ANALISIS PELEPASAN DAN TRANSPOR TRANSDERMAL IN VITRO MATRIKS PENTAGAMAVUNON-0

Beti Pudyastuti, Akhmad Kharis Nugroho, Sudibyo Martono

Abstract


Pentagamavunon-0 (PGV-0) memiliki aktivitas sebagai antioksidan dan anti-inflamasi namun memiliki bioavailabilitas yang rendah pada sistem penghantaran per oral karena mengalami metabolisme lintas pertama yang intensif. Sistem penghantaran transdermal dapat menjadi alternatif untuk mengatasi hal tersebut. Penelitian ini bertujuan untuk menganalisis profil pelepasan dan transpor transdermal PGV-0 secara in vitro pada matriks dengan kombinasi polimer PVP K30 sebesar 1,98% dan HPMC sebesar 4,52%. Uji pelepasan PGV-0 dari matriks dilakukan selama 6 jam dengan membran millipore 0,45 mm, sedangkan uji transpor transdermal secara in vitro dilakukan selama 24 jam melewati membran kulit tikus. Kedua uji menggunakan sel difusi Franz tipe vertikal. Jumlah kumulatif PGV-0 yang dapat dilepaskan dari matriks dan tertranspor dianalisis dengan metode model kompartemen menggunakan piranti lunak WinSAAM versi 3.0.7. Hasil penelitian menunjukkan profil pelepasan PGV-0 dari matriks transdermal mengikuti model 4 kompartemen dengan 2 kompartemen lag. Rerata jumlah PGV-0 yang dapat dilepaskan selama 6 jam sebesar 101,93 ± 6,00 µg sesuai dengan hasil prediksi sebesar 102,22 µg dari total 800 µg PGV-0 dalam matriks. Hasil uji transpor transdermal in vitro selama 24 jam menunjukkan PGV-0 tertranspor masih di bawah batas deteksi 0,021 µg/mL. Penelitian lebih lanjut diperlukan untuk meningkatkan transpor transdermal PGV-0.

Kata kunci: Pentagamavunon-0, Matriks, Transdermal, Transpor

 

Pentagamavunon-0 (PGV-0) has antioxidant and anti-inflamatory activity, but the bioavailability of PGV-0 in peroral route is low due to high intensity of first pass metabolism. Transdermal delivery system could becomes an alternative of PGV-0 delivery. The purposes of this research were to observe the release and in vitro transport profile of PGV-0 from optimum PGV-0 transdermal matrix with a combination of 1,98% PVP K30 and 4,52% HPMC polymers. PGV-0 release study was carried out for 6 hours using 0,45 mm millipore membran, while in vitro transdermal transport study was carried out for 24 hours using full-thickness skin of rat. Both of the study used vertical Franz diffusion cells. Cumulative amounts of PGV-0 that released and transported were analyzed by using WinSAAM 3.0.7 software. The results showed that the release profile of PGV-0 from the matrix followed 4 compartments model with 2 lag compartments. The mean cumulative amount of PGV-0 that could be released for 6 hours was 101,93 ± 6,00 µg as like as prediction value 102,22 µg of 800 µg total in the matrix. The in vitro transdermal transport study during 24 hours showed that the transported PGV-0 was still under detection limit of 0,021 µg/mL. It needs further research to increase the transdermal transport of PGV-0.

Key words: Pentagamavunon-0, Matrix, Transdermal, Transport


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