STABILITAS SEDIAAN MIKROEMULGEL SENYAWA 3,4-DIMETOKSIKALKON DAN UJI AKTIVITASNYA SEBAGAI PELINDUNG SINAR UV-A SECARA IN VITRO

RIZA MAULANA, Dr. Abdul Karim Zulkarnain, M.Si., Apt.

2021 | Tesis | MAGISTER ILMU FARMASI

Senyawa aktif 3,4-dimetoksikalkon diduga memiliki aktivitas sebagai sunscreen yang dapat mengabsorbsi dan mencegah penetrasi sinar ultraviolet A (UV-A) yang dapat menyebabkan berbagai gangguan pada kulit. Tujuan penelitian ini adalah untuk mengevaluasi karakter fisik 3,4-dimetoksikalkon, optimasi dan formulasi sediaan mikroemulgel 3,4-dimetoksikalkon serta mengidentifikasi aktivitasnya sebagai sunscreen, yang dibandingkan dengan bentuk sediaan gelnya. Metode penelitian ini terdiri dari karakterisasi 3,4-dimetoksikalkon meliputi uji kelarutan, koefisien partisi, titik leleh, dan nilai pKa. Selanjutnya, optimasi formula mikroemulsi 3,4-dimetoksikalkon yang terdiri dari campuran minyak (olive oil), surfaktan (tween 80), dan kosurfaktan (PEG 400) menggunakan metode D-Optimal dengan bantuan software Design Expert versi 10 serta aquadest sebagai fase airnya. Pengujian aktivitas mikroemulgel dan gel 3,4-dimetoksikalkon meliputi uji UV-A Protection Factor secara in vitro, uji persen transmisi eritema (%TE) dan persen transmisi pigmentasi (%TP) serta identifikasi pergeseran spektra. Hasil dan kesimpulan yang didapatkan yaitu senyawa 3,4-dimetoksikalkon praktis tidak larut dalam air, lipofilik (log P 5,39 ± 0,019), meleleh pada suhu 79,67 - 81,67 ± 0,58 C dan nilai pKa 11,59 ± 0,02. Formula optimum mikroemulsi, didapatkan dari kombinasi olive oil 3,33%; Tween 80 93,33%; dan PEG-400 3,34% yang didispersikan dalam 8 mL aquadest. Sediaan mikroemulgel 3,4-dimetoksikalkon, baik basis HPMC maupun CMC-Na, memiliki homogenitas yang baik. Viskositas basis HPMC sebesar 298700 ± 1212,44 cP, basis CMC-Na sebesar 87833,3 ± 351,2 cP. Nilai pH 4,64 ± 0,01 (HPMC) dan 6,40 ± 0,01 (CMC-Na), dengan daya lekat >1 detik pada keduanya namun daya sebar kurang baik. Gel dan mikroemulgel 3,4-dimetoksikalkon memiliki kemampuan ultraprotektif terhadap paparan UVA dan perlindungan terhadap pigmentasi (nilai %TP rendah), namun tidak stabil di bawah paparan sinar UVA.

The active compound 3,4-dimethoxychalcone is known to have the activity as a sunscreen that can absorb and prevent ultraviolet A (UV-A) rays, which can cause various skin disorders. The purpose of this study was to evaluate the physical characteristics of 3,4-dimethoxychalcone, optimization and formulation of 3,4-dimethoxychalcone microemulgel, and to identify its activity as a sunscreen compared to its gel dosage form. The research methods consist the characterization of 3,4-dimethoxychalcone included solubility test, partition coefficient, melting point, and pKa value. Furthermore, optimization of the 3,4-dimethoxychalcone microemulsion formula consisting of a mixture of oil (olive oil), surfactant (tween 80), and cosurfactant (PEG 400) using the D-optimal method with the help of Design-Expert software version 10. The mixture would be dispersed onto aquadest as the water phase. Testing for microemulgel and gel 3,4-dimethoxychalcone activity included in vitro UV-A Protection Factor test, test for percent erythema transmission (% TE) and percent transmission pigmentation (% TP), and identification of spectral shifts. Results and conclusions suggest that the compound 3,4-dimethoxychalcone practically insoluble in water, lipophilic (log P 5.39 ± 0.019), melted at a temperature of 79.67 - 81.67 ± 0.58 C and a pKa value of 11.59 ± 0.02. The optimum microemulsion formula was obtained from a combination of olive oil 3.33%; Tween 80 93.33%; and PEG-400 3.34%, which was dispersed in 8 mL of aquadest. Microemulgel 3,4-dimethoxychalcone, both HPMC and CMC-Na bases, had good homogeneity. The base viscosity of HPMC was 298700 ± 1212.44 cP, and the base CMC-Na was 87833.3 ± 351.2 cP. The pH value was 4.64 ± 0.01 (HPMC) and 6.40 ± 0.01 (CMC-Na), with adhesiveness > 1 second for both of them, but the spreadability was not good. Gel and microemulgel of 3,4-dimethoxychalcone had the ultraprotective ability against UVA exposure and protection against pigmentation (low% TP value) but were unstable under UVA exposure.

Kata Kunci : Kata kunci: 3,4-dimetoksikalkon, %TE, %TP, UV-A Protection Factor.