Micelles from lipid derivatives of water-soluble polymers as delivery systems for poorly soluble drugs

Lukyanov, Anatoly N.; Torchilin, Vladimir P.

doi:10.1016/j.addr.2003.12.004

Cited by 595 publications

(414 citation statements)

References 68 publications

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“…3, f1, f2, i1 and i2) N,N,N',N',N"-pentaacetic acid; EDC·HCl, N-(3-dimethylaminopropyl) 3 The ester bonds of the protected Lam-D conjugates were labile; hence, to avoid problems with hydrolysis, we minimized the deprotection steps after condensation. 4 The yield for the deprotection was 84% working on a 20-30 mg scale.…”

Section: Esterification and Synthesis Of Conjugates 1-4mentioning

confidence: 99%

Lamellarin D Bioconjugates II: Synthesis and Cellular Internalization of Dendrimer and Nuclear Location Signal Derivatives

et al. 2009

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BarcelonaRECEIVED DATE (to be automatically inserted after your manuscript is accepted if required according to the journal that you are submitting your paper to) TITLE RUNNING HEAD. Lamellarin D -NLS and DTPA conjugates.ABSTRACT: The design and synthesis of Lamellarin D conjugates with a nuclear localization signal peptide and a poly(ethylene glycol)-based dendrimer are described. Conjugates 1-4 were obtained in 8-84% overall yields from the corresponding protected Lamellarin D. Conjugates 1 and 4 are 1.4 to 3.3-fold more cytotoxic than the parent compound against three human tumor cell lines (MDA-MB-231 breast, A-549 lung, and HT-29 colon). Besides, conjugates 3, 4 showed a decrease in activity potency in BJ skin fibroblasts, a normal cell culture. Cellular internalization was analyzed and nuclear distribution pattern was observed for 4, which contains a nuclear localization signalling sequence.

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Section: Esterification and Synthesis Of Conjugates 1-4mentioning

confidence: 99%

Lamellarin D Bioconjugates II: Synthesis and Cellular Internalization of Dendrimer and Nuclear Location Signal Derivatives

et al. 2009

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“…[19] Since PEG is easily oxidized, the lower molecular weight of PEG is preferable and generally use as a solvent and higher molecular weight is used as a component in the micelle, possibly due to the fact that oxidative degradation significantly decreases with increasing molar mass. [12] There are some other polymers which are used as hydrophilic shell-forming polymer including: a. Poly (N-vinyl-2-pyrrolidone) [20] The surfactant molecules are separated (left). Above CMC: Surfactant molecules are assembled and formed a micelle (right) [8] b. Poly(N-(2-hydroxypropyl) methacrylamide): It is a nonimmunologic polymer which is multifunctional and several ligands can be attached to, to use in targeting drug delivery.…”

Section: Shell Of Polymeric Micellesmentioning

confidence: 99%

Untitled

Esfahani¹

2017

AJP

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Almost half of the orally administered drugs are poorly soluble in water; therefore they have low absorption in the gastrointestinal (GI) tract. In addition, drugs which are administered orally must remain stable during passing the GI tract, despite different physiologic challenges such as pH changes, and dilution effect. Hence, new methods are needed to increase the solubility of these drugs while making them more stable in the physiologic environment. Polymeric micelles are one of the new nanocarriers which are able to increase the solubility of these drugs while protecting them from pH changes, dilution effect, and biological barriers such as filtration in the spleen or scavenging by the phagocytic system. This article provides some important and basic information including polymeric micelles characteristics, structure, and preparation.

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“…For example, Torchilin's group has synthesized several PEGdiacyllipid conjugates, in which the hydrophobic segments are lipids of various acyl chains such as phosphatidylethanolamine (PEG-PE) (19). Due to the strong hydrophobic interactions between the double acyl chains (20), the PEG-PE conjugates can form stable micelles with very low CMC value (~10 −5 M) (21). These micelles can solubilize many types of poorly water-soluble drugs including paclitaxel (2), tamoxifen (2), porphyrin (2), camptothecin (22), and vitamin K3 (23).…”

Section: Introductionmentioning

confidence: 99%

“…These micelles can solubilize many types of poorly water-soluble drugs including paclitaxel (2), tamoxifen (2), porphyrin (2), camptothecin (22), and vitamin K3 (23). The PEG-PE micelles exhibit favorable stability, longevity in blood and tumor accumulation via the EPR effect (20,24). In contrast to liposomes (25), the small size of micelles enables them to effectively penetrate the vasculature of tumors, even for those with very low cutoff size (26).…”

Section: Introductionmentioning

confidence: 99%

Polymeric Micelles: Nanocarriers for Cancer-Targeted Drug Delivery

2014

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Abstract. Polymeric micelles represent an effective delivery system for poorly water-soluble anticancer drugs. With small size (10-100 nm) and hydrophilic shell of PEG, polymeric micelles exhibit prolonged circulation time in the blood and enhanced tumor accumulation. In this review, the importance of rational design was highlighted by summarizing the recent progress on the development of micellar formulations. Emphasis is placed on the new strategies to enhance the drug/carrier interaction for improved drugloading capacity. In addition, the micelle-forming drug-polymer conjugates are also discussed which have both drug-loading function and antitumor activity.

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Micelles from lipid derivatives of water-soluble polymers as delivery systems for poorly soluble drugs

Cited by 595 publications

References 68 publications

Lamellarin D Bioconjugates II: Synthesis and Cellular Internalization of Dendrimer and Nuclear Location Signal Derivatives

Lamellarin D Bioconjugates II: Synthesis and Cellular Internalization of Dendrimer and Nuclear Location Signal Derivatives

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Polymeric Micelles: Nanocarriers for Cancer-Targeted Drug Delivery

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