Hasil Pencarian  ::  Simpan CSV :: Kembali

"ABSTRAKLuteolin merupakan kandidat yang poten sebagai alternatif pengobatan penyakit asam urat karena aktivitas antiinflamasi dan penghambatan xantin oksidase. Akan tetapi, kelarutan dan permeabilitas luteolin yang kurang baikmerupakan masalahdalam pengembangan formula. Penelitian ini bertujuan untuk meningkatkan penetrasi luteolin ke dalam kulitmelalui formulasi transfersom luteolin.Luteolin diformulasikan dalam transfersomdan beberapa variasi formula meliputi konsentrasi total lipid (fosfolipid-Tween 80) dan luteolin dioptimalisasi menggunakan response surface methodology. Respon optimalisasiyang diukur adalah ukuran partikel, indeks polidispersitas, potensial zeta dan efisiensi penjerapan. Uji penetrasi in vitro dan in vivo dilakukan menggunakan tikus putih jantan galur Sprague Dawley.Hasil optimalisasi transfersom luteolin mengindikasikan bahwa konsentrasi total lipid 4,88% dan luteolin 0,5% merupakan formula optimal. Gambaran vesikel menggunakan transmission electron microscope (TEM) memperlihatkan partikel sferis dengan beberapa partikel yang beragregasi. Transfersom luteolin formula optimal mempunyai ukuran partikel 257,18±15,20 nm, indeks polidispersitas0,480±0,013, potential zeta -18,67±0,379 mV danefisiensi penjerapan 94,97±0,28%. Penetrasi luteolin secarain vitropada gel transfersom luteolin sebesar 16,49% dengan nilai fluks 126,80±5,09 μg/cm2/jam. Hasil tersebut lebih tinggi dibandingkan dengan gel luteolin yaitu 6,27% dan fluks 24,03±2,32 μg/cm2/jam. Penetrasi in vivomemberikan nilai Cmaksdan AUC0-∞ sebesar 9982,29 ng/mL dan 25329,94 ng.jam/mL pada gel transfersom luteolin dan 2908,34 ng/mL dan 7965,88 ng.jam/mL pada gel luteolin.Dari hasil penelitian dapat disimpulkan bahwa transfersom luteolin mampu meningkatkan penetrasi melalui kulit, baik secara in vitromaupunin vivo.

---

ABSTRACTLuteolin is a potent candidate as an alternative treatment for gout due to its xanthine oxidase inhibition and anti-inflammatory activities. However, its poor solubility and permeability are hampering its formulationand development process. This study aimed to improve skin penetration of luteolin by luteolin transfersome formulation. Luteolin transfersome fistly was prepared, and various formulation variables including total lipid (phospholipid-Tween 80) and luteolin concentration were optimized using response surface methodology. Measured responses of optimization were particle size, polydispersity index, zeta potential and entrapment efficiency. In vitro and in vivo penetration studies were carried out using Sprague Dawley male rats. The results of optimization indicate that 4.88% total lipid and 0.5% luteolin concentration is the optimum formulation. Vesicle image using transmission electron microscope (TEM) revealed spherical particles and occurrence of particle aggregation. The optimumluteolin transfersome had particle size of 257.18±15.20 nm, polidispersity index of 0.480±0.013, zeta potential of -18.67±0.379 mV and entrapment efficiency of 94.97±0.28%. In vitro penetration experiment of luteolin transfersome gel showed that16.49% of luteolin was penetrated with flux parameter was of 126.80±5.09 μg/cm2/h. It was significantly higher compared to luteolin gel which only6.27%of luteolin was penetrated and flux of 24.03±2.32 μg/cm2/h. Moreover, in vivo penetration study showed that Cmax and AUC0-∞of luteolin transfersome gel were 9982.29ng/Ml and 25329.94 ng.h/mL,respectively, which was higher than those of luteolin gel (2908.34 ng/mL and7965.88 ng.h/mL). It was concluded that luteolin transfersome enhaced in vitro and in vivo penetration of luteolin"

"ABSTRAKFormulasi, Karakterisasi, dan Evaluasi in vivo Fitosom Luteolin Dalam penelitian ini, telah dikembangkan fitosom luteolin, suatu sistempenghantaran obat baru. Luteolin dilaporkan memiliki aktivitas antioksidan,antimikroba, dan antiinflamasi namun memiliki ketersediaan hayati oral yang rendahkarena memiliki kelarutan dalam lipid yang rendah. Tujuan penelitian ini adalahuntuk meningkatkan absorpsi luteolin dalam saluran cerna. Fitosom luteolin dibuatdengan metode hidrasi lapis tipis, kemudian dikarakterisasi menggunakan ParticleSize Analyzer PSA , mikroskop transmisi elektron TEM , dan spektrofotometerFourier Transforms Infrared FTIR . Larutan luteolin dalam metanol dan larutanfosfatidilkolin dalam diklorometan direfluks 4 jam, 60oC , kemudian pelarutdiuapkan menggunakan vacuum evaporator 337 mbar, 40oC untuk membentuklapis tipis yang kemudian dihidrasi dengan air suling. Evaluasi in vivo kemudiandilakukan untuk melihat kadar plasma luteolin pada tikus yang diberi suspensifitosom luteolin per oral dan dibandingkan dengan kadar plasma luteolin pada tikusdalam kelompok kontrol yang diberi suspensi luteolin murni. Hasil karakterisasimenunjukkan partikel fitosom luteolin berbentuk spheric dengan diameter rata-ratapartikel 105,3 nm dan efisiensi penjerapan 91,12 . Spektrum FTIR menunjukkanbahwa pembentukan fitosom terjadi karena adanya interaksi ikatan hidrogen antaraluteolin dengan fosfatidilkolin yang ditandai dengan munculnya puncak baru padabilangan gelombang 1360 cm-1 dan perubahan intensitas pita pada bilangangelombang 1730 cm-1. Hasil evaluasi in vivo menunjukkan peningkatan kadarplasma luteolin AUC = 5426 ?g.menit/mL sebesar 3,54 kali jika dibandingkandengan kelompok kontrol. Formulasi fitosom yang dibuat berhasil meningkatkanabsopsi luteolin sehingga dapat dijadikan sebagai sistem penghantaran yangmenjanjikan untuk obat-obat dengan kelarutan dalam lipid yang rendah. Kata kunci : fitosom, fosfatidilkolin, hidrasi lapis tipis, kadar plasma, luteolinxiv 75 halaman; 16 gambar; 6 tabel; 12 lampiranBibliography : 31 1998-2015.

---

ABSTRACTFormulation, Characterization, and in vivo Evaluation of Luteolin Loaded Phytosome In this study, a novel drug delivery system, luteolin loaded phytosome LLP hasbeen developed. Luteolin exhibits antioxidant, antimicrobial, andantiinflammation activities. However, it shows poor oral bioavailability due to itslow lipid solubility. The aim of this study was to improve absorption of luteolin inthe gastro intestinal tract. The LLPs were prepared by thin film hydration methodand characterized using particle size analyzer PSA , transmission electronmicroscopy TEM , and fourier transforms infrared spectroscopy FTIR . Thesolution of luteolin in methanol and phosphatidilcholine solution indichloromethane were refluxed 4h, 60 oC , solvents then removed by vacuumevaporator 337 mbar, 40oC to produce the thin film which was hydrated withdistilled water. In vivo evaluations were then performed to see plasma levels ofluteolin in rats given oral luteolin phytosome suspension and compared with thosein the control group given pure luteolin suspension. Final phytosome wasspherical with average particle size of 105.3 nm and entrapment efficiency of91.12 . FTIR spectra demonstrated that phytosomes were formed, as there washydrogen bonding between luteolin and phosphatidilcholine, marked byappearance of new peak at wave numbers of 1360 cm 1 and changes in bandintensity at 1730 cm 1 wave numbers. In vivo studies showed a 3.54 fold increasein plasma level AUC AUC 5426 g.min mL of luteolin compared with thosein control group. Phytosomes formulation successfully increased the absorption ofluteolin hence it can serve as a promising delivery system for drugs with lowlipids solubility. Keywords luteolin, phosphatidilcholine, phytosome, plasma concentration,thin film hydrationxiv 75 pages 16 pictures 6 tables 12 appendicesBibliography 31 1998 2015 "