Mechanical properties and long-term stability of novel lipid formulations with simvastatin
Mehanička svojstva i dugotrajna stabilnost novih lipidnih formulacija sa simvastatinom
Конференцијски прилог (Објављена верзија)
Метаподаци
Приказ свих података о документуАпстракт
Mixing selected liquid SMEDDS with polymethacrylate polymers (Eudragit ®) led to
solidification of the samples to form solid, ductile, transparent systems (1). The purpose of
this study was to define mechanical properties and long-term stability of novel simvastatin-
loaded SMEDDS-based drug delivery systems. SMEDDS-based formulations were prepared
by adding liquid SMEDDS (10% oleoyl macrogol-6 glycerides and 90% caprylocaproyl
macrogol-8 glycerides/macrogol-15-hydroxystearate, in 3 ratios: 1:1, 2:1 and 3:1) to
Eudragit ® S100 or Eudragit ® S100/Eudragit ® L100 combination (in 1:1 ratio), until
SMEDDS/polymer ratio 2:1 w/w was reached. SMEDDS-based formulations with simvastatin
(SV) were prepared by dissolving SV (5%) into liquid SMEDDS and mixing with
polymethacrylate polymers in the same ratio. Prepared formulations were evaluated in
terms of their mechanical properties and long-term stability. The results indicated that the
increase in the caprylocaproyl macrogol-8 glycer...ides concentration resulted in higher
penetration force (F1 S100–F3 S100 = 5.83-7.22 N and F1 SL100-F3 SL100 = 4.20-5.99 N).
However, addition of SV was negatively correlated with the hardness, i.e. samples with SV
were softer in comparison to unloaded samples. Moreover, it was noticeable that
formulations with Eudragit ® S100 had greater penetration force values compared to
formulations containing Eudragit ® S100/Eudragit ® L100. After six months of storage at
room and elevated temperature, only slight decrease in SV content (less than 5%) was
observed in these samples. This study demonstrated that novel SMEDDS-based formulations
with higher concentration of caprylocaproyl macrogol-8 glycerides and those with Eudragit ®
S100 were more robust, which may further serve as a guide for formulating tailor-made
formulations.
Mešanje odabranih tečnih samomikroemulgujućih sistema (SMEDDS) sa
kopolimerima metakrilne kiseline (Eudragit ® ) dovodi do očvršćavanja uzoraka i formiranja
čvrstih, rastegljivih, transparentnih sistema (1). Cilj ovog rada je bio ispitivanje mehaničkih
svojstva i dugotrajne stabilnosti novih lipidnih sistema sa simvastatinom (SV). Lipidne
formulacije su izrađene mešanjem tečnih SMEDDS (10% oleoil makrogol-6 glicerida i 90%
kaprilokaproil makrogol-8 glicerida/makrogol-15-hidroksistearat, u 3 odnosa: 1:1, 2:1 i 3:1)
i Eudragit ® S100 ili kombinacije Eudragit ® S100/Eudragit ® L100 (u odnosu 1:1). Odnos
SMEDDS/polimer bio je 2:1, m/m. Uzorci sa SV su izrađeni rastvaranjem SV (5%) u tečnim
SMEDDS i mešanjem sa kopolimerima metakrilne kiseline u navedenom odnosu. Sprovedena
su ispitivanja mehaničkih osobina i dugotrajne stabilnosti izrađenih lipidnih formulacija.
Rezultati su pokazali da povećanje koncentracije kaprilokaproil makrogol-8 glicerida dovodi
do povećanja vrednosti s...ile penetracije (F1 S100–F3 S100 = 5,83-7,22 N i F1 SL100-F3
SL100 = 4,20-5,99 N). Uzorci sa SV su bili mekši, u poređenju sa uzorcima bez lekovite
supstance. Takođe, uočeno je da uzorci sa polimerom Eudragit ® S100 imaju već e vrednosti
sile penetracije, u poređenju sa formulacijama koje sadrže kombinaciju Eudragit ®
S100/Eudragit ® L100. Posle šest meseci skladištenja uzoraka na sobnoj i povišenoj
temperaturi, sadržaj SV je neznatno smanjen (manje od 5%). Ova studija je pokazala da nove
lipidne formulacije izrađene sa većom koncentracijom kaprilokaproil makrogol-8 glicerida i
sa Eudragit ® S100 polimerom imaju veće vrednosti sile penetracije i prihvatljivu dugotrajnu
stabilnost, što je od značaja za razvoj lipidnih formulacija željenih karakteristika.
Извор:
Arhiv za farmaciju, 2022, 72, 4 suplement, S396-S397Издавач:
- Savez farmaceutskih udruženja Srbije (SFUS)
Финансирање / пројекти:
- Министарство науке, технолошког развоја и иновација Републике Србије, институционално финансирање - 200161 (Универзитет у Београду, Фармацеутски факултет) (RS-MESTD-inst-2020-200161)
Напомена:
- VIII Kongres farmaceuta Srbije sa međunarodnim učešćem, 12-15.10.2022. Beograd
Институција/група
PharmacyTY - CONF AU - Ćetković, Zora AU - Vasiljević, Ivana AU - Cvijić, Sandra AU - Vasiljević, Dragana PY - 2022 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/4567 AB - Mixing selected liquid SMEDDS with polymethacrylate polymers (Eudragit ®) led to solidification of the samples to form solid, ductile, transparent systems (1). The purpose of this study was to define mechanical properties and long-term stability of novel simvastatin- loaded SMEDDS-based drug delivery systems. SMEDDS-based formulations were prepared by adding liquid SMEDDS (10% oleoyl macrogol-6 glycerides and 90% caprylocaproyl macrogol-8 glycerides/macrogol-15-hydroxystearate, in 3 ratios: 1:1, 2:1 and 3:1) to Eudragit ® S100 or Eudragit ® S100/Eudragit ® L100 combination (in 1:1 ratio), until SMEDDS/polymer ratio 2:1 w/w was reached. SMEDDS-based formulations with simvastatin (SV) were prepared by dissolving SV (5%) into liquid SMEDDS and mixing with polymethacrylate polymers in the same ratio. Prepared formulations were evaluated in terms of their mechanical properties and long-term stability. The results indicated that the increase in the caprylocaproyl macrogol-8 glycerides concentration resulted in higher penetration force (F1 S100–F3 S100 = 5.83-7.22 N and F1 SL100-F3 SL100 = 4.20-5.99 N). However, addition of SV was negatively correlated with the hardness, i.e. samples with SV were softer in comparison to unloaded samples. Moreover, it was noticeable that formulations with Eudragit ® S100 had greater penetration force values compared to formulations containing Eudragit ® S100/Eudragit ® L100. After six months of storage at room and elevated temperature, only slight decrease in SV content (less than 5%) was observed in these samples. This study demonstrated that novel SMEDDS-based formulations with higher concentration of caprylocaproyl macrogol-8 glycerides and those with Eudragit ® S100 were more robust, which may further serve as a guide for formulating tailor-made formulations. AB - Mešanje odabranih tečnih samomikroemulgujućih sistema (SMEDDS) sa kopolimerima metakrilne kiseline (Eudragit ® ) dovodi do očvršćavanja uzoraka i formiranja čvrstih, rastegljivih, transparentnih sistema (1). Cilj ovog rada je bio ispitivanje mehaničkih svojstva i dugotrajne stabilnosti novih lipidnih sistema sa simvastatinom (SV). Lipidne formulacije su izrađene mešanjem tečnih SMEDDS (10% oleoil makrogol-6 glicerida i 90% kaprilokaproil makrogol-8 glicerida/makrogol-15-hidroksistearat, u 3 odnosa: 1:1, 2:1 i 3:1) i Eudragit ® S100 ili kombinacije Eudragit ® S100/Eudragit ® L100 (u odnosu 1:1). Odnos SMEDDS/polimer bio je 2:1, m/m. Uzorci sa SV su izrađeni rastvaranjem SV (5%) u tečnim SMEDDS i mešanjem sa kopolimerima metakrilne kiseline u navedenom odnosu. Sprovedena su ispitivanja mehaničkih osobina i dugotrajne stabilnosti izrađenih lipidnih formulacija. Rezultati su pokazali da povećanje koncentracije kaprilokaproil makrogol-8 glicerida dovodi do povećanja vrednosti sile penetracije (F1 S100–F3 S100 = 5,83-7,22 N i F1 SL100-F3 SL100 = 4,20-5,99 N). Uzorci sa SV su bili mekši, u poređenju sa uzorcima bez lekovite supstance. Takođe, uočeno je da uzorci sa polimerom Eudragit ® S100 imaju već e vrednosti sile penetracije, u poređenju sa formulacijama koje sadrže kombinaciju Eudragit ® S100/Eudragit ® L100. Posle šest meseci skladištenja uzoraka na sobnoj i povišenoj temperaturi, sadržaj SV je neznatno smanjen (manje od 5%). Ova studija je pokazala da nove lipidne formulacije izrađene sa većom koncentracijom kaprilokaproil makrogol-8 glicerida i sa Eudragit ® S100 polimerom imaju veće vrednosti sile penetracije i prihvatljivu dugotrajnu stabilnost, što je od značaja za razvoj lipidnih formulacija željenih karakteristika. PB - Savez farmaceutskih udruženja Srbije (SFUS) C3 - Arhiv za farmaciju T1 - Mechanical properties and long-term stability of novel lipid formulations with simvastatin T1 - Mehanička svojstva i dugotrajna stabilnost novih lipidnih formulacija sa simvastatinom VL - 72 IS - 4 suplement SP - S396 EP - S397 UR - https://hdl.handle.net/21.15107/rcub_farfar_4567 ER -
@conference{ author = "Ćetković, Zora and Vasiljević, Ivana and Cvijić, Sandra and Vasiljević, Dragana", year = "2022", abstract = "Mixing selected liquid SMEDDS with polymethacrylate polymers (Eudragit ®) led to solidification of the samples to form solid, ductile, transparent systems (1). The purpose of this study was to define mechanical properties and long-term stability of novel simvastatin- loaded SMEDDS-based drug delivery systems. SMEDDS-based formulations were prepared by adding liquid SMEDDS (10% oleoyl macrogol-6 glycerides and 90% caprylocaproyl macrogol-8 glycerides/macrogol-15-hydroxystearate, in 3 ratios: 1:1, 2:1 and 3:1) to Eudragit ® S100 or Eudragit ® S100/Eudragit ® L100 combination (in 1:1 ratio), until SMEDDS/polymer ratio 2:1 w/w was reached. SMEDDS-based formulations with simvastatin (SV) were prepared by dissolving SV (5%) into liquid SMEDDS and mixing with polymethacrylate polymers in the same ratio. Prepared formulations were evaluated in terms of their mechanical properties and long-term stability. The results indicated that the increase in the caprylocaproyl macrogol-8 glycerides concentration resulted in higher penetration force (F1 S100–F3 S100 = 5.83-7.22 N and F1 SL100-F3 SL100 = 4.20-5.99 N). However, addition of SV was negatively correlated with the hardness, i.e. samples with SV were softer in comparison to unloaded samples. Moreover, it was noticeable that formulations with Eudragit ® S100 had greater penetration force values compared to formulations containing Eudragit ® S100/Eudragit ® L100. After six months of storage at room and elevated temperature, only slight decrease in SV content (less than 5%) was observed in these samples. This study demonstrated that novel SMEDDS-based formulations with higher concentration of caprylocaproyl macrogol-8 glycerides and those with Eudragit ® S100 were more robust, which may further serve as a guide for formulating tailor-made formulations., Mešanje odabranih tečnih samomikroemulgujućih sistema (SMEDDS) sa kopolimerima metakrilne kiseline (Eudragit ® ) dovodi do očvršćavanja uzoraka i formiranja čvrstih, rastegljivih, transparentnih sistema (1). Cilj ovog rada je bio ispitivanje mehaničkih svojstva i dugotrajne stabilnosti novih lipidnih sistema sa simvastatinom (SV). Lipidne formulacije su izrađene mešanjem tečnih SMEDDS (10% oleoil makrogol-6 glicerida i 90% kaprilokaproil makrogol-8 glicerida/makrogol-15-hidroksistearat, u 3 odnosa: 1:1, 2:1 i 3:1) i Eudragit ® S100 ili kombinacije Eudragit ® S100/Eudragit ® L100 (u odnosu 1:1). Odnos SMEDDS/polimer bio je 2:1, m/m. Uzorci sa SV su izrađeni rastvaranjem SV (5%) u tečnim SMEDDS i mešanjem sa kopolimerima metakrilne kiseline u navedenom odnosu. Sprovedena su ispitivanja mehaničkih osobina i dugotrajne stabilnosti izrađenih lipidnih formulacija. Rezultati su pokazali da povećanje koncentracije kaprilokaproil makrogol-8 glicerida dovodi do povećanja vrednosti sile penetracije (F1 S100–F3 S100 = 5,83-7,22 N i F1 SL100-F3 SL100 = 4,20-5,99 N). Uzorci sa SV su bili mekši, u poređenju sa uzorcima bez lekovite supstance. Takođe, uočeno je da uzorci sa polimerom Eudragit ® S100 imaju već e vrednosti sile penetracije, u poređenju sa formulacijama koje sadrže kombinaciju Eudragit ® S100/Eudragit ® L100. Posle šest meseci skladištenja uzoraka na sobnoj i povišenoj temperaturi, sadržaj SV je neznatno smanjen (manje od 5%). Ova studija je pokazala da nove lipidne formulacije izrađene sa većom koncentracijom kaprilokaproil makrogol-8 glicerida i sa Eudragit ® S100 polimerom imaju veće vrednosti sile penetracije i prihvatljivu dugotrajnu stabilnost, što je od značaja za razvoj lipidnih formulacija željenih karakteristika.", publisher = "Savez farmaceutskih udruženja Srbije (SFUS)", journal = "Arhiv za farmaciju", title = "Mechanical properties and long-term stability of novel lipid formulations with simvastatin, Mehanička svojstva i dugotrajna stabilnost novih lipidnih formulacija sa simvastatinom", volume = "72", number = "4 suplement", pages = "S396-S397", url = "https://hdl.handle.net/21.15107/rcub_farfar_4567" }
Ćetković, Z., Vasiljević, I., Cvijić, S.,& Vasiljević, D.. (2022). Mechanical properties and long-term stability of novel lipid formulations with simvastatin. in Arhiv za farmaciju Savez farmaceutskih udruženja Srbije (SFUS)., 72(4 suplement), S396-S397. https://hdl.handle.net/21.15107/rcub_farfar_4567
Ćetković Z, Vasiljević I, Cvijić S, Vasiljević D. Mechanical properties and long-term stability of novel lipid formulations with simvastatin. in Arhiv za farmaciju. 2022;72(4 suplement):S396-S397. https://hdl.handle.net/21.15107/rcub_farfar_4567 .
Ćetković, Zora, Vasiljević, Ivana, Cvijić, Sandra, Vasiljević, Dragana, "Mechanical properties and long-term stability of novel lipid formulations with simvastatin" in Arhiv za farmaciju, 72, no. 4 suplement (2022):S396-S397, https://hdl.handle.net/21.15107/rcub_farfar_4567 .