl alcohol) and chitosan incorporated with moxifloxacin hydrochloride (MH/PVA/CS) were fabricated through the blending electrospinning, and the morphological features were tested using scanning electron microscopy (SEM). Further characterization of the new nanofiber was accomplished by Thermogravimetric analysis (TG), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FTIR). Antibacterial activity of the MH-loaded nanofibers at different drug loading were tested and compared with the blank group. Experimental results show that the MH/PVA/CS nanofibers exhibited the good antibacterial properties against Staphylococcus aureus and Pseudomonas aeruginosa due to the MH incorporation. Compared with blank nanofibers, MH/PVA/CS nanofibers have significantly better antibacterial properties, and different proportions of PVA and CS have a certain effect on the antibacterial activity of nanofibers. The conclusions in this paper show that MH/PVA/CS composite nanofibers may have great potential in antibacterial materials.


2020 ◽  
Vol 10 (3) ◽  
pp. 280-289
Author(s):  
Kanchan Kashyap ◽  
Mayank Handa ◽  
Rahul Shukla

Background: Glioblastoma multiforme (GBM) is a belligerent brain tumor constituting about 67% of primary brain tumours. The current therapy for glioblastoma multiforme is surgery, radiations and chemotherapy though the success rate is quite limited. Azacitidine is a hydrophilic anti-cancer agent which acts by demethylation and is used in the treatment of both acute and chronic myelomonocytic leukaemia along with GBM. Objective: Formulation of stable Azacitidine loaded poly-lactide-co-glycolide (PLGA) nanoparticles (NPs) with tailor-made release profiles. Methods: Preparation of Azacitidine loaded PLGA nanoparticles was done by double emulsion (w/o/w) solvent evaporation technique. PLGA was used in the formulation, as it is biocompatible and biodegradable. Polyvinyl alcohol worked as an emulsifier while Span 80 decreased the interfacial tension among two immiscible phases (aqueous and organic), resulting in increased stability of the formulation. Results: Polymer concentration was directly proportional to the entrapment and drug loading and inversely proportional to particle size. Azacitidine loaded PLGA NPs showed a biphasic release model. At the first stage, burst release was observed, followed by sustained release. About 43.93 ± 0.69% drug was released in 1 hour and the remaining drug was released in 48 hours. Conclusion: Dual release behavior first delivered an ample amount of dose which provided cytotoxic dose, followed by the maintenance dose for sustaining the cytotoxic drug levels. Future prospective requires In-vitro cell viability evaluation of tailor-made polymeric nanoparticles along with In-vivo evaluation for therapeutic intervention in a glioblastoma tumor model.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 67-71
Author(s):  
R. K Panik ◽  
◽  
M. R Singh ◽  
D. Singh

Aim of the study was to develop PLGA nanoparticles (PLGA-NP) of mupirocin (MP) and to study the effect of independent variables in order to optimize the formulation for effective delivery. Drug loaded PLGA-NPs were successfully prepared by nanoprecipitation method and characterized by mean particle size, zeta potential, entrapment efficiency, drug loading, drug release, TEM, and DSC study. Independent variables like drug-polymer ratio, surfactant concentration, and stirring speed showed significant effect on the dependent variables like particle size, entrapment efficiency and drug loading. The ANOVA results showed that selected independent variables had a significant effect on the preparation of mupirocin loaded PLGA-NP.


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