Self-assembled drug delivery systems. Part 6: In vitro/in vivo studies of anticancer N-octadecanoyl gemcitabine nanoassemblies

Jin, Yiguang; Lian, Yanju; Du, Lina; Wang, Shuangmiao; Su, Chang; Gao, Chunsheng

doi:10.1016/j.ijpharm.2012.03.046

Cited by 24 publications

(10 citation statements)

References 28 publications

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“…The behavior of Langmuir monolayers at interfaces could reveal the amphiphilic and self-assembled properties of amphiphiles [27, 28]. The different π-A isotherms of blank RUB particles showed that RUB molecular area was 25 nm 2 and the collapse pressure of the RUB Langmuir monolayer was merely 33 mN/m (Fig.…”

Section: Resultsmentioning

confidence: 99%

A Novel Solubility-Enhanced Rubusoside-Based Micelles for Increased Cancer Therapy

2017

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Many anti-cancer drugs have a common problem of poor solubility. Increasing the solubility of the drugs is very important for its clinical applications. In the present study, we revealed that the solubility of insoluble drugs was significantly enhanced by adding rubusoside (RUB). Further, it was demonstrated that RUB could form micelles, which was well characterized by Langmuir monolayer investigation, transmission electron microscopy, atomic-force microscopy, and cryogenic transmission electron microscopy. The RUB micelles were ellipsoid with the horizontal distance of ~25 nm and vertical distance of ~1.2 nm. Insoluble synergistic anti-cancer drugs including curcumin and resveratrol were loaded in RUB to form anti-cancer micelles RUB/CUR + RES. MTT assay showed that RUB/CUR + RES micelles had more significant toxicity on MCF-7 cells compared to RUB/CUR micelles + RUB/RES micelles. More importantly, it was confirmed that RUB could load other two insoluble drugs together for remarkably enhanced anti-cancer effect compared to that of RUB/one drug + RUB/another drug. Overall, we concluded that RUB-based micelles could efficiently load insoluble drugs for enhanced anti-cancer effect.Electronic supplementary materialThe online version of this article (doi:10.1186/s11671-017-2054-4) contains supplementary material, which is available to authorized users.

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Section: Resultsmentioning

confidence: 99%

A Novel Solubility-Enhanced Rubusoside-Based Micelles for Increased Cancer Therapy

2017

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“…139 Gemcitabine prodrugs were also developed by Jin and co-workers through the conjugation of lipid derivatives such as cholesterol-phosphonyl gemcitabine and N -octadecanonyl gemcitabine. 140, 141 Li et al also successfully applied this lipid conjugation technique adefovir for the treatment of hepatitis, overcoming the drug’s hydrophilic disadvantage and proving the system’s capability to target hepatocytes while exhibiting an enzyme-triggered drug release. 142 Similarly, a lipidated Irinotecan prodrug was developed by Liang and co-workers that demonstrated increased cytotoxicity in cancer cells.…”

Section: Small Molecule Sapdsmentioning

confidence: 99%

Self-assembling prodrugs

et al. 2017

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Covalent modification of therapeutic compounds is a clinically proven strategy to devise prodrugs with enhanced treatment efficacies. This prodrug strategy relies on modified drugs that possess advantageous pharmacokinetic properties and administration routes over their parent drug. Self-assembling prodrugs represent an emerging class of therapeutic agents capable of spontaneously associating into well-defined supramolecular nanostructures in aqueous solutions. The self-assembly of prodrugs expands the functional space of conventional prodrug design, providing a possible pathway to more effective therapies as the assembled nanostructure possesses distinct physicochemical properties that can be tailored to specific administration routes and disease treatment. In this review, we will discuss the various types of self-assembling prodrugs in development, providing an overview of the methods used to control their structure and function and, ultimately, our perspective on their current and future potential.

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“…Classification of the anticancer drugs, lipids used for their derivatization and the nanoscale drug delivery system based on these prodrugs are reported in Table 1. A C C E P T E D M A N U S C R I P T Liposomes [37][38][39] Stearic acid C18 (stearoyl) Liposomes [36][37][38][39] Micelles [40,41] Polymer nanoparticles [42] Solid lipid nanoparticles [43][44][45][46] Self-assembled nanoparticles [47] Squalene Nanoparticles [50][51][52][53] [54-57, 59-63, 66, 67] Isoprenoids (monoisoprenoyl, geranyl farnesyl,polyisoprenoyl) Nanoparticles [68,69] Squalene Liposomes [58] Gemcitabine monofosfate Squalene Nanoparticles [64,65] Cytosine arabinoside Oleic acid Palmitic acid Liposomes [73] Cholesterol Liposomes [74] Glycerol substituted Liposomes [75] Phospholipids Thioether lipids (1-Salkylthioglycerols) Micelles [76] Squalene Liposomes [77][78] 5-fluorouracil Stearic acid Solid lipid nanoparticles [79] Floxuridine Octanoic acid; palmitic acid Liposomes [80][81][82] Octanoic acid; Solid lipid nanoparticles [84] Capecitabine Palmitic acid, Phytic acid,Oleic acid, Stearic acid, Linoleic acid, Linolenic acid Solid lipid nanoparticles, cubosomes, gyroids, double diamonds [85][86]…”

Section: Nanoparticulate Lipid Prodrugs For Drug Deliverymentioning

confidence: 99%

“…The possibility of incorporation of the stearoyl gemcitabine derivative (C18Gem) into other nanocarriers such as micelles [40][41], polymer nanoparticles [42], solid lipid nanoparticles (SLN) [43][44][45][46] or, self-assembled nanoparticles [47] has been also investigated.…”

Section: Antimetabolite Agentsmentioning

confidence: 99%