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At least 19 recordsLinked to original sources
PubMed2006

[Recent advances in liposomes and nanoparticles as drug carriers for drug delivery].

Liposomes and nanoparticles have been used as drug carriers to increase solubility, prolong drug duration in vivo, target drug delivery, reduce toxicity and combat multi-drug resistance. With major advances in the preparation techniques, preparation material, and surface modifiers in recent years, liposomes and nanoparticles delivery systems have achieved success in fields including cancer therapy, overcoming biological barriers, and biological drugs and vaccine carriage.

Drug Carriers↗
PubMed2002

Lipid formulation as a drug carrier for drug delivery.

In recent years, a Drug Delivery System (DDS), a preparative approach attracts the attention in the development of new drugs. DDS focuses on the regulation of the in vivo dynamics, such as absorption, distribution, metabolism, and elimination, thereby improving the effectiveness and the safety of the drugs by an applicable use of drug preparation technologies. A conventional intravenous dosage form of Amphotericin B (AmB), Fungizone, is the most effective clinically available for treating fungal infections. However, the clinical efficacy of AmB is limited by its adverse effects. Several lipid formulations, such as Liposomal AmB (L-AmB), AmB lipid complex (ABLC), and AmB colloidal dispersion (ABCD), with reduced side effects have been developed. These formulations are reported to have excellent safety and efficacy. However, comparable efficacy can be achieved only when they are administered at high doses than AmB. One of the problems of using these formulations is that they are easily taken up by the reticuloendothelial system (RES). An artificial lipoprotein-like particles, a novel drug carrier Lipid Nano-Sphere (LNS), which is 25 - 50 nm in size and is composed of phospholipids and simple lipid. LNS show a higher plasma concentration of drugs and lower uptake by RES-tissue different forms other lipid base drug carriers. In vitro and in vivo, LNS incorporating AmB, NS-718, shows reduced toxicity, while maintaining activity against fungi. LNS have a unique characteristic as an effective carrier of AmB for treatment of fungal infection.

Amphotericin B↗
PubMed2004

A nanometer lipid emulsion, lipid nano-sphere (LNS), as a parenteral drug carrier for passive drug targeting.

We attempted to develop an artificial lipoprotein-like particle, lipid nano-sphere (LNS), incorporating dexamethasone palmitate (DMP). LNS is 25-50 nm in diameter and is composed of soybean oil and egg lecithin. Potential drug carriers were compared with a conventional fat emulsion for intravenous nutrition, lipid microsphere (LM, d=200-300 nm), which is already used clinically. LM easily entered reticuloendothelial systems, such as the liver, and was rapidly cleared from the circulation. However, LNS showed much higher plasma levels of DMP after intravenous administration to rats and recovered more than 80% of the injected dose in the perfusate in single-pass rat liver perfusion. The calculated volume for the distribution of the lipid emulsion within the liver showed that LNS underwent fenestration and was distributed into the Disse space in the liver. Because of the lower uptake of LNS particles by the liver, LNS showed good recovery from the liver and prolonged the plasma half-life of DMP after intravenous injection. In addition, higher efficiency in the targeting of DMP into inflammation sites and higher anti-inflammatory efficacy were observed in LNS. Thus, LNS easily and selectively passed through the leaky capillary wall by passive diffusion depending on the plasma concentration. Nanometer-sized lipid emulsion particles, LNS, seem to be a promising carrier system for passive drug targeting of lipophilic drugs.

Animals↗
PubMed2000

The physical properties of biogels and their permeability for macromolecular drugs and colloidal drug carriers.

Macromolecular drugs, either free or complexed with colloidal drug carriers, have created a great deal of interest during the last decade. If one wants to administer these new therapeutics via the oral, nasal, and cervical routes or through the conductive airways, one of the first barriers to overcome is the mucus layer that adheres to the related epithelia. In this review, the physicochemical properties of biogels, macromolecular drugs, and colloidal drug carriers that play a major role in transport through biogels are reviewed. Also, methods of studying the mobility of macromolecular drugs and colloidal drug carriers in and through biogels are addressed.

Animals↗
PubMed2006

Amphiphilogels as drug carriers: effects of drug incorporation on the gel and on the active drug.

Amphiphilogels (a subset of organogels) are being studied as drug carriers in our laboratories. In this paper, the effects of drug incorporation on the drugs and the gels are discussed. Amphiphilogels were prepared by heating a mixture of the gelator (sorbitan monostearate or sorbitan monopalmitate) and the liquid (e.g. Tweens or liquid Spans) to form a solution/dispersion, which was cooled to the gel state. Drugs were dissolved by heating a mixture of the drug and the gel and cooling the resulting solution. Hydrophilic gels (composed of hydrophilic Tweens as the liquid) were more effective solvents than hydrophobic ones (composed of hydrophobic Span 20 or 80 liquids). The latter's solvent capacity could, however, be increased by the inclusion of co-solvents, such as propylene glycol and ethanol. Drug incorporation at 10% w/w did not cause any detrimental changes in gel stability, while the drug's release rate was dependent on its concentration and on the nature of the gel's liquid component (which influences drug solubility), but not on gelator concentration or on the method of drug incorporation. This study shows the importance of the nature of the gels' liquid component and the possibility of using hydrophilic amphiphilogels as solvents for poorly water-soluble drugs.

Acetaminophen↗
PubMedDate not supplied

[Pharmaceutical applications of the zeta potential--use in characterization of colloidal drug carriers].

Colloidal drug carriers which mainly involve submicron emulsions, nanoparticles, microparticles, liposomes and lipid complexes have received increasing interest in recent years mainly as vehicles of lipophilic drugs and as improved delivery systems for drug targeting. Size and encapsulation efficiency are, in general, the two parameters used to characterize these pharmaceutical forms. Nevertheless, the surface characteristics of these dispersion have been known to influence their physical, chemical and biological properties. Then, the aim of these study is to evaluate, with some examples and illustrations, the interest of zeta potential determinations to improve the characterization of these colloidal drug carriers.

Chemical Phenomena↗
PubMed1994

Fluorinated phospholipid-based vesicles as potential drug carriers: encapsulation/sustaining of drugs and stability in human serum.

The release of entrapped 5(6)-carboxyfluorescein from fluorinated vesicles in a buffer or in human serum is considerably less than that from hydrogenated liposomes. The presence of a fluorinated core inside the liposomal membrane definitely reduces its permeability. In some cases, the stability of liposomes made from fluorinated phospholipids alone is better than that of egg phosphatidylcholine cholesterol 1/1 vesicles, which are among the least permeable and most stable hydrogenated liposomes.

Blood Physiological Phenomena↗
PubMed2000

Therapeutic applications of colloidal drug carriers.

Colloidal drug carriers such as liposomes and nanoparticles can be used to improve the therapeutic index of both established and new drugs by modifying their distribution, and thus increasing their efficacy and/or reducing their toxicity. This is because the drug distribution then follows that of the carrier, rather than depending on the physicochemical properties of the drug itself. If these delivery systems are carefully designed with respect to the target and the route of administration, they may provide one solution to some of the delivery problems posed by new classes of active molecules, such as peptides and proteins, genes and oligonucleotides. They may also offer alternative modes for more conventional drugs, such as highly hydrophobic small molecules. This review discusses the use of colloidal, particulate carrier systems (25 nm to 1 µm in diameter) in such applications.

Journal Article↗
PubMed1986

Use of lipid microspheres as a drug carrier for antitumour drugs.

9-Oxo-15-hydroxy-delta 7,10,13-prostatrienoic acid methyl ester (delta 7-PGA1), an antitumour drug was incorporated into lipid microspheres of 0.2 micron diameter (lipo-delta 7-PGA1). In in-vivo experiments, lipo-delta 7-PGA1 had a significantly greater antitumour activity than free delta 7-PGA1 against P388 leukaemia. Lipo-delta 7-PGA1 slightly, but significantly, prolonged the survival time of mice inoculated with L1210 leukaemia, whereas free delta 7-PGA1 did not. Against MM46 ascites tumour, the survival time after treatment with 10 mg kg-1 of lipo-delta 7-PGA1 was significantly greater than that after the same dose of free delta 7-PGA1. The results suggest that lipid microspheres can be used as drug delivery carriers for lipid soluble antitumour agents.

Animals↗
PubMed1989

[Liposomes--drug carriers for retinally active drugs?].

Small lipid droplets, the so-called liposomes, can serve as drug carriers and can in theory be targeted directly at diseased tissue. Thus, comparatively smaller quantities of drugs than usual are necessary. However, liposomes are recognized by the immune system and are absorbed by the reticuloendothelial system and therefore also by the Kupffer cells in the liver. These cells are storage compartments for esterified vitamin A. As about 80% of the liposomes are metabolized in the liver, retinoids form a pool for substances transported with retinoid-binding proteins. Whether retinoids reach the retina via direct liposome contact or through the endocytotic process is still not clear. In rabbits, however, retinoids applied in small unilamellar liposomes (SUV) produce photoreceptor malfunctioning (isotretinoin and etretinate) and photoreceptor outer segment damage with an increase in phagocytotic activity of the retinal pigment epithelium (etretinate).

Drug Carriers↗
PubMedDate not supplied

Fractionation and characterization of a conjugate between a polymeric drug-carrier and the antitumor drug camptothecin.

A conjugate between the antitumor drug camptothecin and the polymeric drug-carrier poly[N-(2-hydroxypropyl)methacrylamide] was synthesized and fractionated. The conjugate samples, both fractionated and unfractionated, were characterized with a multi-detector SEC system using three on-line detectors: a multi-angle light scattering photometer, a viscometer, and a refractometer. The used mobile phase (DMF + 0.01 M LiBr + 0.05 M CH(3)COOH) derives from previous experience with similar conjugates. Narrow molar mass distribution fractions of the conjugate obtained by means of a semipreparative LC system were used to derive the coefficients of the Mark-Houwink-Sakurada relationship and to check the universal calibration of the SEC system. This study has demonstrated that the conjugate elutes according to the hydrodynamic volume. Thus, a conventional SEC method that uses only an on-line refractometer detector, commercially available narrow standards, and the universal calibration is adequate for the characterization of the molar mass distribution. Also the size and the conformation of the conjugate were studied by means of the gyration radius-molar mass power law.

Antineoplastic Agents↗
PubMed2005

Role of polyanhydrides as localized drug carriers.

Many drugs that are administered in an unmodified form by conventional systemic routes fail to reach target organs in an effective concentration, or are not effective over a length of time due to a facile metabolism. Various types of targeting delivery systems and devices have been tried over a long period of time to overcome these problems. Targeted delivery or localized drug delivery offers an advantage of reduced body burden and systemic toxicity of the drugs, especially useful for highly toxic drugs like anticancer agents. Local drug delivery via polymer is a simple approach and hypothesized to avoid the above stated problems. Polyanhydrides are a unique class of polymer for drug delivery because some of them demonstrate a near zero order drug release and relatively rapid biodegradation in vivo. Further, the release rate of polyanhydride fabricated device can be altered over a thousand fold by simple changes in the polymer backbone. Hence, these are one of the best-suited polymers for drug delivery, with biodegradability and biocompatibility. The review focuses on the advantages of polyanhydride carriers in localized drug delivery along with their degradability behavior, toxicological profile and role in various disease conditions.

Antineoplastic Agents↗
PubMed2004

Drug delivery to the brain--realization by novel drug carriers.

Delivery of drugs to the brain is still a major challenge. Successful delivery across the bloodbrain barrier has only been achieved in some cases, e.g., using pro-drugs. The review describes the delivery to the brain using nanoparticulate drug carriers in combination with the novel targeting principle of "differential protein adsorption" (PathFinder technology). The PathFinder technology exploits proteins in the blood which adsorb onto the surface of intravenously injected carriers for targeting. Apolipoprotein E is the targeting moiety for the delivery of particles to the endothelials of the blood-brain barrier. To reach therapeutic drug level in the brain, nanoparticulate drug carriers with sufficiently high loading capacity are reviewed, including drug nanocrystals (nanosuspensions), lipid drug conjugate (LDC) nanoparticles and lipid nanoparticles (solid lipid nanoparticles-SLN, nanostructured lipid carriers-NLC). The features are described, including regulatory aspects and large scale production.

Animals↗
PubMed2006

Evaluation of polyamidoamine (PAMAM) dendrimers as drug carriers of anti-bacterial drugs using sulfamethoxazole (SMZ) as a model drug.

Sulfamethoxazole (SMZ), a sulfonamide with well-known anti-bacterial properties, is not freely soluble in water and causes problems in its clinical applications. In the present study we investigated the potential of ethylenediamine (EDA) core polyamidoamine (PAMAM) dendrimers as drug carriers of SMZ by aqueous solubility, in vitro release as well as anti-bacterial activity studies. Results showed that the aqueous solubility of SMZ was approximately proportional to dendrimer concentration (a 40-fold increase in solubility in 10mg/ml G3 PAMAM dendrimer solutions compared with that in double-distilled water at 37 degrees C). The in vitro release of SMZ in the presence of PAMAM dendrimers was significantly slower compared to pure SMZ dissolved in ethanol. Microbiology studies showed that PAMAM dendrimers could increase the anti-bacterial activity of SMZ (a 4- or 8-fold increase in the anti-bacterial activity of SMZ in dendrimer solution compared to pure SMZ dissolved in dimethylsulfoxide (DMSO) or 0.01 M NaOH solution). The in vitro release behavior and anti-bacterial activity studies indicated that PAMAM dendrimers might be considered as potential drug carriers of sulfonamides with a sustained release behavior under suitable conditions.

Anti-Bacterial Agents↗
PubMed2006

Targeting cancer cells: magnetic nanoparticles as drug carriers.

Magnetic drug targeting employing nanoparticles as carriers is a promising cancer treatment avoiding side effects of conventional chemotherapy. We used iron oxide nanoparticles covered by starch derivatives with phosphate groups which bound mitoxantrone as chemotherapeutikum. In this letter we show that a strong magnetic field gradient at the tumour location accumulates the nanoparticles. Electron microscope investigations show that the ferrofluids can be enriched in tumour tissue and tumour cells.

Animals↗
PubMed2004

Synthesis and characterization of branched poly(L-glutamic acid) as a biodegradable drug carrier.

Polymeric drug delivery systems are used not only to improve aqueous solubility of drug molecules but also to achieve desirable pharmacokinetics and an enhanced therapeutic index. New biodegradable polymers are needed to improve the biodistribution and targeting-ability of polymeric carriers. In this study, the synthesis and characterization of branched poly(L-glutamic acid) (PG) containing multiple PG chains centered on a poly(amidoamine) (PAMAM) dendrimer or polyethyleneimine (PEI) cores were described. The branched PG polymers were obtained by ring-opening polymerization of benzyl ester of L-glutamic acid N-carboxyanhydride using PAMAM or PEI as the initiator. These polymers were degradable in the presence of the lysosomal enzyme cathepsin B, albeit more slowly than linear PG. Unlike conventional linear PG, each branched PG possessed multiple terminal amino groups. This made it possible to attach multiple targeting moieties selectively to the termini of branched PG. Conjugation of monofunctional or heterodifunctional polyethylene glycol to the chain ends of branched PG was demonstrated in the presence of side chain carboxyl groups. Furthermore, folic acid, a model targeting moiety, and the near-infrared dye indocyanine green, a model diagnostic agent, were successfully conjugated to the terminal amino groups and the side chain carboxyl groups of branched PG, respectively. The resulting conjugate had reduced nonspecific interaction and bound selectively to tumor cells expressing folate receptors. Thus, branched PG may be useful as a polymeric carrier for targeted drug delivery.

Cell Line, Tumor↗