Vrednotenje stabilnosti resveratrola v bukalnih filmih : Magistrski študijski program Industrijska farmacija

Planinšek Parfant, Timeja (avtor), Zega, Anamarija (mentor), Roškar, Robert (komentor)

V zadnjih letih se je na znanstvenem področju zelo povečalo zanimanje za proučevanje vpliva resveratrola na zdravje ljudi, saj študije kaţejo, da le-ta izkazuje številne terapevtske učinke. Zaradi slabe vodotopnosti in obseţnega metabolizma I. prehoda ima resveratrol nizko biološko uporabnost po peroralni uporabi. Bukalni filmi so eden izmed obetavnih pristopov za izboljšanje biološke uporabnosti, saj se z njihovo uporabo učinkovine izognejo metabolizmu I. prehoda in drugim neugodnim pogojem v gastrointestinalnem traktu. V magistrski nalogi smo z različnimi analiznimi metodami (HPLC, IR spektroskopija, LC/MS-MS, NMR, optični mikroskop in SEM) preučevali in vrednotili stabilnost resveratrola v bukalnih filmih, ki se uporabljajo kot prehransko dopolnilo. Pri 3-mesečni stabilnostni študiji pri 25 °C in 60 % relativni vlaţnosti ter 40 °C in 75 % relativni vlaţnosti ter pri fotostabilnostni študiji, kjer smo UV svetlobi izpostavili praškasti standard trans-resveratrola in bukalne filme, ki vsebujejo trans-resveratrol, smo s HPLC, IR in 1H NMR analizami ugotovili, da je trans-resveratrol stabilen v obeh primerih. Cis-resveratrol smo zaznali in identificirali le z LC/MS-MS analizo, kjer je bila njegova vsebnost v primerjavi s trans-resveratrolom zelo nizka (<1%). S HPLC analizo smo ugotovili, da se je vsebnost trans-resveratrola v metanolni raztopini po 5-dnevni izpostavljenosti UV svetlobi zmanjšala na 10 % in z LC/MS-MS analizo dokazali, da pri tem pride tudi do izomerizacije v cis-resveratrol. Da bi čim bolj posnemali realne pogoje, katerim so lahko bukalni filmi izpostavljeni pri uporabi, smo izvedli še 1-mesečno stabilnostno študijo, kjer smo filme izpostavili sončni svetlobi ter sobnim pogojem. Ugotovili smo, da shranjevanje bukalnih filmov na sončni svetlobi ni priporočljivo, saj se v njih zmanjša vsebnost trans-resveratrola. Z vrednotenjem stabilnosti resveratrola smo ugotovili, da je shranjevanje bukalnih filmov v primarni ovojnini zelo pomembno, saj jih ščiti pred zunanjimi dejavniki. Ključna zunanja dejavnika, ki lahko vplivata na stabilnost resveratrola v bukalnih filmih, sta vlaţnost zraka in UV svetloba, saj vplivata na fizikalno stabilnost filmov; bukalni filmi zaradi niţje ali višje vlaţnosti postanejo trši oziroma mehkejši, zaradi UV svetlobe pa se njihova barva spremeni v oranţno-rjavo ter povzroči razpoke na površini. Bukalni filmi so primerna farmacevtska oblika za vgrajevanje trans-resveratrola, saj je ta, v primeru da so filmi shranjeni v primarni ovojnini, stabilen pri različnih pogojih shranjevanja.

• Jezik: Slovenski jezik
• Ključne besede: tekočinska kromatografija visoke ločljivosti, resveratrol, bukalni filmi, fotostabilnost
• Vrsta gradiva: Magistrsko delo/naloga
• Tipologija: 2.09 - Magistrsko delo
• Organizacija: FFA - Fakulteta za farmacijo
• Kraj izida: Ljubljana
• Založnik: [T. Planinšek Parfant ]
• Leto izida: 2018
• Št. strani: IX, 7 f.
• PID: 20.500.12556/RUL-129030
• UDK: 543.544.5:615.011.015(043.3)
• COBISS.SI-ID: 4612209
• Datum objave v RUL: 24.08.2021

Sekundarni jezik

• Jezik: Angleški jezik
• Naslov: Evaluation of resveratrol stability in buccal films : Master's Study Programme Industrial Pharmacy

Izvleček

In recent years, interest in studying the beneficial properties of resveratrol on human health has greatly increased because it exhibits a number of therapeutic effects. Due to poor water solubility and extensive first-pass metabolism, resveratrol has low bioavailability after oral administration. Buccal films are one of the approaches to improve the bioavailability, since the active ingredient bypasses the first-pass metabolism and variable environment in the gastrointestinal tract. In the master thesis, the stability of resveratrol in buccal films used as a dietary supplement was studied, which was evaluated by several analytical methods (HPLC, IR spectroscopy, LC/MS-MS, NMR, optical microscope and SEM). In a 3-month stability study (25 °C / 60 % relative humidity and 40 °C / 75 % relative humidity) and photostability study where the powder standard of trans-resveratrol and buccal films with incorporated trans-resveratrol were exposed to UV light, with HPLC, IR and 1H NMR analytical methods it was found that trans-resveratrol is stable in both cases. Cis-resveratrol was detected and identified only with LC/MS-MS analysis, where the content was very low compared to trans-resveratrol (<1%). In HPLC analysis it was found that the content of trans-resveratrol in the methanol solution after 5 days of exposure to UV light is reduced to 10%, and in LC/MS-MS analysis it was found that isomerization to cis-resveratrol also occurs. Since we also wanted to simulate the real conditions as much as possible, we carried out a 1-month stability study, where buccal films were exposed to the sunlight and room conditions. In this study, we found that the storage of buccal films on the sunlight is not recommended, as the content of trans-resveratrol in films is reduced. By evaluating the stability of resveratrol in buccal films, we also found that the storage of films in the primary packaging is very important since it protects them from environmental factors. Humidity and UV light are two critical environmental factors that can affect the stability of resveratrol in buccal films, as they affect the physical stability of films; due to low or high humidity, buccal films become more rigid or softer, and due to UV light, color of the buccal film turns into orange-brown and cracks on the surface occurs. Buccal films represent an adequate pharmaceutical form for incorporating trans-resveratrol, as these, if films are stored in the primary packaging, are stable under different storage conditions.