- Self-crosslinkable and intracellularly decrosslinkable biodegradable micellar nanoparticles: A robust, simple and multifunctional nanoplatform for high-efficiency targeted cancer chemotherapy
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Nanomedicines based on biodegradable micelles offer a most promising treatment for malignant tumors. Their clinical effectiveness, however, remains to be improved. Here, we report that self-crosslinkable and intracellularly decrosslinkable micellar nanoparticles (SCID-Ms) self-assembled from novel amphiphilic biodegradable poly(ethylene glycol)-b-poly(dithiolane trimethylene carbonate) block copolymer achieve high-efficiency targeted cancer chemotherapy in vivo. Interestingly, doxorubicin (DOX)-loaded SCID-Ms showed favorable features of superb stability, minimal drug leakage, long circulation time, triggered drug release inside the tumor cells, and an unprecedented maximum-tolerated dose (MTD) of over 100?mg DOX equiv./kg in mice, which was at least 10 times higher than free drug. The in vivo studies in malignant B16 melanoma-bearing C57BL/6 mice revealed that DOX-SCID-Ms at a dosage of 30?mg DOX equiv./kg could effectively suppress tumor growth and prolong mice survival time without causing obvious systemic toxicity. Moreover, DOX-SCID-Ms could be readily decorated with a targeting ligand like cRGD peptide. The biodistribution studies showed that cRGD20/DOX-SCID-Ms had a high tumor accumulation of 6.13% ID/g at 6?h post injection, which was ca. 3-fold higher than that for clinically used pegylated liposomal doxorubicin (DOX-LPs). Accordingly, cRGD20/DOX-SCID-Ms exhibited significantly better therapeutic efficacy and lower side effects than DOX-LPs in B16 melanoma-bearing mice. These self-regulating biodegradable micellar nanoparticles offer a robust, multifunctional and viable nanoplatform for targeted cancer chemotherapy.
- Zou, Yan,Fang, Ya,Meng, Hao,Meng, Fenghua,Deng, Chao,Zhang, Jian,Zhong, Zhiyuan
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- The influence of OH groups in [Fe(CO)3]2[(μ- ECH2)2C(CH2OH)2] (E = S, Se) complexes toward the cathodic process
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[FeFe] hydrogenase model complexes [Fe(CO)3]2[(μ- ECH2)2C(CH2OH)2] (E = S (1) or Se (2)) containing CH2OH bridgehead substituents were synthesized via reaction of equimolar amounts of 4, 4-bis(hydroxymethyl)-1, 2-dithiolane (A) or 4, 4-bis(hydroxymethyl)-1, 2-diselenolane (B) with Fe3(CO) 12 in toluene at 100°C. The presence of OH groups in complexes 1 and 2 is found to influence the cathodic processes and their potentials. The catalytic reduction of acetic acid (AcOH) occurs by the anions 1- and 2-, while the neutral complexes are procatalysts. Copyright
- Trautwein, Ralf,Almazahreh, Laith R.,Goerls, Helmar,Weigand, Wolfgang
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- Disulfide-containing five-membered ring cyclic carbonate functional groups of monomer and its preparation method
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Disclosed are a cyclic carbonate monomer containing a double-sulfur five-membered ring functional group, and preparation method thereof. The cyclic carbonate monomer can be simply and efficiently synthesized without protection and deprotection processes. The cyclic carbonate monomer of the present invention can be utilized to obtain polycarbonate having a controllable molecular weight and molecular weight distribution via ring opening polymerization, and has biodegradability and reduction-sensitive reversible crosslinking properties. The present invention can be used in a carrier having controllably released drug, a biological tissue scaffold or a biochip.
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Paragraph 0046
(2017/02/09)
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- Molecular rods based on oligo-spiro-thioketals
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We report on an extension of the previously established concept of oligospiroketal (OSK) rods by replacing a part or all ketal moieties by thioketals leading to oligospirothioketal (OSTK) rods. In this way, some crucial problems arising from the reversible formation of ketals are circumvented. Furthermore, the stability of the rods toward hydrolysis is considerably improved. To successfully implement this concept, we first developed a number of new oligothiol building blocks and improved the synthetic accessibility of known oligothiols, respectively. Another advantage of thioacetals is that terephthalaldehyde (TAA) sleeves, which are too flexible in the case of acetals can be used in OSTK rods. The viability of the OSTK approach was demonstrated by the successful preparation of some OSTK rods with a length of some nanometers.
- Wessig,Gerngro?,Freyse,Bruhns,Przezdziak,Schilde,Kelling
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p. 1125 - 1136
(2016/02/19)
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- ANTIOXIDANT POLYMERS CONTAINING [1,2]-DITHIOLANE MOIETIES AND USES THEREOF
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The present invention describes polymers containing 1,2-dithiolanes capable of acting as scavengers of free radicals, metals and reactive oxygen species. Also described are methods of synthesizing the antioxidant 1,2-dithiolane derivatives and polymerization thereof to produce biodegradable antioxidant polymers. The antioxidant polymers of the present invention may be used to treat diseases or conditions caused by oxidative stress and other free radical mediated conditions. The antioxidant polymers may also be used for the preparation of antioxidant particulate delivery devices of therapeutic agents.
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Page/Page column 53-54
(2008/12/07)
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- Sensitive and selective method and device for the detection of trace amounts of a substance
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A piezoelectric crystal element and a sensor utilizing the same are presented for use in a sensor device for identifying at least one foreign material from environment. The crystal element comprises at least one crystal resonator in the form of a inverted mesa structure, which has a membrane-like region and has a certain resonance frequency value. A surface region of the crystal resonator is modified by reactive molecules of a kind capable of interacting with the foreign material to yield a reaction product that effects a change in the resonance frequency of the crystal resonator from said certain resonance frequency value. This change is indicative of the identity and quantity of the foreign material.
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Page/Page column 9-10
(2010/11/27)
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- Preparation of cyclic disulfides from bisthiocyanates
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A mild method for the preparation of disulfides from acyclic bisthiocyanates is presented. The method involves cleavage of thiocyanates with TBAF to form the cyclic disulfides in moderate to good yield. The method can also be applied to the synthesis of a
- Burns, Christopher J.,Field, Leslie D.,Morgan, Jacqueline,Ridley, Damon D.,Vignevich, Valentina
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p. 6489 - 6492
(2007/10/03)
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