ABSTRAK
Linestrenol merupakan derivat hormon progestin yang dapat menekan produksihormon estrogen dan progesteron sehingga ovulasi tidak terjadi. Akan tetapibioavaailabilitas linestrenol dalam sediaan oral 65% dengan waktu paruh 5-6 jam, dan efeksamping rasa tegang pada payudara. Penelitian ini bertujuan untuk meningkatkan penetrasisubkutan linestrenol dengan formulasi transfersom. Optimalisasi linestrenol dalamtransfersom dilakukan dengan variasi lipid surfaktan (fosfolipid-Tween 80) denganperbandingan 90:10 (F1) dan 80:20 (F2). Karakterisasi transfersom linestrenol meliputiukuran partikel, indeks polidipersitas, potensial zeta dan efisiensi penjerapan.Hasiloptimalisasi terbaik diformulasikan dalam gel untuk uji penetrasi subkutan in vitro dan invivo.Uji penetrasi subkutan in vitro dilakukan dengan sel difusi Franz dan uji in vivodilakukan menggunakan tikus putih betina galur Sprague Dawley. Hasil optimalisasiterbaik transfersom yaitu F2 dengan ukuran partikel 73,113 ± 1,340 nm, indekspolidipersitas 0,312 ± 0,03, potensial zeta -32,166 ± 1,64 mV, dan efisiensi penjerapan89,668 ± 0,602%. Penetrasi subkutan gel transferom linestrenol secara in vitrolebih tinggidibandingan gel non transfersom dengan nilai fluks40,02 ± 5,236 ng/cm2.. Pada hasil uji invivo konsentrasi linestrenol dalam plasma dari sediaan gel transfersom linestrenol lebihtinggi dari sediaan gel non transfersom dengan nilaiarea under the curve (AUC) sebesar24.336 ng/mL jam.Berdasarkan hasil tersebut dapat disimpulkan bahwa formula geltransferosom dapat meningkatkan penetrasi subkutandan ketersediaan hayati linestrenolbila dibandingkan dengan formula gel non transfersom.
ABSTRACT
Lynestrenol is a progestin hormone derivative that can suppress the production ofendogenous estrogen and progesterone hormones (ovaries) so that ovulation does not occur.However, bioavailability of linestrenol in oral preparations 65% with half life of 5-6 hours,and side effects of tension in the breast. This aim of this study was toimprovedsubcutaneous penetration of lynestrenol by transferosome formulation.Lynestrenol transferosome was optimalizaed by lipid:surfactant variation 90:10 (F1) and80:20 (F2). The characterization of lynestrenol transferosome were particle size,polydispersity index, zeta potential, and entrapment efficiency. The best result ofoptimalization was formulated into gel dosage form for in vitro subcutaneous penetrationand in vivo study. In vitro subcutaneous penetration study conducted using cell difussionFranz and in vivo study conducted using female white rats Sprague Dawley strain. The bestoptimalization transferosome was F2 with particle size of 73.113 ± 1.340 nm,polydispersity index of 0.312 ± 0.03, zeta potential of -32.166 ± 1.64 mV, and entrapmentefficiency of 89.091 ± 0.310 %. Subcutaneous penetration of lynestrenol transferosomal gelin in vitro higher than non transferosomal gel with flux 40.02 ± 5.236 ng/cm2.. The resulf ofin vivo study showed that lynestrenol in plasma from lynestrenol transferosomal gel washigher than non transferosomal gel with area under the curve (AUC) 24336ng/mL.hour. Itcould be concluded that formula transferosomal gel increased subcutaneous penetration andbioavailability of lynestrenol compared with non transferosomal gel. |
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