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UDK 615 (497.

11) YU ISSN 004-1963

Godina 60 Broj 5 Beograd, 2010.

Tematski broj

OD LEKA DO ZDRAVSTVENIH ISHODA

5/20 1 0
ARH. FARM. Godina 60 Br. 5 Strana 425- 1218 Beograd
ČASOPIS FARMACEUTSKOG DRUŠTVA SRBIJE
ARCHIVES DE PHARMACIE - ARCHIVES OF PHARMACY
IZLAZI OD 1951. GODINE

YU ISSN 004-1963 Godina 60 Broj 5 2010


Ministarstvo za nauku i tehnološki razvoj Republike Srbije je pomoglo izdavanje casopisa „Arhiv za farmaciju”

IZDAVAČ
FARMACEUTSKO DRU Š TVO SRBIJE
11000 Beograd, Bulevar vojvode Mišića 25, pošt. fah 664
tel/fax: + 381 11 2648 385; +381 11 2648 386
e-mail: fds@sbb.rs; fds@farmacija.org
www.farmacija.org

IZDAVAČKI SAVET
Milana Dučić, Sonja Kuštrin-Ðorđević, Ivanka Miletić,
Dubravka Urošev i Nenad Vulović

UREDNICE ARHIVA
Gordana Vuleta,
Univerzitet u Beogradu, Farmaceutski fakultet, Katedra za farmaceutsku tehnologiju i kozmetologiju,
Nada Kovačević,
Univerzitet u Beogradu, Farmaceutski fakultet, Katedra za farmakognoziju

LEKTOR
Mirjana Blažić

ARHIV ZA FARMACIJU izlazi šest puta godišnje.


Godišnja pretplata iznosi 3.000,00 dinara.
Pretplata za inostranstvo iznosi 70 US dolara.
Pretplata se uplaćuje na žiro račun broj: 205-14830-24 poziv na broj: 02-014406,
Farmaceutsko društvo Srbije, Beograd

Priprema za štampu: Zoran Božović (e-mail: zbozovic@gmail.com)


Štampa: štamparija DRAMIT, Barajevo, tel. +381 11 83-01-115
Tiraž: 500 primeraka
UREDNIŠTVO
Agbaba Danica,
Katedra za farmaceutsku hemiju, Farmaceutski fakultet, Univerzitet u Beogradu,
Antonijević Biljana,
Katedra za toksikologiju - akademik Danilo Soldatović, Farmaceutski fakultet,
Univerzitet u Beogradu,
Couladis Maria,
Department of Pharmacognosy & Chemistry of Natural Products, School of
Pharmacy University of Athens, Greece,
Đurović Dragan,
Agencija za lekove i medicinska sredstva Srbije, Beograd,
Harding Ljiljana,
Pfizer Global Research & Development Sandwich, Kent, UK,
Jovanović Aleksandar,
Division of Medical Sciences, Medical School, University of Dundee, UK,
Karljiković-Rajić Katarina,
Katedra za analitičku hemiju, Farmaceutski fakultet, Univerzitet u Beogradu,
Kowalska Teresa,
Institute of Chemistry, Silesian University, Katowice, Poland,
Laban-Božić Olivera,
Agencija za lekove i medicinska sredstva Srbije, Beograd,
Milenković Marina,
Katedra za mikrobiologiju i imunologiju, Farmaceutski fakultet,
Univerzitet u Beogradu,
Petruševska-Tozi Lidija,
Institute for Applied Biochemistry, Faculty of Pharmacy,
University Ss Cyril and Methodus, Skopje, R. Macedonia,
Plećaš Bosiljka,
Katedra za fiziologiju, Farmaceutski fakultet, Univerzitet u Beogradu,
Pokrajac Milena,
Katedra za farmakokinetiku, Farmaceutski fakultet, Univerzitet u Beogradu,
Primorac Marija,
Katedra za farmaceutsku tehnologiju i kozmetologiju, Farmaceutski fakultet,
Univerzitet u Beogradu,
Srčič Stanko,
Pharmaceutical Technology Department, The Faculty of Pharmacy,
University of Ljubljana, Slovenia,
Stepanović- Petrović Radica,
Katedra za farmakologiju, Farmaceutski fakultet, Univerzitet u Beogradu,
Šobajić Slađana,
Katedra za bromatologiju, Farmaceutski fakultet, Univerzitet u Beogradu,
Tamburić Slobodanka,
School of Management&Science, London College of Fashion,
University of the Arts, London, UK

CIP - Katalogizacija u publikaciji


Narodna biblioteka Srbije, Beograd
615 (497.11)
ARHIV za farmaciju : časopis Farmaceutskog društva Srbije / urednice
Gordana Vuleta, Nada Kovačević. - God. 1, BR. 1 (1951) - Beograd :
Farmaceutsko društvo Srbije, 1951. (Barajevo : Dramit). - 24 cm
Dvomesečno
ISSN 0004-1963 = Arhiv za farmaciju
COBISS.SR-ID 3115778
Arh. farm. 2010;60: 743 PP-5

FORMULATION AND EVALUATION OF SILICA


BASED XEROGEL MICROPARTICLES FOR COLON
DELIVERY OF 5-FU

Beti Djurdjic, Marija Dodov Glavas, Nikola Geskovski,


Maja Simonoska Crcarevska, Vesna Petrovska,
ppKaterina Goracinova
UKIM Faculty of Pharmacy, Macedonia
Introduction and aim:
The aim of the present study was to formulate sol-gel derived silica xerogel
microparticles (MPs) that can effectively deliver 5-FU to the colon region after peroral
administration.
Methodology:
MPs were prepared by one-step acid-catalyzed hydrolysis followed by spray-
drying of tetraethoxysilane(TEOS) based silica sol (sample 1) and TEOS co-hydrolyzed
with 2.5 mol% 3-aminopropyltriethoxysilane(APTES) (sample 2). Prepared particles
were further coated with mixture of Eudragit®RS100 and L100 (mass ratio 2:3) by the
same procedure (sample 3). The final MPs/polymer ratio was 1:5. Samples were
characterized in a terms of mean particle size and particle size distribution, surface
morphology and drug loading efficiency. Comparative in vitro drug release studies
under different pH conditions (0.1M HCl pH 1.2 and phosphate buffer pH 7.4) were
also performed.
Results and discussion:
Prepared particles were spherical with smooth surfaces and unimodal narrow
size distribution. Mean particle size was 1.41 μm (SPAN factor 1.15), 1.95 μm (SPAN
factor 1.03) and 14.63 μm (SPAN factor 1.85) for uncoated (sample1 and 2) and
Eudragit coated particles. The quantitative drug content was 46.4mg and 93.3mg 5-
FU/gMPs for TEOS-based and alkyl-substituted MPs, respectively. Partial substitution
of TEOS with APTES resulted in increased release rate of 5-FU fromMPs, probably due
to the increased hydrophilicity of the network and modified porosity of silica matrix.
Also, release profiles from uncoated MPs showed that they were unable to control drug
release in acidic pH, while the ones from Eudragit coated MPs were favorable for
efficient delivery of 5-FU to the colon.
Conclusion:
Presented study reveals the potential of alkyl-substituted silica xerogel MPs as
carriers for local colon delivery of 5-FU and efficient treatment of colon cancer.

743

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