SVIBOR - Papers quoted in CC - project code: 3-04-321
MINISTRY OF SCIENCE AND TECHNOLOGY
Strossmayerov trg 4, HR - 10000 ZAGREB
tel.: +385 1 459 44 44, fax: +385 1 459 44 69
E-mail: ured@znanost.hr
SVIBOR - Collecting Data on Projects in Croatia
Papers quoted in Current Contents on project 3-04-321
Quoted papers: 36
Other papers: 50
Total: 86
Title: Macromolecular prodrugs. III. Esters of Fenoprofen and
Probenecid
- Authors:
- Butula, Ivan (6372)
- Zorc, Branka
Journal: Acta Pharm.
Number: 1
ISSN: 1330-0075
Volume: 44
Year: 1994
Pages: from 103 to 108
Number of references: 13
Language: engleski
Summary: Fenkoprofen and probenecid were covalently linked by ester
bonds to ŕ,á-poly(N-hydroxyethul)-DL-aspartamide (PHEA), hydrophilic
polymer, previously proposed as a drug carrier and plasma expander. In
addition, two simple esters of fenoprofen and probenecid were prepared.
Ester bondings were achieved via benzotriazolides synthesized by the
reaction of 1-benzotriazole carboxylic acid chloride with fenoprofen and
probenecid, respectively. Release of the drug from PHEA-drug esters in
alkaline medium was studied.
Keywords: prodrug, macromolecular carrier, ŕ,á-poly(N-hydroxyethyl)-DL-aspartamide, fenoprofen ester, probenecid ester, 1-benzotriazole carboxylic acid chloride
Title: Macromolecular prodrugs V. Polymer-broxuridine conjugates
- Authors:
- Zorc, Branka
- Maysinger, Dušica
- Kalčić, Igor
- Butula, Ivan (6372)
Journal: Int.J.Pharmac.
ISSN: 0378-5173
Volume: 123
Year: 1995
Pages: from 65 to 70
Number of references: 15
Language: engleski
Summary: Broxuridine was covalently bound to PHEA and PAHA.
Broxuridine was first chemically modified and bound to PHEA by carbonate
and phosphodiester linkages, and to PAHA by an amide type bond.
Neuroepithelia cells were used as a model system to assess the suitability
of the conjugated broxuridine for cell proliferation. Parallel experiments
were perormed with unconjugated broxuridine and the extent of incorporation
into DNA was determined by immunocytochemistry using an broxuridine
antibody.
Keywords: polymeric prodrug, polymer-drug conjugate, broxuridine, cell proliferation, immunocytochemistry
Title: Controlled release formulations of potassium chloride
produced by fluidized bed film coating and spray-drying technique
- Authors:
- Bećirević, Mira (2761)
- Begić, Veronika
Journal: Pharmazie
Number: H5
ISSN: 0031-7144
Volume: 49
Year: 1994
Pages: from 339 to 342
Number of references: 10
Language: engleski
Summary: Fluidized bed film coating and a spray-drying technique
provided by Eudragit RS were used for prolonging potassium chloride
release. The effect of the polymers on the dissolution data of the prepared
formulations was investigated. In an attempt to obtain more information on
the release kinetics, dissolution data kof coated drug crystals, their
tablets and spray-dried products were examined from the viewpoint of
first-order kinetics, the Higuchi square root law and the modified
Hixson-Crowell model. The drug release was characterized by a rapid release
phase followed by a slow release phase. The dissolution data showed that
the release of potassium chloride from the formulations proceeded in
sustained patterns at a moderate rate.
Keywords: potassium chloride, controlled release, fluidized bed film coating, spray-drying technique
Title: Inclusion complexation of indomethacin with cyclodextrins
in solid state
- Authors:
- Bećirević, Mira (2761)
Journal: S.T.P. Pharma Sciences
Number: 4
ISSN: 1157-1489
Volume: 4
Year: 1994
Pages: from 282 to 286
Number of references: 14
Language: engleski
Summary: Complex formation of lindomethacin with ŕ-, á- and
g-cyclodextrins and dimethyl á-cyclodextrin (DIMEB) were studied by the
solubility and UV-spectrophotometric methods. By comparing the apparent
stability constants evaluated by the two methods, it was possible to
characterize the stability of the inclusion complexes and to establish, in
part, their stoichiometries. The solid complexes of indomethacin with
cyclodextrins in molar rations of 1/1 were prepared by employing the
freeye-drying technique. The influence of cyclodextrins on diffusion throuh
a semi-permeable membrane were evaluataed according to the first-order
kinetics of diffusion from the solutions containing indomethacin alone or
in the complex form. The apparent dialytic rate constants of the complexes
were lower than that of the free indomethacin.
Keywords: Indomethacin inclusion complexes, cyclodextrins, stability constants, apparent dialztic rate constants
Title: The properties of some ambiphilic vehicles
- Authors:
- Čajkovac, Mira (7606)
- Milojica, Draga
Journal: Acta Pharm.
Number: 2
ISSN: 1330-0075
Volume: 45
Year: 1995
Pages: from 131 to 138
Number of references: 9
Language: engleski
Summary: The properties of self-prepared ambiphilic vehicles and of
a similar commercial product have been investigated. It was established
that thez are either O/W systems or belong to a mixed type. According to
their appearance and rheological properties they can be defined as creams
or emulsoids. Self-prepared vehicles can bind a maximum of 64.5 to 105.5%
(m/m) of liquid paraffin whereas a commercial sample is only able to bind
51% (m/m). The addition of a maximal amount of oil creates preparation of
W/O type which are very sensitive to mechanical stress. Therefore, their
rheological properties cannot be determined. Samples with 45% (m/m) of
liquid paraffin or almond oil are emulsoids too, but not all of them belong
to the W/O tzpe. A comparison with "basic" vehicles showts that they are
characterized by lower viscosities and values for theoretical yield shear.
On the contrary, the hydrophilicity of all samples was much higher because
they accept 565 to 756% (m/m) of water (the commeracial sample 810%). The
addition of 300% (m/m) and more of water changes the structure of the
initial "basic" vehicles, so that mobile O/W type emulsions develop from
the lamellar gel structure which is characteristic for ambiphilic systems.
These (highly) diluted emulsions possess pseudoplastic properties and low
values for apparent viscosity and theoretical yield shear.
Keywords: ambiphilic vehicles, ambiphilicity, structural properties, apparent viscosity
Title: QSPR and QSAR study of phthalimidohydroxamic acids
- Authors:
- Nikolić, Sonja
- Medić-Šarić, Marica (74265)
- Matijević-Sosa, Julija (71850)
Journal: Acta Pharm.
Number: 1
ISSN: 1330-0075
Volume: 45
Year: 1995
Pages: from 15 to 24
Number of references: 9
Language: engleski
Summary: Newly prepared phthalimidkohydroxamic acids are tested for
their mitodepressive effect on the growth of Lepidium sativum L. seeds
(Cresson). Their partition coefficients, log P (o/w), are calculated by
Rekker method. In the structure-property-activity study we have used
topological indices to predict the physico-chemical properties and
bioactivity of the prepared compounds. The optimal QSPR and QSAR models are
obtained by using the valence connectivity index and the
information-theoretic index.
Keywords: QSPR, QSAR, phthalimidohydroxamic acids
Title: 1-(3-Benzoylphenyl)ethanone (I) and
3-Benzoyl-ŕ-methylbenzeneacetamide Methylene Chloride Solvate (2/1) (II)
- Authors:
- Matak, Dijana
- Vinković, Mladen
- Dumić, Miljenko (133202)
Journal: Acta Crystallogr. Sect. C
Volume: 50
Year: 1994
Pages: from 1339 to 1342
Number of references: 8
Language: engleski
Summary: 1-(3-Benzoylpherojektuspace group P21/c, with a 10.681 (1),
b 10.509 (1), c 11.157 (1) A, and á 107.38 (2); Z = 4, dc = 1.22; R =
0.070, Rw = 0.099 for 1227 reflections. 3-Benzoyl-ŕ-methylbenzeneacetamide
methylene chloride solvate (2/1) (II), is monoclinic, space group C2/c,
with a 23.902 (10), b 8.064 (2), c 15.669 (3) A, and á 93.11 (2); Z = 8, dc
= 1.30; R = 0.0826, Rw = 0.1210 for 1947 reflections. At. coordinates are
given. While the acetyl group in I is nearly coplanar with the Ph ring
(O2-C14-C1-C2 6.8 (5) and positioned opposite the C7 = O1 group, the
2-propanamido group in II is almost perpendicular to the corresponding Ph
ring (C16-C14-C1-C2 134.0 (4), C15-C14-C1-C2 - 102.4 (5) and occupies the
same side as the C7=O1 group.
Keywords: 1-(3-Benzoylphenyl)ethanone, 3-Benzoyl-ŕ-methylbenzeneacetamide methylene chloride solvate (2/1), X-ray diffraction
Title: Preparation, characterization and release of
microencapsulated bromodeoxyuridine
- Authors:
- Maysinger, Dušica
- Filipović-Grčić, Jelena (136683)
- Alebić-Kolbah, Tanja
Journal: Life Sciences
ISSN: 0024-3205
Volume: 54
Year: 1994
Pages: from 27 to 34
Number of references: 16
Language: engleski
Summary: Biodegradable and biocompatible microspheres with
bromodeoxyuridine (BrUrd) have been prepared, characterized and tested in
vitro and in vivo. Scaning electron microscopy and image analysis revealed
regular spherical shapes and an average size of 2.47 Šm. Total content of
BrUrd as determined by HPLC was within the range of 0.2 - 1.5 %.
Preliminary data from immunocytochemical studies revealed efficient
incorporation of BrUrd delivered from these microcapsules into nuclei of
proliferating cells surrounding brain lesions in rats.
Keywords: microspheres, bromodeoxyuridine, immunocytochemistry, proliferating cells
Title: Alginate microspheres of microbial spores and viable cells
of Bacillus subtilis
- Authors:
- Pepeljnjak, Stjepan
- Filipović-Grčić, Jelena (136683)
- Jalšenjak, Vesna (52171)
Journal: Pharmazie
Number: H.6
ISSN: 0031-7144
Volume: 49
Year: 1994
Pages: from 436 to 437
Number of references: 6
Language: engleski
Summary: Microspheres of Bacillus subtilis (microbial spores and
viable cells) were prepared by using sodium alginate. Some typical
properties of microencapsulated systems such as content of microorganisms,
particle size and germination time were studied. Very mild conditions
during the preparation step enables one to produce microspheres containing
cells with no apparent changes in their general biological properties, but
gives them protection with a soft hydrogel matrix in the same time does not
prevent completely the communication with the surrounding medium.
Keywords: microspheres, Bacillus subtilis, sodium alginate, hydrogel matrix
Title: Microparticles with neuroactive agents
- Authors:
- Filipović-Grčić, Jelena (136683)
- Maysinger, Dušica
- Jalšenjak, Ivan
Journal: J. Microencapsulation
Number: 4
ISSN: 0265-2048
Volume: 12
Year: 1995
Pages: from 343 to 362
Number of references: 65
Language: engleski
Summary: An overview of biodegradable and biocompatible
microcapsules and microspheres loaded with neuroactive substances, or cells
producing neuroactive substances, and their role as drug delivery systems
(DDS) for drug administration to the central nervous system (CNS) is given.
In addition, closely related systems are also summarized.
Keywords: microcapsule, microsphere, biodegradable, biocompatible, neuroactive
Title: Macromolecular prodrugs. IV. Alginate-chitosan
microspheres of PHEA-L-dopa adduct
- Authors:
- Filipović-Grčić, Jelena (136683)
- Maysinger, Dušica
- Zorc, Branka
- Jalšenjak, Ivan
Journal: Int.J.Pharmac.
ISSN: 0378-5173
Volume: 116
Year: 1995
Pages: from 39 to 44
Number of references: 11
Language: engleski
Summary: A polymeric prodrug ŕ,á-poly(N-hydroxyethyl-DL-
aspartamide-L-dopa adduct (PHEA-L-dopa) was microencapsulated in
alginate-chitosan microspheres in order to achieve drug release from a
complex reservoir device. The gel/matrix material of alginate-chitosan
complex protects the adduct from hydrolysis by the surrounding medium. On
the basic of a 10000-fold difference between the drug released from
microspheres as the adduct and that released in the unbound form, a model
of the microencapsulated system was proposed.
Keywords: PHEA-L-dopa adduct, alginate, chitosan, microsphere, prodrug
Title: Encapsulated genetically engineered fibrobasts: release of
nerve growth factor and effects in vivo on recovery of cholinergic markers
after devascularizing cortical lesions
- Authors:
- Maysinger, Dušica
- Piccardo, P.
- Liberini, Paolo
- Jalšenjak, Ivan
- Cuello, Claudio
Journal: Neurochem.Int.
Number: 5
ISSN: 0197-0186
Volume: 24
Year: 1994
Pages: from 495 to 503
Number of references: 38
Language: engleski
Summary: Genetically engineered rat fibroblasts producing nerve
growth factor (NGF) were encapsuled in alginate-polylysine-alginate gels
with the objective to produce viable "minifactories" continuously producing
and secreting NGF into the rat brain. Microencapsulated fibroblasts (NGF)
secretors and NGF non-secretors) were placed onto the surface of the
lesioned rat cortex (unilateral devascularizing lesion) and animals were
sacrificed 30 days after surgery. Fibroblasts NGF-non sescreters normally
produce tumors after implantation, therefore, they were irradiated prior to
encapsulation. Three other experimental groups were studied in parallel:
non-lesioned (controls), lesioned rats receiving "empty" alginate spheres
and lesioned animals without treatment and microspheres. Biochemical
analysis of microdissected brain tissues of lesioned animals treated with
encapsulated NGF-secretor fibroblasts showed a significant increase in
choline acetyltransferase (ChAT) activity in cortices adjacent to the
lesion but not far from it (entorhinal cortex). Morphometric analysis of
ChAT-IR and low affinity NGF-receptor IR cholinergic neurons in the middle
ortion of the NBM shows a prevention of neuronal shrinkage and extensive
neuropil in animals treated with microencapsulated NGF-secretor
fibroblasts. The results of this study demonstrate that NGF from
encapsulated genetically engineered fibroblasts can be secreted for at
least long enough to prevent degenerative changes of cholinergic neurons in
the NBM.
Keywords: microcapsule, nerve growth factor, alginate-polylysine gels, genetically engineered cells, fibroblasts
Title: A Non-Ionic Surfactant Vesicle-in-Water-in-Oil (v/w/o)
System: Potential Uses in Drug and Vaccine Delivery
- Authors:
- Yoshioka, Toshimitsu
- Škalko, Nataša (34134)
- Gursel, Mayda
- Gregoriadis, Gregory
- Florence, Alexander T.
Journal: J. of Drug Targeting
Volume: 2
Year: 1995
Pages: from 533 to 539
Number of references: 16
Language: engleski
Summary: An aqueous dispersion of niosomes (non-ionic surfactant
vesicles) emulsified in an external oil phase forms the
vesicle-in-water-in-oil (v/w/o) system described in this paper. The
properties of the surfactant used to form the vesicles, the surfactant or
surfactant mixture used to stabilize the emulsion and the nature of the oil
phase can be changed to provide systems of different capacities for drug or
antigen and different release characteristics. The same nonionic surfactant
is used as the principle amphipile to form the niosomes and to stabilize
the w/o emulsion, thus promoting stability by decreasing transfer of
surfactant between the stabilizing monolayers and the vesicle bilayers. The
in vitro release of carboxyfluoroscein and 5-fluorouracil encapsulated
within the niosomes of the v/w/o system has been investigated, the nature
of the oil phase and surfactant-oil interactions being important in
determining the rate of solute release. Initial studies of the system in
vivo, as an adjuvant for tetanus toxoid, using cottonseed oil as the
external oil phase, showed enhanced immunological ativity over the free
antigen or vesicles.
Title: Antibodies against phosphatidylinositol and inositol
monophosphate specifically inhibit tumour necrosis factor induction by
malaria exoantigens
- Authors:
- Bate, Clive
- Taverne, Janice
- Bootsma, Harry
- Mason, Richard
- Škalko, Nataša (34134)
- Gregoriadis, Gregory
- Playfair, John
Journal: Immunology
Volume: 76
Year: 1992
Pages: from 35 to 41
Language: engleski
Summary: The active component of the exoantigens of malarial
parasites which stimulates macrophages to secrete tumour necrosis factor
(TNF) has been shown to depend upon a phospholipid, the activity of which
was blocked by phosphadidylinositol (PI) and inositol monophosphatae (IMP)
in competitive inhibition studies. Antisera made against the exoantigens of
Plasmodium yoelli, which inhibited their induction of TNF, were found by an
ELISA assay to contai antibody against several other phospholipids. When
incorporated into liposomes several other phospholipids did give rise to
inhibitory antibodies but, in contrast to the antisera against parasite
exoantigens, PI and IMP, the inhibitory activity was removed by adsorption
with heterologous phospholipid liposomes, suggesting that it was directed
against a common determinant, presumably the phosphate ester head group.
Inhibitory antibodies in the antisera tested wer predominantly IgM and
titres were not increased after repeated injections. Antisera raised
against Pi, IMP or the crossreacting phospholipid liposomes also inhibited
TNF secretion by macrophages stimulated by exoantigens of the human
parasites P. falciparum and P. vivax, but not by bacterial
lipopolysaccharide. These findings confirm our conclusion that exoantigens
from these different species contain phosphate bound to inositol in their
TNF-inducing moiety.
Keywords: antibody, liposomes, malaria exoantigens
Information: svibor@znanost.hr