Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA–mPEG nanoparticles

Avgoustakis, Konstantinos; Beletsi, A.; Panagi, Z.; Klepetsanis, Pavlos; Livaniou, Evangelia; Evangelatos, Gregory P.; Ithakissios, Dionyssis S.

doi:10.1016/s0378-5173(03)00224-2

Cited by 195 publications

(124 citation statements)

References 27 publications

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“…However, in present study, contrary results were observed and spleen showed lower uptake compared to liver. These could be due to smaller size of micelles, below 100 nm, which can penetrate more in liver compared to particle size of nanocarrier above 100 nm (Avgoustakis et al, 2003). A higher tumoral uptake of micellar formulations due to the EPR effect was observed due to presence of PEG chains on the surface of micelles, which made the micelles to remain in circulation for longer duration for passive targeting (Yadav et al, 2008).…”

Section: Discussionmentioning

confidence: 99%

Investigation on design of stable etoposide-loaded PEG-PCL micelles: effect of molecular weight of PEG-PCL diblock copolymer on thein vitroandin vivoperformance of micelles

et al. 2012

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Section: Discussionmentioning

confidence: 99%

Investigation on design of stable etoposide-loaded PEG-PCL micelles: effect of molecular weight of PEG-PCL diblock copolymer on thein vitroandin vivoperformance of micelles

et al. 2012

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“…2A). Previous work on PLGA-PEG DCP showed that NP size depended on size of the PEG polymer (23,24). We sought to determine whether varying the length of the PEG segment in the TCP could control the NP-Apt bioconjugate size.…”

Section: Effects Of Copolymer Composition On Np Biophysicochemical Prmentioning

confidence: 99%

“…We believed that by avoiding the unnecessary masking of PEG on NP surface by excess Apt that did not confer additional targeting benefit, we could maximize the exposure of PEG to retain its antibiofouling properties, resulting in maximally stealth and maximally targeted NPs. Our group and others had shown that PEG can increase the antibiofouling properties of NPs in vivo resulting in long circulating NPs for systemic delivery (24,26,27). NPs containing different Apt ligand densities were synthesized by controlling the mixing ratios of PLGA 0.67 -b-PEG 3400 -b-Apt to PLGA 0.67 -PEG 3400 .…”

Section: Determination Of Optimal Apt Density On Np Surface In Vitro mentioning

confidence: 99%

Precise engineering of targeted nanoparticles by using self-assembled biointegrated block copolymers

Zhang²,

Teply

et al. 2008

Proc. Natl. Acad. Sci. U.S.A.

638

566

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There has been progressively heightened interest in the development of targeted nanoparticles (NPs) for differential delivery and controlled release of drugs. Despite nearly three decades of research, approaches to reproducibly formulate targeted NPs with the optimal biophysicochemical properties have remained elusive. A central challenge has been defining the optimal interplay of parameters that confer molecular targeting, immune evasion, and drug release to overcome the physiological barriers in vivo. Here, we report a strategy for narrowly changing the biophysicochemical properties of NPs in a reproducible manner, thereby enabling systematic screening of optimally formulated drug-encapsulated targeted NPs. NPs were formulated by the self-assembly of an amphiphilic triblock copolymer composed of end-to-end linkage of poly(lactic-co-glycolic-acid) (PLGA), polyethyleneglycol (PEG), and the A10 aptamer (Apt), which binds to the prostate-specific membrane antigen (PSMA) on the surface of prostate cancer (PCa) cells, enabling, respectively, controlled drug release, ''stealth'' properties for immune evasion, and cell-specific targeting. Fine-tuning of NP size and drug release kinetics was further accomplished by controlling the copolymer composition. By using distinct ratios of PLGA-b-PEG-b-Apt triblock copolymer with PLGA-b-PEG diblock copolymer lacking the A10 Apt, we developed a series of targeted NPs with increasing Apt densities that inversely affected the amount of PEG exposure on NP surface and identified the narrow range of Apt density when the NPs were maximally targeted and maximally stealth, resulting in most efficient PCa cell uptake in vitro and in vivo. This approach may contribute to further development of targeted NPs as highly selective and effective therapeutic modalities.aptamer ͉ controlled release ͉ chemotherapy ͉ combinatorial screening

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“…To achieve controlled drug release, biodegradable polymeric nanoparticles are often used in advanced anticancer drug delivery systems (13)(14)(15). Some drug delivery systems that employ a biodegradable polymer, such as nanoparticles delivering anticancer agents, are commercially available.…”

Section: Introductionmentioning

confidence: 99%

Study of the Composition of Polycaprolactone/Poly (Ethylene Glycol)/Polycaprolactone Copolymer and Drug-to-Polymer Ratio on Drug Loading Efficiency of Curcumin to Nanoparticles

HosseinDanafar

2016

Jundishapur J Nat Pharm Prod

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Background: Natural products derived from plants play a significant function in healthcare in many cultures, both ancient and modern. curcumin (CUR) is a chemical constituent of turmeric with anticancer activity, but its poor water solubility limits its use clinically. Methods: To improve the bioavailability and water solubility of curcumin, we synthesized five series of poly (caprolactone)-poly (ethylene glycol)-poly (caprolactone) (PCL-PEG-PCL) triblock copolymers. The structure of the copolymers was characterized by HNMR, FT-IR, DSC, and GPC techniques. The nanoparticles (NPs) were prepared using a solvent evaporation method. To achieve the best delivery system, we assigned the effect of the length of the copolymers' hydrophilic and hydrophobic chains on the encapsulation of hydrophobic CUR, performed entrapment efficiency and drug loading assignments, as well as evaluated the particle distribution and in vitro release using the direct dispersion method. Results: CUR was encapsulated with 71% and 83% efficiency in biodegradable nanoparticulate formulations, based on NP4 and NP5. Dynamic laser light scattering (DLS) indicated a particle diameter of 112 nm and 110 nm for NP4 and NP5, respectively. FT-IR and DSC analysis of the NPs showed that CUR was encapsulated into the NPs. The in vitro release experiments showed that NP5 controlled the release of CUR more effectively, with only 51% of CUR released after 120 hours. Conclusions:The results indicate the successful formulation of curcumin-loaded PCL-PEG-PCL nanoparticles and improved water solubility of curcumin, which may have potential application in cancer treatment.

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Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA–mPEG nanoparticles

Cited by 195 publications

References 27 publications

Investigation on design of stable etoposide-loaded PEG-PCL micelles: effect of molecular weight of PEG-PCL diblock copolymer on thein vitroandin vivoperformance of micelles

Investigation on design of stable etoposide-loaded PEG-PCL micelles: effect of molecular weight of PEG-PCL diblock copolymer on thein vitroandin vivoperformance of micelles

Precise engineering of targeted nanoparticles by using self-assembled biointegrated block copolymers

Study of the Composition of Polycaprolactone/Poly (Ethylene Glycol)/Polycaprolactone Copolymer and Drug-to-Polymer Ratio on Drug Loading Efficiency of Curcumin to Nanoparticles

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