Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: Synthesis, characterization, and in vivo biodistribution

Saravanakumar, G.; Min, Kyung Hyun; Min, Dong Sik; Kim, Ah Young; Lee, Chang Moon; Cho, Yong Woo; Lee, Sang Cheon; Kim, Kwangmeyung; Jeong, Seo Young; Park, Kinam; Park, Jae Hyung; Kwon, Ick Chan

doi:10.1016/j.jconrel.2009.06.015

Cited by 91 publications

(60 citation statements)

References 32 publications

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“…Among the drug delivery systems, self-assembled nanoparticles have been studied for the encapsulation and sustained release of poorly soluble drugs. [13][14][15] Amphiphilic polymers can be used to form nanoparticles with a hydrophobic core and a hydrophilic shell. This structure enables the encapsulation and delivery of poorly soluble drugs, extending the circulation time of nanoparticles in the bloodstream.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Kim¹,

Termsarasab²,

Cho³

et al. 2014

IJN

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Low-molecular-weight heparin (LMWH)–stearylamine (SA) conjugates (LHSA)-based self-assembled nanoparticles were prepared for intravenous delivery of docetaxel (DCT). 1-Ethyl-3-(3-dimethylaminopropyl) carbodiimide and N -hydroxysuccinimide were used as coupling agents for synthesis of LHSA conjugates. The physicochemical properties, in vitro antitumor efficacy, in vitro cellular uptake efficiency, in vivo antitumor efficacy, and in vivo pharmacokinetics of LHSA nanoparticles were investigated. The LHSA nanoparticles exhibited a spherical shape with a mean diameter of 140–180 nm and a negative surface charge. According to in vitro release and in vivo pharmacokinetic test results, the docetaxel-loaded LHSA5 (LMWH:SA =1:5) nanoparticles exhibited sustained drug release profiles. The blank LHSA nanoparticles demonstrated only an insignificant cytotoxicity in MCF-7 and MDAMB 231 human breast cancer cells; additionally, higher cellular uptake of coumarin 6 (C6) in MCF-7 and MDAMB 231 cells was observed in the LHSA5 nanoparticles group than that in the C6 solution group. The in vivo tumor growth inhibition efficacy of docetaxel-loaded LHSA5 nanoparticles was also significantly higher than the Taxotere ® -treated group in the MDAMB 231 tumor-xenografted mouse model. These results indicated that the LHSA5-based nanoparticles could be a promising anticancer drug delivery system.

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Section: Introductionmentioning

confidence: 99%

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Kim¹,

Termsarasab²,

Cho³

et al. 2014

IJN

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“…Hence, formulation of these drugs is a challenging issue in cancer therapy [ 43 ] . Injectable or implantable formulations allow these drugs to bypass oral absorption barriers and gain direct entry into the general circulation or targeting site.…”

Section: Drugs Of Poor Oral Bioavailabilitymentioning

confidence: 99%

Drugs for Long Acting Injections and Implants

Shen

Burgess

2011

Long Acting Injections and Implants

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Long acting injections and implants have been developed for controlled drug delivery to improve therapeutic effects, decrease dosing frequency, and also avoid potential drug toxicity. Many pharmaceutical agents, such as biomacromolecules (e.g. peptides, proteins and gene therapeutics), drugs with poor bioavailability, and drugs for local delivery are good candidates for developing long acting injections and implants. However, not all drugs are suitable for these formulations (for example, drugs with high dose or narrow therapeutic index). IntroductionDrug formulations should deliver the API (active pharmaceutical agent) to the site of action at the correct therapeutic concentration for as long as the treatment is desired. The therapeutic and the physicochemical properties of a drug determine the preferred route of administration (oral or parenteral) as well as the most appropriate delivery systems.Due to convenience and patient acceptability, oral drug delivery is the most attractive and preferred route for administering medicines. However, some drugs cannot be tolerated via the oral route due to the acid environment and the variety of proteolytic enzymes (proteases) in the gastrointestinal tract (GIT). These conditions tend to degrade or metabolize drugs such as proteins and peptides, resulting in low bioavailability [ 1 ] . Moreover, patients who are unable to tolerate oral ingestion (e.g. patients with aspiration problems or GI disorders) require nonoral administration (e.g. parenteral administration) to receive medications and nutrition. Parenteral administration (e.g. intravenous, intramuscular, and subcutaneous) is also useful

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“…The reason for the low cytotoxicity could be that tripterine in both the formulations was completely associated with nanoparticles and released in a controlled manner over 24 hours. 34 The cellular uptake of the CT-NLCs was higher than that of the T-NLCs. This result could be related to the properties of the CPP, which is composed mainly of arginine and leucine residues, which confer a positive charge to the nanoparticles; nanoparticle uptake is enhanced by interactions between the CPP and the negatively charged components of the cell membrane.…”

mentioning

confidence: 91%

Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine

Chen

Yuan²,

Zhou³

et al. 2012

IJN

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Purpose: To develop nanostructured-lipid carriers (NLCs) coated with cell-penetrating peptides (CPP) for improving the oral bioavailability of tripterine. Methods: We prepared CPP-coated tripterine-loaded NLCs (CT-NLCs) by using a solvent evaporation method, and determined their physical properties. In vitro drug release was determined by using a dialysis bag diffusion technique, and intestinal toxicity was evaluated by performing MTT assay using Caco-2 cells. In vivo absorption was studied in an in situ rat intestinal perfusion model, and oral bioavailability was examined in beagles. Results: The average particle size, zeta potential, and encapsulation efficiency of the optimized CT-NLCs were 126.7 ± 9.2 nm, 28.7 ± 3.4 mV, and 72.64% ± 1.37%, respectively. The CT-NLCs showed a controlled release profile in vitro and had significantly lower intestinal cytotoxicity than the tripterine solution (P , 0.05). The absorption levels of tripterine from the CT-NLCs in the rat duodenum and jejunum were markedly higher than with tripterine-loaded NLCs without the CPP coating (T-NLCs), and with tripterine solution. Pharmacokinetic study showed that the maximum concentration of the CT-NLCs was greater than that of the T-NLCs and tripterine suspension, and that the time to maximum concentration of the CT-NLCs as well as the T-NLCs, was longer than that of the tripterine suspension. The relative oral bioavailability of the CT-NLCs compared to that of tripterine suspension and T-NLCs were 484.75% and 149.91% respectively. Conclusion: The oral bioavailability of tripterine is dramatically increased by CT-NLCs. Therefore, CT-NLCs seem to be a promising carrier for oral delivery of tripterine.

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Hydrotropic oligomer-conjugated glycol chitosan as a carrier of paclitaxel: Synthesis, characterization, and in vivo biodistribution

Cited by 91 publications

References 32 publications

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Preparation and characterization of self-assembled nanoparticles based on low-molecular-weight heparin and stearylamine conjugates for controlled delivery of docetaxel

Drugs for Long Acting Injections and Implants

Effect of cell-penetrating peptide-coated nanostructured lipid carriers on the oral absorption of tripterine

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