The Study of Tacrolimus-Loaded Polyion Complex Micelles for Oral Delivery

Chen, Yan; Jiao, Yan; Ge, Yanxiu; Liu, Guoxia; Xu, Wei Da; Li, Lingbing

doi:10.1166/jbn.2017.2403

Cited by 7 publications

(4 citation statements)

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“…The different CMC values may be due to the different linkers between PEG and UA (Bao et al, 2014). The small CMC values of both micellar preparations could protect them against dilution effects in the blood circulation, thereby improving their stability (Chen et al, 2017). Subsequently, the stability of these micelles in PBS and PBS supplemented with 10% FBS was investigated.…”

Section: Micellar Preparation and Characterizationmentioning

confidence: 99%

A novel redox-responsive ursolic acid polymeric prodrug delivery system for osteosarcoma therapy

et al. 2021

Drug Delivery

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Ursolic acid (UA), found widely in nature, exerts effective anti-tumoral activity against various malignant tumors. However, the low water solubility and poor bioavailability of UA have greatly hindered its translation to the clinic. To overcome these drawbacks, a simple redox-sensitive UA polymeric prodrug was synthesized by conjugating UA to polyethylene glycol using a disulfide bond. This formulation can self-assemble into micelles (U-SS-M) in aqueous solutions to produce small size micelles ($62.5 nm in diameter) with high drug loading efficiency ($16.7%) that exhibit pH and reduction dual-sensitivity. The cell and animal studies performed using the osteosarcoma MG-63 cell line and MG-63 cancer xenograft mice as the model systems consistently confirmed that the U-SS-M formulation could significantly prolong the circulation in blood and favor accumulation in tumor tissue. Targeted accumulation allows the U-SS-M to be effectively internalized by cancer cells, where the rapid release of UA is favored by a glutathione-rich and acidic intracellular environment, and ultimately achieves potent antitumor efficacy.

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Section: Micellar Preparation and Characterizationmentioning

confidence: 99%

A novel redox-responsive ursolic acid polymeric prodrug delivery system for osteosarcoma therapy

et al. 2021

Drug Delivery

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“…The preparation of IGG-loaded TPGS/soluplus mixed micelles was carried out by film hydration method [ 24 ]. In short, IGG (2 mg), soluplus (60 mg), TPGS (20 mg) was precisely weighed and dissolved in 20 mL methanol in a round bottom flask by stirring at room temprature.…”

Section: Methodsmentioning

confidence: 99%

Preparation, evaluation and metabolites study in rats of novel Isoginkgetin-loaded TPGS/soluplus mixed nanomicelles

Xue¹,

Chen²,

Li³

et al. 2020

Journal of Food and Drug Analysis

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At present, cancer is one of the most lethal diseases in the world, and researchers are committed to developing effective anticancer drugs. Isoginkgetin (IGG) is a kind of biflavone with the potential to treat cancer due to the features of altering the cell cycle and inhibiting tumor cell infiltration. However, its solubility, absorbability and bioavailability are poor, so in this study, IGG was prepared into mixed nanomicelles and evaluated in vitro and in vivo. After condition optimization, IGG-loaded TPGS/soluplus mixed nanomicelles with particle size of 62.34 ± 1.10 nm, entrapment efficiency of 96.92 ± 0.66% and drug loading of 2.42 ± 0.02% were successfully prepared. The physicochemical properties of the nanomicelles were stable within 60 days, and the cytotoxicity of the nanomicelles was significantly higher than that of IGG. The metabolism results showed that 32 kinds of metabolites of IGG and 21 kinds of IGG-loaded nanomicelles were detected. The metabolites of IGG can only be detected in feces of rats, while the metabolites of IGG-loaded nanomicelles can be detected in plasma, bile, urine and feces. All these indicated that after prepared into nanomicelles, the stability, solubility, cytotoxicity and bioavailability of IGG were increased significantly, which provided a new choice for the development of new drugs.

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“…Finally, PIC-micelles have been used to accommodate various low-molar mass hydrophilic drugs which, in most cases, coassociate in aqueous media with the double hydrophilic oppositely charged copolymer(s) into nanosized drug delivery vehicles [29][30][31]. On the other hand, the reports concerning the evaluation of PIC micelles as nanovehicles for hydrophobic active compounds are still limited [32][33][34]. In the majority of cases, one of the pairs of copolymers involved in the electrostatically-driven association besides the charged groups possesses hydrophobic segments in order to accommodate the drug via hydrophobic interactions.…”

Section: Introductionmentioning

confidence: 99%

Solvent-Free Synthesis of Multifunctional Block Copolymer and Formation of DNA and Drug Nanocarriers

Kalinova,

Mladenova,

Petrova

et al. 2023

Nanomaterials

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The synthesis of well-defined multifunctional polymers is of great importance for the development of complex materials for biomedical applications. In the current work, novel and multi-amino-functional diblock copolymer for potential gene and drug delivery applications was successfully synthesized. A highly efficient one-step and quantitative modification of an alkyne-functional polycarbonate-based precursor was performed, yielding double hydrophilic block copolymer with densely grafted primary amine side groups. The obtained positively charged block copolymer co-associated with DNA, forming stable and biocompatible nanosized polyplexes. Furthermore, polyion complex (PIC) micelles with tunable surface charge and decorated with cell targeting moieties were obtained as a result of direct mixing in aqueous media of the multi-amino-functional block copolymer and a previously synthesized oppositely charged block copolymer bearing disaccharide end-group. The obtained well-defined nanosized PIC–micelles were loaded with the hydrophobic drug curcumin. Both types of nanoaggregates (polyplexes and PIC–micelles) were physico-chemically characterized. Moreover, initial in vitro evaluations were performed to assess the nanocarriers’ potential for biomedical applications.

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The Study of Tacrolimus-Loaded Polyion Complex Micelles for Oral Delivery

Cited by 7 publications

References 0 publications

A novel redox-responsive ursolic acid polymeric prodrug delivery system for osteosarcoma therapy

A novel redox-responsive ursolic acid polymeric prodrug delivery system for osteosarcoma therapy

Preparation, evaluation and metabolites study in rats of novel Isoginkgetin-loaded TPGS/soluplus mixed nanomicelles

Solvent-Free Synthesis of Multifunctional Block Copolymer and Formation of DNA and Drug Nanocarriers

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