Non-stealth (poly(lactic acid/albumin)) and stealth (poly(lactic acid-polyethylene glycol)) nanoparticles as injectable drug carriers

Verrecchia, T.; Spenlehauer, G.; Bazile, Didier; Murry-Brelier, Anne; Archimbaud, Y.; Veillard, M.

doi:10.1016/0168-3659(95)00053-b

Cited by 175 publications

(103 citation statements)

References 23 publications

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“…81 Within 5 min, however, ϳ50% (PEG 20000 ) to 75% (PEG 5000 ) of injected nanoparticles (estimated from the blood clearance curves) had been cleared from the blood compartment (compared with 95% with control PLGA nanoparticles). In another study performed in rats, the blood half-lives of [ 14 C]PLA-labeled mPEG-PLA 30,000 nanoparticles with PEG molecular weight of 2000 73 (205 nm diameter) or 5000 78 (140 Ϯ 60 nm) were markedly higher (6 h) and independent of the PEG molecular weights. Less prolonged blood circulation times were observed with PLGA nanoparticles coated with PLA 3000 -PEG 4000 (147 Ϯ 3.6nm) or PLA 3000 -PEG 5000 (161 Ϯ 3.7nm) (T [1/2] ϭ 15 min and T [1/2] ϭ 1 h, respectively, estimations from the blood clearance curves).…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…Covalent linkage of the PEG coating and sufficient PLA block molecular weight is essential to ensure a sufficient stability and to avoid loss of the coating benefit by desorption and/or displacement in vivo. 57,72,73,80 In mice, blood circulation times of 111 In-labeled mPEG-PLGA 5000-20000 nanoparticles (140 Ϯ 10 nm diameter) increased compared to PLGA ones with an advantage to the higher PEG molecular weight. 81 Within 5 min, however, ϳ50% (PEG 20000 ) to 75% (PEG 5000 ) of injected nanoparticles (estimated from the blood clearance curves) had been cleared from the blood compartment (compared with 95% with control PLGA nanoparticles).…”

Section: Pharmacokineticsmentioning

confidence: 99%

“…44,72 Blood half-lives are generally around 2-3 min. 44,[73][74][75] After intravenous administration, the first step of the process that leads to the nanoparticle uptake by the MPS is the opsonization phenomenon. Opsonins, including complement proteins, apolipoproteins, fibronectin, and Igs, 31 interact with specific membrane receptors of monocytes and tissue macrophages, resulting in recognition and phagocytosis.…”

Section: Pharmacokineticsmentioning

confidence: 99%

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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: Pharmacokineticsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

Section: Pharmacokineticsmentioning

confidence: 99%

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Drug transport to brain with targeted nanoparticles

2005

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“…[43,44,45] Blood half-lives are generally around 2-3 min. [46,47] .It is generally admitted that hydrophobic surfaces promote protein adsorption and that negative surfaces are activators of the complement system.…”

Section: Advantages Of Polymeric Nanoparticlesmentioning

confidence: 99%

Drug Delivery to The Brain Using Polymeric Nanoparticles: A Review

Bhatt¹,

Ganesh²,

Kothiyal³

2013

Int. J. Pharma Life Sci.

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Nanoparticle drug carriers consist of solid biodegradable particles in size ranging from 10 to 1000 nm (50-300 nm generally). The use of minute particles as drug carriers for targeted treatment has been studied over a long period of time. A selective accumulation of active substances in target tissues has been demonstrated for certain so-called nanocarrier systems that are administered bound to pharmaceutical drugs. Great expectations are placed on nanocarrier systems that can overcome natural barriers such as the blood-brain barrier (BBB) and transport the medication directly to the desired tissue and thus heal neurological diseases that were formerly incurable. Polymeric Nanoparticle have been shown to be promising carriers for CNS drug delivery due to their potential both in encapsulating drugs, hence protecting them from excretion and metabolism, and in delivering active agents across the blood -brain barrier without inflicting any damage to the barrier. Different polymers have been used and different strategies like surface modification have been done to increase the retention time of nanoparticles.

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“…Recently, a new class of the drug delivery systems has emerged that is based on nano-sized polymeric micelles with a core-shell structure formulated through the selfassembly of PEG-block-poly(D,L-lactide) (PLA) copolymer (PEG-b-PLA). 34,35 These systems exhibit improved biocompatibility, nontoxicity, long blood-circulation time, [36][37][38] and biodegradability. 39,40 The hydrophobic PLA core is able to accommodate hydrophobic drugs, and the brush-like hydrophilic PEG shell prevents protein adsorption and subsequent non-specific uptake by the reticuloendothelial system after intravenous injection.…”

Section: Introductionmentioning

confidence: 99%

Boron neutron capture therapy assisted by boron-conjugated nanoparticles

Sumitani

Nagasaki

2012

Polym J

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For high-performance boron neutron capture therapy (BNCT), core-shell-type biodegradable nanoparticles possessing boron clusters in their cores are designed to improve their accumulation tendency in the tumor region. The copolymerization of styrene carrying carborane with a poly(ethylene glycol)-block-poly(lactide) copolymer (PEG-b-PLA) that possesses an acetal group at its PEG end and a methacryloyl group at its PLA end (acetal-PEG-b-PLA-MA) was performed in an aqueous medium. As the acetal-PEG-b-PLA-MA forms a polymeric micelle in an aqueous medium, the carborane monomer in the hydrophobic core is solubilized, and the carborane in the core of the micelle is given covalent conjunction. Two carborane compounds, carborane with a mono-vinylbenzyl group [1-(4-vinylbenzyl)-closo-carborane (VB-carborane)] and carborane with di-vinylbenzyl groups [1,2-bis(4-vinylbenzyl)-closo-carborane ((VB) 2 -carborane)], were newly prepared and employed for the core polymerizations. The encapsulation efficiency of the VB-carborane in the micelles is much higher than that of the (VB) 2 -carborane. This improved efficiency is most likely caused by the interaction of the hydrogen bonding of the VB-carborane with the polymer micelle matrix, while no hydrogen bonding sites remain in the case of the (VB) 2 -carborane. The obtained corepolymerized and boron-conjugated micelles (PM, which were prepared from VB-carborane) showed extremely high stability under physiological conditions, which suppressed the leakage of boron compounds owing to the existence of the covalent bonds. The accumulation of the PM (7.2 ID% per g) in tumors is much higher than that of the non-polymerized micelles (NPM) (0.7 ID% per g) under the same conditions (at 24 h after injection) because of the enhanced stability of the micelles under physiological conditions. In addition, thermal neutron irradiation experiments indicated significant suppression of the growth of tumor volume in tumor-bearing mice treated with the PM. It is important to note that the PM administered via intravenous injection were excreted almost completely from the major organs, except for the tumor, after a week. Therefore, these boronconjugated micelles represent a promising approach to the creation of a novel boron carrier for BNCT.

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Non-stealth (poly(lactic acid/albumin)) and stealth (poly(lactic acid-polyethylene glycol)) nanoparticles as injectable drug carriers

Cited by 175 publications

References 23 publications

Drug transport to brain with targeted nanoparticles

Drug transport to brain with targeted nanoparticles

Drug Delivery to The Brain Using Polymeric Nanoparticles: A Review

Boron neutron capture therapy assisted by boron-conjugated nanoparticles

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