Paclitaxel-loaded PLGA nanoparticles surface modified with transferrin and Pluronic®P85, anin vitrocell line andin vivobiodistribution studies on rat model

Shah, Neha; Chaudhari, Kiran; Dantuluri, Prudhviraju; Murthy, R. S. R.; Das, Susobhan

doi:10.1080/10611860903046628

Cited by 106 publications

(64 citation statements)

References 22 publications

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“…With the increased ratio from 1:10 to 3:10, however, the drug entrapment of M-C-PLA-NP was decreased and the particle size got bigger, which was consistent with previous reports (Budhian et al, 2007;Shah et al, 2009). An increase in the polymer concentration led to an increase in the viscosity of the organic phase, which resulted in rapid diffusion of the organic phase into the aqueous phase.…”

Section: Physicochemical Characterization and Effect Of Formulation Vsupporting

confidence: 82%

Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency

et al. 2014

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Purpose: To prepare a mixture of multiple-coated aniracetam nasal polylactic-acid nanoparticles (M-C-PLA-NP) and evaluate its stability preliminarily in vitro and its brain-targeting efficiency in vivo. Methods: The solvent diffusion-evaporation combined with magnetic stirring method has been chosen for the entrapment of aniracetam. The M-C-PLA-NP was characterized with respect to its morphology, particle size, size distribution and aniracetam entrapment efficiency. The in vivo distribution was studied in male SD rats after an intranasal administration.Results: In vitro release of M-C-PLA-NP showed two components with an initial rapid release due to the surface-associated drug and followed by a slower exponential release of aniracetam, which was dissolved in the core. The AUC 0!30 min of M-C-PLA-NP in brain tissues resulted in a 5.19-fold increase compared with aniracetam solution. The ratios of AUC in brain to that in other tissues obtained after nasal application of M-C-PLA-NP were significantly higher than those of aniracetam solution. Conclusion: Therefore, it can be concluded that M-C-PLA-NP demonstrated its potential on increasing the brain-targeting efficiency of drugs and will be used as novel brain-targeting agent for nasal drug delivery.

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Section: Physicochemical Characterization and Effect Of Formulation Vsupporting

confidence: 82%

Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency

et al. 2014

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“…An increase in drug:polymer ratio from 1:1 to 1:15 caused an increase in entrapment efficiency and decrease in particle size. Nevertheless, further increase in the drug:polymer ratio increased the particle size (Budhian et al, 2007;Shah et al, 2009). This may be due to the fact that an increase in the polymer concentration increased the viscosity of the organic phase leading to rapid diffusion of the organic phase into the aqueous phase.…”

Section: Formulation Development and Optimizationmentioning

confidence: 99%

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Alex

Joseph

Shavi³

et al. 2014

Drug Delivery

108

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Context: The study was aimed to develop a polymeric nanoparticle formulation of anticancer drug carboplatin using biodegradable polymer polycaprolactone (PCL). The formulation is intended for intranasal administration to treat glioma anticipating improved brain delivery as nasal route possess direct access to brain and nanoparticles have small size to overcome the mucosal and blood-brain barrier. Objective: Development and evaluation of carboplatin-PCL nanoparticles for brain delivery by nasal route. Methodology: Carboplatin-loaded PCL nanoparticles (CPCs) were prepared by double emulsionsolvent evaporation technique and characterized by particle size, zeta potential, entrapment efficiency, scanning electron microscopy and differential scanning calorimetry. The CPCs were assessed for in vitro release kinetics, ex vivo permeation and in situ nasal perfusion. Cytotoxic potential of CPCs in vitro was evaluated on LN229 human glioblastoma cells. Results and discussion: The optimized formulation of carboplatin-PCL nanoparticle CPC-08 with particle size of 311.6 ± 4.7 nm and zeta potential À16.3 ± 3.7 mV exhibited percentage entrapment efficiency of 27.95 ± 4.21. In vitro drug release showed initial burst release followed by slow and continues release indicating biphasic pattern. The ex vivo permeation pattern through sheep nasal mucosa also exhibited a similar release pattern as for in vitro release studies. In situ nasal perfusion studies in Wistar rats demonstrate that CPCs show better nasal absorption than carboplatin solution. In vitro cytotoxicity studies on LN229 cells showed an enhancement in cytotoxicity by CPCs compared to carboplatin alone. Conclusion: CPC-08 effectively improves nasal absorption of carboplatin and can be used for intranasal administration of carboplatin for improved brain delivery.

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“…Only the drug presenting in the cell membrane can be effluxed out of the cancer cell. The drug delivered by nanoparticles is internalized in the cytoplasm or the lysosome and not pumped out by P-gp (1). Dox-loaded liposomes are able to overcome MDR by increasing Dox uptake in the nuclei and extending retention in the nuclei of the MDR cells (2,3).…”

mentioning

confidence: 99%

Multifunctional Nanoparticles Delivering Small Interfering RNA and Doxorubicin Overcome Drug Resistance in Cancer

Chen

Bathula

et al. 2010

Journal of Biological Chemistry

198

131

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Drug resistance is a major challenge to the effective treatment of cancer. We have developed two nanoparticle formulations, cationic liposome-polycation-DNA (LPD) and anionic liposome-polycation-DNA (LPD-II), for systemic co-delivery of doxorubicin (Dox) and a therapeutic small interfering RNA (siRNA) to multiple drug resistance (MDR) tumors. In this study, we have provided four strategies to overcome drug resistance. First, we formed the LPD nanoparticles with a guanidinium-containing cationic lipid, i.e. N,N-distearyl-N-methyl-N-2-(N-arginyl) aminoethyl ammonium chloride, which can induce reactive oxygen species, down-regulate MDR transporter expression, and increase Dox uptake. Second, to block angiogenesis and increase drug penetration, we have further formulated LPD nanoparticles to co-deliver vascular endothelial growth factor siRNA and Dox. An enhanced Dox uptake and a therapeutic effect were observed when combined with vascular endothelial growth factor siRNA in the nanoparticles. Third, to avoid P-glycoprotein-mediated drug efflux, we further designed another delivery vehicle, LPD-II, which showed much higher entrapment efficiency of Dox than LPD. Finally, we delivered a therapeutic siRNA to inhibit MDR transporter. We demonstrated the first evidence of c-Myc siRNA delivered by the LPD-II nanoparticles down-regulating MDR expression and increasing Dox uptake in vivo. Three daily intravenous injections of therapeutic siRNA and Dox (1.2 mg/kg) co-formulated in either LPD or LPD-II nanoparticles showed a significant improvement in tumor growth inhibition. This study highlights a potential clinical use for the multifunctional nanoparticles with an effective delivery property and a function to overcome drug resistance in cancer. The activity and the toxicity of LPDand LPD-II-mediated therapy are compared.The occurrence of drug resistance is a main impediment to the success of cancer chemotherapy. Cancer cells develop different ways to be resistant to chemotherapy drugs. Overexpression of drug transporter proteins, such as P-glycoprotein (P-gp) 2 plays a key role in regulating drug resistance. Development of strategies to down-regulate the expression of P-gp or inhibit P-gp function has been the major subject of cancer research. For example, one of the strategies to overcome MDR is to use carriers like nanoparticles to avoid P-gp-mediated drug efflux. Only the drug presenting in the cell membrane can be effluxed out of the cancer cell. The drug delivered by nanoparticles is internalized in the cytoplasm or the lysosome and not pumped out by P-gp (1). Dox-loaded liposomes are able to overcome MDR by increasing Dox uptake in the nuclei and extending retention in the nuclei of the MDR cells (2, 3). Small interfering RNA (siRNA) is a promising novel approach of cancer therapy. It offers a new strategy to downregulate the targeted oncogene for therapeutic intervention. Systemically delivering siRNA to tumors remains a major hurdle in cancer gene therapy (4, 5). Major problems of siRNA delivery include poor cellula...

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Paclitaxel-loaded PLGA nanoparticles surface modified with transferrin and Pluronic^®P85, anin vitrocell line andin vivobiodistribution studies on rat model

Cited by 106 publications

References 22 publications

Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency

Preparation of surface multiple-coated polylactide acid drug-loaded nanoparticles for intranasal delivery and evaluation on its brain-targeting efficiency

Development and evaluation of carboplatin-loaded PCL nanoparticles for intranasal delivery

Multifunctional Nanoparticles Delivering Small Interfering RNA and Doxorubicin Overcome Drug Resistance in Cancer

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