Effect of Polymer Blending on the Release of Ganciclovir from PLGA Microspheres

Duvvuri, Sridhar; Janoria, Kumar G.; Mitra, Ashim K.

doi:10.1007/s11095-005-9042-6

Cited by 62 publications

(51 citation statements)

References 24 publications

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“…To analyze the dependence of PLGA combination on drug release, in vitro release studies were conducted. In agreement with previous reports, 18,37 PLGA 50-50 nanoparticles showed faster in vitro release of 5-FU compared with PLGA 90-10 ( Figure 5), which might be due to the presence of higher glycolide content in the 50-50 combination that accounts for its faster degradability.…”

supporting

confidence: 92%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

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Nanoscaled devices have great potential for drug delivery applications due to their small size. In the present study, we report for the first time the preparation and evaluation of antitumor efficacy of 5-fluorouracil (5-FU)-entrapped poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles with dependence on the lactide/glycolide combination of PLGA. 5-FU-loaded PLGA nanoparticles with two different monomer combinations, 50-50 and 90-10 were synthesized using a modified double emulsion method, and their biological evaluation was done in glioma (U87MG) and breast adenocarcinoma (MCF7) cell lines. 5-FU-entrapped PLGA 50-50 nanoparticles showed smaller size with a high encapsulation efficiency of 66%, which was equivalent to that of PLGA 90-10 nanoparticles. Physicochemical characterization of nanoparticles using differential scanning calorimetry and X-ray diffraction suggested the presence of 5-FU in molecular dispersion form. In vitro release studies showed the prolonged and sustained release of 5-FU from nanoparticles with both the PLGA combinations, where PLGA 50-50 nanoparticles showed faster release. Nanoparticles with PLGA 50-50 combination exhibited better cytotoxicity than free drug in a dose- and time-dependent manner against both the tumor cell lines. The enhanced efficiency of PLGA 50-50 nanoparticles to induce apoptosis was indicated by acridine orange/ethidium bromide staining. Cell cycle perturbations studied using flow cytometer showed better S-phase arrest by nanoparticles in comparison with free 5-FU. All the results indicate that PLGA 50-50 nanoparticles possess better antitumor efficacy than PLGA 90-10 nanoparticles and free 5-FU. Since, studies have shown that long-term exposure of ailing tissues to moderate drug concentrations is more favorable than regular administration of higher concentration of the drug; our results clearly indicate the potential of 5-FU-loaded PLGA nanoparticles with dependence on carrier combination as controlled release formulation to multiplex the therapeutic effect of cancer chemotherapy.

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supporting

confidence: 92%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

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“…The resulting nanosuspension was subjected to 3 cycles of homogenization at a pressure of 10,000 bar (EmulsiFlex-C5, Avestin, Inc., Canada). GCV-NPs were collected by centrifugation at 15,000 rpm for 10 min at 4°C, washed three times with distilled water, and Lyophilization was carried out in a freezedrier (Heto DRYWINNER, Germany) at 0.05 mBar for 24 h. The entrapment efficiency for the GCV in prepared formulation was then determined using the method reported by Duvvuri et al (13) by UPLC quantification technique.…”

Section: Preparation Of Gcv Nanocarriers Preparation Of Plga Nanopartmentioning

confidence: 99%

Ocular pharmacoscintigraphic and aqueous humoral drug availability of ganciclovir-loaded mucoadhesive nanoparticles in rabbits

Akhter¹,

Ramazani²,

Ahmad³

et al. 2016

Nano Online

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Abstract:The present report describes the improved ocular retention and aqueous humoral drug availability of ganciclovir (GCV) when administered via topical instillation of different kind of nanoparticles onto the rabbit eye. GCV was loaded into PLGA nanoparticles, chitosancoated nanoparticles and chitosan-coated niosomal nanoparticles. All three formulations contained nanoparticles equally round in shape with a mean particle size in the range of 180-200 nm. The ocular corneal retention property was evaluated by gamma scintigraphy, revealing that the clearance was slowest in the case of the chitosancontaining formulations. GCV in chitosan-coated PLGA nanoparticles and chitosan-coated niosomal nanoparticles showed approx. 6-fold higher aqueous humor drug availability as compared to a GCV solution and nearly 2.5-fold higher as compared to the chitosan-lacking GCV-PLGA nanoparticles. The results indicate that the use of a mucoadhesive chitosan coating can improve the ocular residence time and aqueous humoral availability of GCV when administered topically in nanoparticles.

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“…HCE or SV40 cells were seeded in 96-well plate at a density of 10 4 cells per well and incubated at 37°C, 5% CO 2 , and 98% humidity for 24 h. Polymer solutions were prepared in culture medium and sterilized by filtration with 0.2-μm syringe filters. Following incubation period, cells were exposed to various concentrations of polymer (25,50, and 100 mg/mL, n= 6) and incubated for 48 h. Cells without treatment were selected as negative control whereas cells treated with Triton-X 100 (0.1% v/v) as positive control. According to the protocol provided by the manufacturer, LDH release in cell supernatant was quantified by LDH assay kit (Takara Bio Inc., Japan).…”

Section: In Vitro Cytotoxicitymentioning

confidence: 99%

“…The release mechanism for DEX from nanomicelles was determined by in vitro release study in simulated tear fluid (STF compositions: 2 g NaHCO 3 , 6.7 g NaCl, 0.08 g CaCl 2 ·2H 2 O, and deionized water was added up to 1 L, Tween-80 (0.5% w/w)) (22) with a dialysis method (23)(24)(25). The optimal formulation obtained from the ED 2 was prepared and characterized for initial drug content.…”

Section: In Vitro Release Of Dexmentioning

confidence: 99%

Novel Dexamethasone-Loaded Nanomicelles for the Intermediate and Posterior Segment Uveitis

et al. 2014

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Abstract. Development and characterization of dexamethasone (DEX)-encapsulated polymeric nanomicelles have been reported. A low molecular weight di-block copolymer was synthesized and characterized for its structure, molecular weights, critical micelle concentration (CMC), and cytotoxicity in ocular cells. In order to delineate the effects of drug-polymer interactions on drug solubilization in micelle core, a response surface methodology was generated with the help of SAS 9.02 (exploratory model). The method for preparing micelle was modified based on the results obtained from exploratory model. The formulation was optimized by response surface methodology (optimization model) to achieve DEX solubility of above 1 mg/mL. The optimized formulation was characterized for DEX solubility, nanomicelle size, polydispersity index, surface morphology, in vitro transport across conjunctival cell line, and ex vivo transport across excised rabbit sclera. Nanomicelles exhibited average sizes in range of 25-30 nm with unimodel size distribution and low polydispersity of 0.125. Nanomicelles increased DEX permeability by 2 times across conjunctival cell line and by 2.5 times across the excised rabbit sclera as compared to DEX suspension. A design of experiment (DOE) strategy was successfully applied to understand the effects of drug-polymer interaction on drug solubility. DOE was also employed to achieve optimal formulation with high DEX solubility. Nanomicellar formulation significantly enhanced DEX permeability across the excised rabbit sclera. Therefore, nanomicellar formulation may provide therapeutic levels in the back of the eye following topical administration.

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Effect of Polymer Blending on the Release of Ganciclovir from PLGA Microspheres

Cited by 62 publications

References 24 publications

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Ocular pharmacoscintigraphic and aqueous humoral drug availability of ganciclovir-loaded mucoadhesive nanoparticles in rabbits

Novel Dexamethasone-Loaded Nanomicelles for the Intermediate and Posterior Segment Uveitis

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