Publications (4)5.2 Total impact
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Article: Fabrication of cationic nanomicelle from chitosan-graft-polycaprolactone as the carrier of 7-ethyl-10-hydroxy-camptothecin.
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ABSTRACT: In this research, amphiphilic brush-like polycations were synthesized, and used to fabricate cationic nanomicelle as the carrier of 7-ethyl-10-hydroxy-camptothecin (SN-38), in order to enhance its cellular uptake, solubility and stability in aqueous media. In particular, cationic chitosan-graft-polycaprolactone (CS-g-PCL) copolymers were synthesized with a facile one-pot manner via ring-opening polymerization of epsilon-CL onto the hydroxyl groups of CS by using methanesulfonic acid as solvent and catalyst. The formation of CS-g-PCL nanomicelles was confirmed by fluorescence spectrophotoscopy and particle size measurements. It was found that all the nanomicelles showed spherical shapes with narrow size distributions. Their sizes ranged from 47 to 113 nm, and the zeta potentials ranged from 26.7 to 50.8 mV, depending on the grafting content of PCL in CS-g-PCL, suggesting their passive targeting to tumor tissue and endocytosis potential. Water-insoluble antitumor drug, SN-38, was easily encapsulated into CS-g-PCL nanomicelles by lyophilization method. In comparison with bare CS-g-PCL nanomicelles, the corresponding SN-38-loaded nanomicelles showed increased particle sizes and a little reduced zeta potentials. With an increase of grafting PCL content, the drug encapsulation efficiency (EE) and drug loading (DL) of the nanomicelles increased from 64.3 to 84.6% and 6.43 to 8.66%, respectively, whereas their accumulative drug release showed a tendency to decrease due to the enhanced hydrophobic interaction between hydrophobic drug and hydrophobic PCL segments in CS-g-PCL. Also, the CS-g-PCL nanomicelles effectively protected the active lactone ring of SN-38 from hydrolysis under physiological condition, due to the encapsulation of SN-38 into the hydrophobic cores in the nanomicelles. Compared with free SN-38, the SN-38-loaded nanomicelles showed essential decreased cytotoxicity against L929 cell line, and bare CS-g-PCL nanomicelles almost showed non-toxicity. These results suggested the potential utilization of the CS-g-PCL nanomicelles as the carriers of hydrophobic drugs with improving the delivery and release properties.Colloids and surfaces. B, Biointerfaces 04/2010; 76(2):475-82. · 2.60 Impact Factor -
Article: Fabrication of nanomicelle with enhanced solubility and stability of camptothecin based on alpha,beta-poly[(N-carboxybutyl)-L-aspartamide]-camptothecin conjugate.
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ABSTRACT: This research is aimed to develop a nanomicelle delivery system in order to enhance the solubility and stability of camptothecin (CPT) in aqueous media. In this case, alpha,beta-poly[(N-carboxybutyl)-L-aspartamide] (PBAsp)-CPT was conjugated by the esterification between PBAsp and 20-OH of CPT, and hence used to fabricate nanomicelles with a particle size between the pore size of blood capillary in normal tissue and that in tumor tissue. It was worthy of note that the drug-loaded system of PBAsp-CPT nanomicelle improved the solubility and stability of CPT in aqueous media. However, with an increase of the CPT loading in PBAsp-CPT, the solubility sharply decreased. Meanwhile, the sizes of PBAsp-CPT nanomicelles showed a tendency of increase. Moreover, the drug release of PBAsp-CPT nanomicelles displayed a linear sustaining profile, and hence resulted in the essential decrease of cytotoxicity to L929 cell line. The assembled nanomicelles based on the PBAsp-CPT conjugates showed a great potential as polymer prodrug of tumor therapy, and the controlled nano-scale might achieve the passive tumor targeting.Colloids and surfaces. B, Biointerfaces 09/2009; 75(2):543-9. · 2.60 Impact Factor -
Article: One-step synthesis of amino-reserved chitosan-graft-polycaprolactone as a promising substance of biomaterial
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ABSTRACT: One-step approach was developed to synthesize amino-reserved chitosan-graft-polycaprolactone (CS-g-PCL) by grafting ε-CL oligomers onto the hydroxyl groups of CS via ring-opening polymerization by using methanesulfonic acid as solvent and catalyst. The controllable grafting content of PCL within CS-g-PCL provided the possibility to manipulate the biodegradation rate, hydrophilicity, and hence the cytotoxicity of CS-g-PCL. As a result, the specimen synthesized from the feed molar ratio of glucosamine units in CS vs. ε-CL as 1:12 showed equivalent cytotoxicity to the neat CS and PCL against KB cell line, and the cell viability was almost close to 100%. In addition, CS-g-PCL exhibited good solubility in organic solvents, facilitating formation of PCL/CS-g-PCL blend nanofibers via electrospinning with the use of DMF/CHCl3 as solvent. Owing to the enhanced cellular attachment results from cationic amino groups, it is promising that these copolymers are ideal substances for developing drug carriers and tissue engineering scaffolds.Carbohydrate Polymers. -
Article: Fabrication of nanomicelle with enhanced solubility and stability of camptothecin based on α,β-poly[(N-carboxybutyl)-l-aspartamide]–camptothecin conjugate
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ABSTRACT: This research is aimed to develop a nanomicelle delivery system in order to enhance the solubility and stability of camptothecin (CPT) in aqueous media. In this case, α,β-poly[(N-carboxybutyl)-l-aspartamide] (PBAsp)–CPT was conjugated by the esterification between PBAsp and 20-OH of CPT, and hence used to fabricate nanomicelles with a particle size between the pore size of blood capillary in normal tissue and that in tumor tissue. It was worthy of note that the drug-loaded system of PBAsp–CPT nanomicelle improved the solubility and stability of CPT in aqueous media. However, with an increase of the CPT loading in PBAsp–CPT, the solubility sharply decreased. Meanwhile, the sizes of PBAsp–CPT nanomicelles showed a tendency of increase. Moreover, the drug release of PBAsp–CPT nanomicelles displayed a linear sustaining profile, and hence resulted in the essential decrease of cytotoxicity to L929 cell line. The assembled nanomicelles based on the PBAsp–CPT conjugates showed a great potential as polymer prodrug of tumor therapy, and the controlled nano-scale might achieve the passive tumor targeting.Colloids and Surfaces B: Biointerfaces. 75(2):543-549.
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Institutions
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2010
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Second Military Medical University, Shanghai
Shanghai, Shanghai Shi, China
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