Importance of the field: Spontaneously constructed from block copolymers in aqueous media, the polymer micelle has been extensively studied as a potential carrier of poorly water-soluble drugs, but cellular uptake pathways and stability of micelles in blood have not yet been clearly understood. An in-depth insight into the physical and biological behaviors of polymer micelles is necessitated for designing next-generation micelles.Areas covered in this review: This review suggests possible solutions to improve micellar drug loading capacity, scrutinizes the parameters influencing the micelle stability in blood, and also discusses the fate of micelles in cellular and in vivo environment, respectively. Direct and indirect evidences from the literatures mostly published after 90's were collected, analyzed and summarized.What the reader will gain: A critical analysis of micelle's stability in vivo and micelle-cell interaction is provided to highlight the key issues to be addressed to affirm that micelle can pr...

Overcoming the barriers in micellar drug delivery: loading efficiency, in vivo stability, and micelle–cell interaction

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 blood-brain barrier (BBB) and require receptor-mediated transport through brain capillary endothelium to deliver their content into the brain parenchyma. Polysorbate 80-coated polybutylcyano-acrylate 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.

https://link.springer.com/content/pdf/10.1602%2Fneurorx.2.1.108.pdf

Drug transport to brain with targeted nanoparticles.

Pegylation, generally described as the molecular attachment of polyethylene glycols (PEGs) with different molecular weights to active drug molecules or surface treatment of drug-bearing particles with PEGs, is one of the most promising and extensively studied strategies with the goal of improving the pharmacokinetic behavior of the therapeutic drugs. A variety of PEGs, both linear and branched, with different molecular weights have been exploited successfully for use in this procedure in the form of reactive PEG species. Both reversible and irreversible PEG-drug conjugates have been prepared with relative advantages/disadvantages. The main pharmacokinetic outcomes of pegylation are summarized as changes occurring in overall circulation life-span, tissue distribution pattern, and elimination pathway of the parent drug/particle. Based on these favorable pharmacokinetic consequences leading to desired pharmacodynamic outcomes, a variety of proteins/peptides as well as small molecule drugs have been pegylated and evaluated successfully. Also a number of corresponding products have been approved by the U.S. FDA for specific clinical indications and some others are underway. In this article, the chemistry, rationale, strategies, pharmacokinetic outcomes, and therapeutic possibilities of pegylated drugs are reviewed with pharmacokinetic aspects presented with more details.

https://www.tandfonline.com/doi/pdf/10.1080/10717540600814402

Pharmacokinetic consequences of pegylation.

Iodinated blood pool contrast media for preclinical X-ray imaging applications--a review.

Fate of micelles and quantum dots in cells.

Block copolymers have a potential utility as drug carriers. In order to study their in vivo fate, the biodegradable block copolymer poly(D,L-lactide ethylene oxide) (PLA/PEO) (Mw 5000/5000) with a p-methoxyphenyl moiety was radio labeled with 1 2 5 I. The copolymer was [ 1 2 5 I] iodinated in the organic medium by a chloramine T method. The labeling efficiency was about 5%, and the agent was freed from [ 1 2 5 I] iodide by dialysis. The tissue distribution of radioactivity was determined at 5 min, 1, 2 and 24hrs after intravenous injection of male rats with 1 2 5 I-labeled copolymer in the dose 4.5-5.5 mg/kg. After administration of the labeled copolymer, a high concentration of radioactivity in the liver during the initial time intervals was found. At the subsequent intervals after dosing, an increase in 1 2 5 I activity in the bowels was determined. The distribution of radioactivity into inflamed areas was evaluated as well. The inflammatory-to-non-inflammatory muscle tissue ratios increased with time from 2.18 (5 min), 3.63 (1h) to 3.68 (2 hrs); after 24hrs, this ratio was significantly lower (1.70). The PLA/PEO copolymer exhibits a long residence time in the blood stream and, therefore, it could be employed as a drug delivery system for inflammatory and cancer treatment.

125I-labeled PLA/PEO block copolymer: Biodistribution studies in rats

The PLA-b-PEO block copolymers were studied as potential carriers for anti-inflammatory and anticancer drugs. The copolymers were labeled with 125I, and their micelles in physiological saline were prepared by dialysis. Copolymer 1, with Mw=12,360 (PLA/PEO=7000/5000), formed particles of about 300 nm in diameter (Rh was 150 nm), whereas copolymer 2, with Mw=20,470 (6000/14,000), made up micelles of about 72 nm in diameter (Rh was 35.8 nm). Their pharmacokinetic and biodistribution profiles were compared in normal rats and rats with carrageenan-induced inflammation after intravenous application of about 5 mg/kg of each copolymer. Copolymer 2, forming smaller particles, showed longer distribution and elimination half-lives. Both copolymers under study exhibited significantly higher uptake by inflammatory tissue compared with noninflammatory one. The study indicates that PLA-b-PEO copolymers, having different molecular weight of the chains, have similar biological behavior in most organs and tissues. Differen...

Pharmacokinetics and distribution of 125I-PLA-b-PEO block copolymers in rats.

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125I-labeled PLA/PEO block copolymer: Biodistribution studies in rats

Pharmacokinetics and distribution of 125I-PLA-b-PEO block copolymers in rats.