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Abstrak :
ABSTRAK
Luteolin 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.

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ABSTRACT
Luteolin 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

Abstrak :
ABSTRAK
Rute penghantaran obat transdermal membutuhkan eksipien khusus untuk menghantarkan obat melalui kulit menuju sistemik. Tujuan penelitian ini adalah membuat dan menganalisis kemampuan penetrasi hidrogel transdermal yang dibuat dari eksipien koproses amilosa tersambungsilang6 – xanthan gum (Ko-CLA6-XG) pada perbandingan 1:2 sebagai pembentuk matriks dan natrium diklofenak sebagai model obat. Uji penetrasi in vitro dilakukan menggunakan sel difusi Franz dan dianalisis dengan spektrofotometer UV. Uji penetrasi in vivo dilakukan dengan mengaplikasikan hidrogel transdermal berukuran 1 x 1 cm pada bagian abdomen tikus jantan galur Sprague-Dawley. Analisis hasil uji penetrasi in vivo dilakukan menggunakan kromatografi cair kinerja tinggi (KCKT) dengan detektor photodiode array (PDA). Hasil uji penetrasi in vitro menunjukkan jumlah kumulatif obat yang terpenetrasi selama 12 jam sebesar 7629 ± 2711 µg.cm-2 dengan fluks sebesar 655,23 ± 216,43 µg.cm-2.jam-1. Profil pelepasan natrium diklofenak dari hasil uji penetrasi in vivo memberikan konsentrasi puncak plasma (Cmax) sebesar 4,35 ± 0,94 µg.ml-1 pada 1 jam dengan nilai area di bawah kurva (AUC 0-∞) 54,35 ± 7,55 µg.ml-1.jam. Berdasarkan hasil tersebut, hidrogel transdermal dengan eksipien Ko-CLA6-XG (1:2) mampu mempenetrasikan dan mengendalikan pelepasan natrium diklofenak selama 12 jam.

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ABSTRACT
Transdermal drug delivery needs specific excipient to deliver drug through the skin. The goals of this research were produced and analyzed penetration ability of transdermal hydrogel based on co-processed excipient of xanthan gum and 6-cross-linked amylose (Co-CLA6-XG) in 1:2 composition as matrix-forming and diclofenac sodium as a drug model. In vitro penetration study was evaluated using Franz diffusion cell and analyzed by UV-spectrophotometre. In vivo penetration study was performed by applying a transdermal hydrogel in size of 1 x 1 cm on the abdomen of Sprague-Dawley rats. Plasma concentration of diclofenac was analyzed by high-performance liquid chromatography (HPLC) with photodiode array (PDA) detector. In vitro penetration study showed that the cumulative drug permeated across the skin for 12 hours was 7629 ± 2711 µg.cm-2 with flux 655.23 ± 216.43 µg.cm-2.hours-1. The results of in vivo study showed that maximum plasma concentration (Cmax) was 4.35 ± 0.94 µg.ml-1 during 1 hour and area under curve (AUC 0-∞) was 54.35 ± 7.55 µg.ml-1.hour. According to the results, it can be concluded that transdermal hydrogel based on Co-CLA6-XG (1:2) excipient is able to deliver and penetrate diclofenac sodium release during 12 hours.

Abstrak :
Transdermal drug delivery system (TDDS) adalah sistem penghantaran obat yang digunakan pada permukaan kulit dengan tujuan sistemik. Untuk itu, diperlukan suatu eksipien pembentuk matriks transdermal yang dapat menghantarkan obat masuk ke dalam kulit. Penelitian ini bertujuan untuk mengembangkan eksipien koproses xanthan gum dan amilosa tersambungsilang-6 (Ko-CLA6-XG) sebagai matriks sediaan transdermal, kemudian dilakukan uji penetrasi secara in vitro dan in vivo. Ko-CLA6-XG diformulasikan dalam bentuk hidrogel dengan model obat natrium diklofenak. Uji penetrasi in vitro dilakukan menggunakan sel difusi Franz yang kemudian dianalisis dengan spektrofotometer UV. Uji in vivo dilakukan dengan cara mengaplikasikan satu gram hidrogel dengan luas aplikasi 1,13 cm2 di atas kulit tikus bagian abdomen, kemudian sampel darah dikumpulkan melalui sinus orbitalis mata dan dianalisis menggunakan kromatografi cair kinerja tinggi (KCKT). Hasil uji penetrasi in vitro menunjukkan jumlah kumulatif obat yang terpenetrasi ke dalam kulit hingga 12 jam sebanyak 1435 ± 180 µg cm-2 dengan fluks total sebesar 118,55 ± 23,01 µg cm-2 jam-1 (r=0,0994) dan waktu tunda selama 48,6 ± 15,6 menit. Profil pelepasan natrium diklofenak selama 12 jam pada uji in vivo mencapai konsentrasi puncak plasma sebesar 2236 ± 398 ng/ml pada 0,86 ± 0,21 jam dengan AUC sebesar 25273 ± 4133 ng ml-1 jam. Kedua hasil uji memberikan gambaran bahwa hidrogel mengandung natrium diklofenak dengan Ko-CLA6-XG sebagai matriks dapat dikembangkan untuk sediaan transdermal. ......Transdermal drug delivery system (TDDS) is the administration of therapeutic agents through the skin for systemic effect. Therefore, it requires an excipient for transdermal matrix-forming that can deliver drug across the skin. This present research was intended to develop the utilization of coprocessed excipient of xanthan gum and 6-cross-linked amylose (Co-CLA6-XG) as a matrix for transdermal and then evaluate the in vitro and in vivo penetration. Co-CLA6-XG was formulated as hydrogel with sodium diclofenac as a drug model. In vitro penetration study was evaluated using Franz diffusion cell analysed with spectrophotometre UV. The in vivo experiment was performed by applied one gram of hydrogel spread over 1,13 cm2 to the rat abdoment skin, then the blood samples were obtained from sinus orbitalis and analysed with high-performance liquid chromatography (HPLC). In vitro study records the cumulative drug permeated across the skin for 12 hours ranged 1435 ± 180 µg cm-2 and shows the transdermal flux 118,55 ± 23,01 µg cm-2 hours-1 (r = 0,994) with the lag time value ranged 48,6 ± 15,6 min. The release profile of sodium diclofenac for 12 hours in vivo reached a maximum peak of 2236 ± 398 ng/ml at 0,86 ± 0,21 hours with the AUC value was 25273 ± 4133 ng ml-1 hour. Thus diclofenaccontaining hydrogel using Co-CLA6-XG as a matrix could be developed as transdermal drug delivery.