Priprava i karakterizacija nanokristala flutikazonpropionata

master's thesis

• Title (english): Preparation and characterization of fluticasone propionate nanocrystals
• Author: Ana Bano
• Mentor: Ivan Pepić (mentor)
• Committee member: Ivan Pepić (predsjednik povjerenstva)
• Committee member: Anita Hafner (član povjerenstva)
• Committee member: Dubravka Vitali Čepo (član povjerenstva)
• Granter: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of pharmaceutical technology); Zagreb
• Defense date and country: 2019-07-02, Croatia
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract

Veliki broj novosintetiziranih djelatnih tvari teško je topljivo. Jedna od metoda postizanja bolje solubilizacije je
priprava nanokristala, odnosno smanjenje veličine čestica djelatnih tvari na nanometarsku veličinu. Veličina
nanokristala je u rasponu od od 1 do 1000 nm. Povećanjem topljivosti djelatne tvari, povećava se i njezina
bioraspoloživost. Nanosuspenzije su termodinamički nestabilni sustavi. Zbog toga, osim djelatne tvari i tekuće faze,
sustav mora sadržavati stabilizator. Za pripravu nanokristala koriste se dvije skupine metoda; metode smanjenja
veličine čestica (engl. top-down methods) i metode povećanja veličine čestica (engl. bottom-up methods). Metoda
vlažnog mljevenja pripada skupini top-down metoda. Nanokristali djelatne tvari mogu se koristiti za nazalnu primjenu
lijekova. Time je moguće postići lokalni, ali i sistemski učinak. Najčešće se nazalna primjena koristi u liječenju
lokalnih infekcija, alergijskog rinitisa ili nazalne kongestije, ali moguć je i učinak na središnji živčani sustav.
Cilj ovog rada bio je pripraviti nanokristale flutikazonpropionata u suspenziji s Tween 80 kao površinski aktivnom
tvari.
Postupkom vlažnog mljevenja izrađeni su nanokristali flutikazonpropionata raspona veličina od 209,74 do 394,42 nm.
Udio Tween 80, odnosno omjer djelatna tvar/Tween 80 te masa kuglica za mljevenje utjecala je na veličinu čestica.
Suspenzije 10:1, 5:1, 4:1 i 1:1 pokazale su zadovoljavajuće rezultate. Najmanja veličina čestica dobivena je u
suspenziji u slučaju omjera djelatna tvar : Tween 80 2:1. Najveća masa od 0,75 g nije imala utjecaj na smanjenje
veličine čestica u odnosu na rezultate dobivene mljevenjem s kuglicama mase 0,5 g. Variranje mase kuglica različitih
veličina također nije imala značajnijeg utjecaja na veličinu nanočestica.

Abstract (english)

A large number of newly synthesized active substances are severely soluble. One of the methods for achieving better
solubilization is the preparation of nanocrystals and the reduction of active substance particles on a nanometric scale.
The size of nanocrystals ranges from 1 to 1000 nm. By increasing the solubility of active substances, their
bioavailability increases. Nanosuspensions are thermodynamically unstable systems. Therefore, in addition to the
active substance and the liquid phase, there also must be a stabilizer in the system. There are two groups of methods
used for preparation of nanocrystals . Those are methods based on particle size reduction (top-down methods) and
methods based on increasing the particle size (bottom-up methods). The method of wet milling is one of top-down
methods. Nanocrystals can be used for nasal administration of drugs. Nasal administration can achieve local but also a
systemic effects. The most common nasal use is for the treatment of local infections, allergic rhinitis and nasal
congestion, or possible effects on the central nervous system.
The aim of this study was to prepare nanocrystals of fluticasone propionate in suspension with Tween 80 as a
surfactant.
By the wet milling method, nanocrystals were obtained from 209.74 nm to 394.42 nm. Concentration of Tween 80,
respectively, the ratio of the active substance/Tween 80 and the mass of milling beads affected the particle size.
Suspensions 10:1, 5:1, 4:1 and 1:1 showed satisfactory results. The minimum particle size was obtained by suspending
the active ingredient : Tween 80 2:1. The maximum weight of 0.75 g milling beads had no impact on the particle size
reduction compared to results given for milling by 0.5 g milling beads. There was no significant influence on the size
of nanocrystals by varying weights of milling beads different sizes.

• Keywords: nanočestice; flutikazonpropionat; tween 80; vlažno mljevenje; nazalna primjena
• Keywords (english): nanoparticles; fluticasone propionate; tween 80; wet milling; nasal administration
• Language: croatian
• URN:NBN: urn:nbn:hr:163:842697
• Study programme: Title: Pharmacy; Study programme type: university; Study level: integrated undergraduate and graduate; Academic / professional title: magistar/magistra farmacije (magistar/magistra farmacije)
• Type of resource: Text
• File origin: Born digital
• Access conditions: Open access
• Created on: 2020-02-28 12:42:51