Lipid, Sugar and Liposaccharide Based Delivery Systems

Wong, A. K.; Tóth, István

doi:10.2174/0929867013372535

Cited by 97 publications

(44 citation statements)

References 33 publications

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“…On the basis of these results, we postulate that bGal-NONOate is preferentially transported into cells through monosaccharide transporters on cell membranes. It has been reported that there are different types of monosaccharide transporters on the cell membrane such as sodium ion-dependent active transporter (SGLT1) and sodium ion-independent facilitative transporter (GLUT5), and attachment of one of monosaccharides transported by these transporters to drugs can increase the drug absorption [20]. These glycosylated conjugates tend to be accumulated inside cells according to the expression of specific hexose transporters on the cell membrane.…”

Section: Discussionmentioning

confidence: 99%

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A Glycosylated Nitric Oxide Donor, β‐Gal‐NONOate, and its Site‐specific Antitumor Activity

Chang¹,

Shi²,

Li³

et al. 2006

Archiv der Pharmazie

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So far, nitric oxide (NO) donors have been applied to various aspects of antitumor therapy. To selectively sensitize tumor cells and avoid unwanted side effects, we recently synthesized a beta-galactosidase-activatable NO-releasing compound, beta-galactosyl-pyrrolidinyl diazeniumdiolate (beta-Gal-NONOate). In this study, we first verified its superiority over its parent diazeniumdiolate (NONOate) in terms of targeted intracellular NO-releasing and antitumor activity with 9L/LacZ cells (rat glioma cell line 9L with transformed LacZ gene) in vitro. beta-Gal-NONOate only released NO when hydrolyzed by induced beta-galactosidase in 9L/LacZ cells, which led to its more powerful cytotoxicity than that of NONOate. The results showed that beta-Gal-NONOate produced higher NO levels than NONOate in 9L/LacZ cells at equal concentration, and hence induced optimal NO levels for antitumor activity. However, in 9L cells, beta-Gal-NONOate showed less toxicity than NONOate. Therefore, it is demonstrated that beta-Gal-NONOate is a site-specific prodrug for targeting NO intracellularly as a beta-galactosidase-sensitive NO donor, and it is also expected to be a promising probe in numerous experimental settings and a potential therapeutic drug for antitumor treatment.

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Section: Discussionmentioning

confidence: 99%

“…Moreover, it has been suggested that human tumor cells can overexpress one or more of these transporters [20]. However, in normal mammalian cells, there is no LacZ gene expression.…”

Section: Discussionmentioning

confidence: 99%

A Glycosylated Nitric Oxide Donor, β‐Gal‐NONOate, and its Site‐specific Antitumor Activity

Chang¹,

Shi²,

Li³

et al. 2006

Archiv der Pharmazie

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“…Despite these advances in physiological modeling and simulation of drug adsorption from the gastrointestinal tract, the fundamental process, which is the small intestinal transit flow, has not been characterized [4][5][6].…”

Section: Introductionmentioning

confidence: 99%

Digestion characteristics and kinetic analysis of bio-molecules in a simulated human intestinal system

Choi¹,

Buisson²,

Kim³

2015

Integr Food Nutr Metab

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We designed and assembled a simulated human intestinal system (SHIS) consisting of a stomach and a small intestine. Each reactor vessel has several ports such as the input and output of medium, a sampler of liquid phase, a pH electrode, a pH control (acid and base), and a thermometer. The SHIS was kept at body temperature (37°C) by pumping water into the space between the jacket and the inside walls. The stomach chamber was initially filled with gas fluids and then digested for 2 hr. After the stomach digestion, the residuals was delivered from stomach chamber into the small intestine chamber by secreting intestinal fluid for 4 hr, followed by secretion of 0.3M NaHCO 3 , 0.1M NaHCO 3 , 4% bile salt, and 2% bile salt for 1, 3, 0.5, and 3.5 hrs, respectively. In order to prepare the alginate/chitosan capsule as a delivery system for bioactive agents, the microencapsulation system was assembled with a control unit, a electrical, a pneumatic systems, and a reaction vessel. After digestion of alginate capsules, the content of total sugar was 7.47% and 60.82% in the stomach and small intestine (simulated human intestinal system, SHIS), respectively. However, in case of alginate/chitosan capsule and alginate/chitosan capsule coated with polyacryl emulsion (alginate/chitosan-PAE), the total sugar content were 3.12 and 4.62% in the stomach model and 43.46 and 42.09% in the small intestine model, respectively. There were no difference on the degree of digestion in the alginate capsule and alginate/polyethylene glycol (alginate/PEG) capsule prepared with 0.1-0.3% of PEG in the stomach model. As a result, the alginate matrix remained in a shrunken state due to conversion of sodium alginate into insoluble alginic acid, which acted as a barrier to chitosan microparticles. And it was effective for digesting by intestinal fluid and releasing of the sugar.

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“…LAAs combine the physico-chemical properties of both lipids and amino acids due to their amphipathic structure; LAAs linkage to drugs, apart from enhancing their lipophilicity, can also facilitate their interaction with cell membranes and penetration across absorption and biological barriers (8). Conjugation of drug molecules to lipoamino acids (LAA) has shown to increase biological uptake and intracellular concentration of drugs (8)(9)(10). The LAAs are also used to develop lipid core peptide systems useful for delivery of genes, drugs, and vaccines (11).…”

Section: Introductionmentioning

confidence: 99%

Development of Indinavir Submicron Lipid Emulsions Loaded with Lipoamino Acids—In Vivo Pharmacokinetics and Brain-Specific Delivery

et al. 2011

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Abstract. The aim of our present work was to develop indinavir O/W submicron lipid emulsions (SLEs) loaded with lipoamino acids for specific delivery to brain. Tetradecyl aspartic acid (A) and decyl glutamic acid (G) loaded stable SLEs of indinavir having a mean size range of 210-220 nm and average zeta potential of −23.54±1.2 mV were developed using homogenization and ultrasonication. The cumulative % drug release from different SLEs varied in between 26% and 85%. The formulations, SLE, SLE-A3, and SLE-G3 were stable to the centrifugal stress, dilution stress, and storage at RT. The total drug content and entrapment efficiency were determined by HPLC method. During pharmacokinetic studies in male Wistar rats there was no significant difference in the serum levels of indinavir for SLE, SLE-A3 and SLE-G3 formulations at all time points. In tissue distribution studies, the therapeutic availability (TA) of indinavir in brain and kidneys for SLE-A3 were 4.27-and 2.66-fold whereas for SLE-G3 were 2.94 and 2.12 times, respectively, higher than that of indinavir solution. But when compared with that of SLE, in brain tissue the levels of indinavir from SLE-G3 and SLE-A3 varied in between 2.5-and 3.38-fold. While in case of the kidney, it was between 1.23-and 1.54-fold only. However, the TA is not significantly different in tissues like the heart, liver, and spleen. Thus, brainspecific delivery of indinavir was improved by including tetradecyl aspartic acid and decyl glutamic acid in submicron lipid emulsions.

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Lipid, Sugar and Liposaccharide Based Delivery Systems

Cited by 97 publications

References 33 publications

A Glycosylated Nitric Oxide Donor, β‐Gal‐NONOate, and its Site‐specific Antitumor Activity

A Glycosylated Nitric Oxide Donor, β‐Gal‐NONOate, and its Site‐specific Antitumor Activity

Digestion characteristics and kinetic analysis of bio-molecules in a simulated human intestinal system

Development of Indinavir Submicron Lipid Emulsions Loaded with Lipoamino Acids—In Vivo Pharmacokinetics and Brain-Specific Delivery

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