OPTIMASI FORMULA MATRIKS TRANSDERMAL PENTAGAMAVUNON-0 DENGAN KOMBINASI POLIMER PVP DAN METILSELULOSA MENGGUNAKAN SIMPLEX LATTICE DESIGN

Metha Anung A, Dr. Akhmad Kharis Nugroho,M.Si., Apt.

2014 | Tesis | S2 Ilmu Farmasi

Pentagamavunon-0 (PGV-0) sangat mungkin dihantarkan melaui sistem penghantaran secara transdermal. Penelitian ini bertujuan untuk membuat matriks transdermal PGV-0 dengan karakter fisikokimia dan laju pelepasan yang optimal serta ingin mengetahui transpor transdermal PGV-0 melewati kulit secara in vitro pada formula matriks transdermal optimal. Kombinasi polimer PVP dan metilselulosa penyusun matriks ditentukan dengan bantuan software Design Expert 7.1.5. Pengujian karakter fisikokimia dilakukan dengan mengevaluasi bobot matriks, tebal matriks, % moisture content, % moisture uptake, folding endurance, dan drug content. Pelepasan PGV-0 dilakukan selama 6 jam menggunakan membran Millipore pada sel difusi vertikal. Optimasi formula dilakukan dengan memasukkan respon yang berpengaruh signifikan. Pengujian transpor transdermal formula matriks PGV-0 optimal dilakukan selama 24 jam menggunakan sel difusi vertikal dan membran kulit tikus. Seluruh formula dapat menghasilkan matriks transdermal yang seragam dan fleksibel. Hasil yang signifikan ditunjukkan oleh respon bobot matriks, tebal matriks, drug content, dan dissolution efficiency uji pelepasan matriks PGV-0. Kombinasi polimer PVP 2,436% dan metilselulosa 1,564% pada formula optimal menghasilkan matriks transdermal PGV-0 yang berwarna kuning muda, rata, dan fleksibel. Matriks yang optimal memiliki bobot 0,304 g, tebal 0,378 mm, drug content 101,37%, dan dissolution efficiency 21,33%. Hasil uji pelepasan pada matriks formula optimal dianalisis dengan menggunakan metode model kompartemen. Data tersebut menunjukkan bahwa pelepasan PGV-0 dari matriks transdermal mengikuti model 4 kompartemen dengan 2 kompartemen lag. Matriks transdermal PGV-0 pada formula optimal belum dapat memberikan transpor PGV-0 melewati kulit.

Transdermal delivery system is possible to transport PGV-0. This study was aimed 1) to formulate PGV-0 transdermal matrix with optimal physicochemical characteristics and release rate, 2) to establish the in vitro transport profile of transdermal PGV-0 across the skin. The combination of PVP and methylcellulose in transdermal matrix of PGV-0 was determined by Design Expert 7.1.5. The physicocemical characteristics consist of weight, thickness, % moisture content, % moisture uptake, folding endurance, and drug content were evaluated. PGV-0 release rate was tested using Millipore membrane in a vertical diffusion cells for 6 hours. Optimization of the matrix formula was performed based on the significant responses. Transdermal transport study was carried out on optimal formula using vertical diffusion cell and full-thickness rat skin for 24 hours. The entire formulas could produce uniform and flexible transdermal matrices. The combination of PVP and methylcellulose had a significant influence on the weight, thickness, drug content, and dissolution efficiency of PGV-0 transdermal matrix. The combination of 2.436 % PVP and 1.564 % methylcellulose as an optimal formula produces light yellow, flat, and flexible PGV-0 transdermal matrix. The optimal matrix had weight of 0.304 g, thickness of 0.378 mm, drug content of 101.37 %, and dissolution efficiency of 21.33%. The release results of optimal matrix was analyzed using compartement model method. The data results indicates that the release profile of PGV-0 from transdermal matrix follow 4 compartements model with 2 compartements lag. The optimal formula of transdermal matrix could not transport PGV-0 across the skin.

Kata Kunci : PGV-0, matriks, transdermal, PVP, metilselulosa