Folate receptor targeted biodegradable polymeric doxorubicin micelles

Yoo, Hyuk Sang; Park, Tae Gwan

doi:10.1016/j.jconrel.2004.02.003

Cited by 568 publications

(426 citation statements)

References 23 publications

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“…64,140 -142 Polymer block conjugation is an alternative method. 144 Biotinylated PEG-PLA nanoparticles may link biotinylated antibodies through an avidin spacer 145 (FIG. 3, panel 1a), or avidinantibody conjugates 146 (FIG.…”

Section: Drug Loadingmentioning

confidence: 99%

Drug transport to brain with targeted nanoparticles

2005

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Summary: Nanoparticle drug carriers consist of solid biodegradable particles in size ranging from 10 to 1000 nm (50 -300 nm generally). They cannot freely diffuse through the bloodbrain barrier (BBB) and require receptor-mediated transport through brain capillary endothelium to deliver their content into the brain parenchyma. Polysorbate 80-coated polybutylcyanoacrylate nanoparticles can deliver drugs to the brain by a still debated mechanism. Despite interesting results these nanoparticles have limitations, discussed in this review, that may preclude, or at least limit, their potential clinical applications. Long-circulating nanoparticles made of methoxypoly(ethylene glycol)-polylactide or poly(lactide-co-glycolide) (mPEG-PLA/ PLGA) have a good safety profiles and provide drug-sustained release. The availability of functionalized PEG-PLA permits to prepare target-specific nanoparticles by conjugation of cell surface ligand. Using peptidomimetic antibodies to BBB transcytosis receptor, brain-targeted pegylated immunonanoparticles can now be synthesized that should make possible the delivery of entrapped actives into the brain parenchyma without inducing BBB permeability alteration. This review presents their general properties (structure, loading capacity, pharmacokinetics) and currently available methods for immunonanoparticle preparation.

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Section: Drug Loadingmentioning

confidence: 99%

Drug transport to brain with targeted nanoparticles

2005

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“…Both adults and children need folic acid to make normal red blood cells and prevent anemia. Children and adults both require folic acid to produce healthy red blood cells and prevent anemia [3,4]. Thus folic acid deficiency hinders DNA synthesis and cell division.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of Surfactants-Assisted Folic Acid-Loaded Pectin Submicrospheres: Characterization and Hemocompatibility Assay

2016

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Folic acid is used for preventing and treating multiple diseases and disorders, administered in the form of oral supplements. The present research work was aimed to study the influence of two non-ionic surfactants Poloxamer and Tween 80 (Polysorbate 80) on pectin submicrospheres formulations. Typical natural polymer pectin was used to encapsulate folic acid by cross linking method. The resultant submicrospheres contributed to improve the aqueous solubility to enhance the bioavailability of folic acid. During investigation, it was observed that pectin polymers influenced kinetics of the rate of reaction more intensively than the surfactants. The physical phenomenon caused the change in their size, shape and chemistry of pectin polymers transforming into submicrospheres in aqueous condition. The characteristic differences of submicrospheres were assessed by scanning electron microscopy, differential scanning calorimetry and Fouriertransform infrared spectroscopy. The average diameters of the submicrospheres ranged between 250 and 500 nm. The encapsulation efficiency of submicrospheres ranged between 80 and 96 %. The characteristic swelling behavior of lyophilized submicrospheres was influenced by the ratio of pectin polymers and folic acid used in the formulations. The submicrospheres systems exhibited controlled release of folic acid due to the pH-dependent solubility of pectin polymers in aqueous medium. The submicrospheres showed good haemocompatibility suggesting them to be promising candidates for oral delivery.

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“…The above micelles showed higher cell toxicity than folate-unconjugated micelles (Yoo and Park, 2004;Han et al, 2009;Liu et al, 2014). In this study, the α-and γ-Fol-PEG-DSPE-DOX micelles were found to promote a greater cellular uptake of DOX as compared to the MPEG-DSPE-DOX micelles.…”

Section: Discussionmentioning

confidence: 60%

Isomeric Folate-Conjugated Polymeric Micelles Bind to Folate Receptors and Display Anticancer Effects

Dong¹,

Xie²,

Xie³

et al. 2014

Asian Pacific Journal of Cancer Prevention

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The present study aimed to prepare and evaluate polymeric micelles conjugated with folic acid through α-or γ-carboxyl groups for antitumor efficacy. The isomeric block copolymers, α-and γ-folate-polyethyleneglycoldistearoyl phosphatidylethanolamine (α-and γ-Fol-PEG-DSPE), were produced by solid phase peptide synthesis. Three types of doxorubicin (DOX)-loaded polymeric micelles (MPEG-DSPE-DOX and α-/ γ-Fol-PEG-DSPE-DOX micelles) were prepared via the film formation method. Compared with MPEG-DSPE-DOX micelles, the α-/ γ-Fol-PEG-DSPE-DOX micelles presented a higher cellular uptake behavior in the live cell study. Cell viability percentages were 81.8%, 57.3%, 56.6% at 2 hours for MPEG-DSPE-DOX, α-and γ-Fol-PEG-DSPE-DOX micelles, respectively (p<0.05). Using the KB xenograft tumor model, both α-and γ-folate-conjugated micelles were found to have better antitumor effects with lower toxicity in comparison with MPEG-DSPE-DOX micelles. No difference in in vivo antitumor efficacy was found between α-and γ-Fol-PEG-DSPE-DOX micelles. The folate-conjugated micelles might be a potentially useful strategy for tumor targeting of therapeutic agents, whether grafting with folic acid through α-or γ-carboxyl groups.

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Folate receptor targeted biodegradable polymeric doxorubicin micelles

Cited by 568 publications

References 23 publications

Drug transport to brain with targeted nanoparticles

Drug transport to brain with targeted nanoparticles

Evaluation of Surfactants-Assisted Folic Acid-Loaded Pectin Submicrospheres: Characterization and Hemocompatibility Assay

Isomeric Folate-Conjugated Polymeric Micelles Bind to Folate Receptors and Display Anticancer Effects

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