Izboljševanje raztapljanja resveratrola iz trdnih disperzij z mezoporoznim silicijevim dioksidom

Berglez, Pia (avtor), Planinšek, Odon (mentor)

Resveratrol je v vodi zelo težko topna snov. Izboljšanje njegove topnosti in hitrosti raztapljanja smo želeli doseči z izdelavo trdnih disperzij z mezoporoznim silicijevim dioksidom Syloid® 244 FP. Izdelovali smo jih z metodo odparevanja topila v rotacijskem uparjevalniku in s sušenjem z razprševanjem. Izdelali smo trdne disperzije z 20 % in 30 % vsebnostjo resveratrola v šestih topilih; v metanolu, acetonu, etanolu, etil acetatu, izopropanolu in tetrahidrofuranu. Z UV-Vis spektrofotometrom smo preverjali vsebnost resveratrola v trdnih disperzijah ter njegovo sproščanje iz trdnih disperzij. Kristalnost oziroma amorfnost vzorca smo vrednotili z diferenčnim dinamičnim kalorimetrom. Preverjali smo fizikalno stabilnost resveratrola in trdnih disperzij po 4-tedenskem staranju na povišani temperaturi in zračni vlagi. Cilj je bil vgraditi resveratrol v mezoporozni silikatni nosilec v amorfnem stanju, kar nam ni popolnoma uspelo. Kljub temu pa smo opazili izboljšano sproščanje resveratrola iz trdnih disperzij v primerjavi s čistim resveratrolom. Ugotovili smo dvostopenjsko sproščanje resveratrola iz trdnih disperzij - hitro začetno, ki čez čas doseže plato in se ustali. Na potek sproščanja resveratrola iz trdne disperzije vpliva kombinacija deleža resveratrola glede na Syloid® 244 FP, izbira topila za izdelavo trdne disperzije in metoda izdelave trdne disperzije. Trdne disperzije, izdelane s sušenjem z razprševanjem, so pokazale hitrejše in obsežnejše sproščanje kot tiste, izdelane z rotacijskim odparevanjem. Trdne disperzije z 20 % deležem resveratrola dajo boljše začetno sproščanje kot 30 % trdne disperzije. Za najbolj polarni topili aceton in metanol smo ugotovili najobsežnejše začetno sproščanje pri 20 % in 30 % trdnih disperzijah. Ugotovili smo, da je stabilnost trdnih disperzij z resveratrolom in Syloid® 244 FP nepredvidljiva in bi jo bilo potrebno še nadalje raziskati.

• Jezik: Slovenski jezik
• Ključne besede: mezoporozni silicijev dioksid, raztapljanje, resveratrol, topnost, trdna disperzija
• Vrsta gradiva: Magistrsko delo/naloga
• Organizacija: FFA - Fakulteta za farmacijo
• Leto izida: 2024
• PID: 20.500.12556/RUL-161219
• Datum objave v RUL: 08.09.2024

Sekundarni jezik

• Jezik: Angleški jezik
• Naslov: Improving the dissolution of resveratrol from solid dispersions with mesoporous silicon dioxide

Izvleček

Resveratrol is a compound with very low solubility in water. To enhance the solubility and dissolution rate of resveratrol, we aimed to create solid dispersions using mesoporous silica Syloid® 244 FP as a carrier. Solid dispersions were prepared via solvent evaporation using rotary evaporation and compared with spray drying. 20 % and 30 % solid dispersions of resveratrol in six solvents (methanol, acetone, ethanol, ethyl acetate, isopropanol, and tetrahydrofuran) were prepared. The resveratrol content in the solid dispersions and its release from these dispersions were analyzed using UV-Vis spectrophotometry. The crystallinity or amorphous nature of the samples was evaluated by differential scanning calorimetry. We assessed the physical stability of resveratrol and the solid dispersions after a 4-week aging period under elevated temperature and humidity conditions. The objective was to incorporate resveratrol into the mesoporous silica carrier in an amorphous state, which was not fully achieved. Nevertheless, we observed improved release of resveratrol from the solid dispersions compared to pure resveratrol. The release profile of resveratrol from solid dispersions exhibited a biphasic pattern - a rapid initial release that eventually reached a plateau. The release behavior of resveratrol from solid dispersions is influenced by the ratio of resveratrol to Syloid® 244 FP, the choice of solvent used for preparing the solid dispersion, and the method of solvent evaporation. Solid dispersions prepared by spray drying demonstrated faster and more extensive release than those prepared by rotary evaporation. Solid dispersions with a 20 % resveratrol content showed better initial release than those with a 30 % content. Among the solvents, acetone and methanol led to the most extensive initial release for both 20 % and 30 % solid dispersions. We concluded that the stability of solid dispersions containing resveratrol and Syloid® 244 FP is unpredictable and requires further investigation.

• Ključne besede: mesoporous silica, dissolution, resveratrol, solubility, solid dispersions