ABSTRAKLinestrenol merupakan derivat hormon progestin yang dapat menekan produksi
hormon estrogen dan progesteron sehingga ovulasi tidak terjadi. Akan tetapi
bioavaailabilitas linestrenol dalam sediaan oral 65% dengan waktu paruh 5-6 jam, dan efek
samping rasa tegang pada payudara. Penelitian ini bertujuan untuk meningkatkan penetrasi
subkutan linestrenol dengan formulasi transfersom. Optimalisasi linestrenol dalam
transfersom dilakukan dengan variasi lipid surfaktan (fosfolipid-Tween 80) dengan
perbandingan 90:10 (F1) dan 80:20 (F2). Karakterisasi transfersom linestrenol meliputi
ukuran partikel, indeks polidipersitas, potensial zeta dan efisiensi penjerapan.Hasil
optimalisasi terbaik diformulasikan dalam gel untuk uji penetrasi subkutan in vitro dan in
vivo.Uji penetrasi subkutan in vitro dilakukan dengan sel difusi Franz dan uji in vivo
dilakukan menggunakan tikus putih betina galur Sprague Dawley. Hasil optimalisasi
terbaik transfersom yaitu F2 dengan ukuran partikel 73,113 ± 1,340 nm, indeks
polidipersitas 0,312 ± 0,03, potensial zeta -32,166 ± 1,64 mV, dan efisiensi penjerapan
89,668 ± 0,602%. Penetrasi subkutan gel transferom linestrenol secara in vitrolebih tinggi
dibandingan gel non transfersom dengan nilai fluks40,02 ± 5,236 ng/cm2.. Pada hasil uji in
vivo konsentrasi linestrenol dalam plasma dari sediaan gel transfersom linestrenol lebih
tinggi dari sediaan gel non transfersom dengan nilaiarea under the curve (AUC) sebesar
24.336 ng/mL jam.Berdasarkan hasil tersebut dapat disimpulkan bahwa formula gel
transferosom dapat meningkatkan penetrasi subkutandan ketersediaan hayati linestrenol
bila dibandingkan dengan formula gel non transfersom.
ABSTRACTLynestrenol is a progestin hormone derivative that can suppress the production of
endogenous 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 to
improvedsubcutaneous penetration of lynestrenol by transferosome formulation.
Lynestrenol transferosome was optimalizaed by lipid:surfactant variation 90:10 (F1) and
80:20 (F2). The characterization of lynestrenol transferosome were particle size,
polydispersity index, zeta potential, and entrapment efficiency. The best result of
optimalization was formulated into gel dosage form for in vitro subcutaneous penetration
and in vivo study. In vitro subcutaneous penetration study conducted using cell difussion
Franz and in vivo study conducted using female white rats Sprague Dawley strain. The best
optimalization 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 entrapment
efficiency of 89.091 ± 0.310 %. Subcutaneous penetration of lynestrenol transferosomal gel
in in vitro higher than non transferosomal gel with flux 40.02 ± 5.236 ng/cm2.. The resulf of
in vivo study showed that lynestrenol in plasma from lynestrenol transferosomal gel was
higher than non transferosomal gel with area under the curve (AUC) 24336ng/mL.hour. It
could be concluded that formula transferosomal gel increased subcutaneous penetration and
bioavailability of lynestrenol compared with non transferosomal gel.
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