Polymeric Drugs

Minko, Tamara; Khandare, Jayant; Jayant, Sreeja

doi:10.1002/9783527631421.ch61

Cited by 9 publications

(2 citation statements)

References 142 publications

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“…A prodrug is an inactive precursor of a drug which is converted into the active drug in the targeted organ, tissue, or cell. – Advantages of the prodrug approach include, but are not limited to, the prevention of systemic side effects, the increase in the bioavailability of the modified drug, and the possibility of using specific organ, tissue, or cellular conditions to convert the inactive prodrug into its active form. In most cases, a prodrug includes a drug bound to (or encapsulated in) a water-soluble carrier.…”

Section: Introductionmentioning

confidence: 99%

Targeted Proapoptotic Anticancer Drug Delivery System

et al. 2007

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A novel targeted proapoptotic anticancer drug delivery system (DDS) was developed and evaluated both in vitro and in vivo. The system contains poly(ethylene glycol) polymer (PEG) as a carrier, camptothecin (CPT) as an anticancer drug/cell death inducer, a synthetic analogue of luteinizing hormone-releasing hormone (LHRH) peptide as a targeting moiety/penetration enhancer, and a synthetic analogue of BCL2 homology 3 domain (BH3) peptide as a suppressor of cellular antiapoptotic defense. The design of the multicomponent DDS allowed for a conjugation of one or two copies of each active ingredient (CPT, LHRH, and BH3) to one molecule of PEG carrier. The complex structure of the PEG conjugates was visualized at nanometer resolution using atomic force microscopy. We found that the ligand-targeted DDS for cancer cells preferentially accumulated in the tumor and allowed the delivery of active ingredients into the cellular cytoplasm and nuclei of cancer cells. Simultaneous apoptosis induction through the caspase-dependent signaling pathway and inhibition of cellular antiapoptotic defense by the suppression of BCL2 protein enhanced cytotoxicity and antitumor activity of the entire DDS to a level which could not be achieved by individual components applied separately. The DDS containing two copies of each active component (CPT, LHRH, and BH3) per molecule of PEG polymer had the highest anticancer efficiency in vitro and in vivo.

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Section: Introductionmentioning

confidence: 99%

Targeted Proapoptotic Anticancer Drug Delivery System

et al. 2007

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“…Numerous review articles – have appeared in the past years, describing in great detail the outstanding role of pullulan and dextran in the fields of biology, medicine, cosmetics, and technology, particularly in the food industry. The three most recent publications using the new approach deal with system water/cellulose (exhibiting a large miscibility gap between the components), with the question of how the system specific parameters of this concept are composed of enthalpy and entropy contributions and apply the concept to random copolymers …”

Section: Introductionmentioning

confidence: 99%

Pullulan and Dextran: Uncommon Composition Dependent Flory–Huggins Interaction Parameters of their Aqueous Solutions

2008

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Vapor pressure measurements were performed for aqueous solutions of pullulan ( M w 280 kg/mol) and dextran ( M w 60 and 2100 kg/mol, respectively) at 25, 37.5, and 50 degrees C. The Flory-Huggins interaction parameters obtained from these measurements, plus information on dilute solutions taken from the literature, show that water is a better solvent for pullulan than for dextran. Furthermore, they evince uncommon composition dependencies, including the concurrent appearance of two extrema, a minimum at moderate polymer concentration and a maximum at high polymer concentration. To model these findings, a previously established approach, subdividing the mixing process into two clearly separable steps, was generalized to account for specific interactions between water and polysaccharide segments. Three adjustable parameters suffice to describe the results quantitatively; according to their numerical values, the reasons for the solubility of polysaccharides in water, as compared with that of synthetic polymers in organic solvents, differ in a principal manner. In the former case, the main driving force comes from the first step (contact formation between the components), whereas it is the second step (conformational relaxation) that is advantageous in the latter case.

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