02762nas a2200205 4500008004100000245012900041210006900170260001800239300001400257490000700271520207900278653001702357653001402374653002902388653003002417100002202447700001902469700002802488856004002516 2021 eng d00aFormulation and Characterization of Bitter Melon (Momordica charantia Linn.) Fruit Fraction Loaded Solid Lipid Nanoparticles0 aFormulation and Characterization of Bitter Melon Momordica chara cNovember 2021 a1347-13540 v133 a

Background: The main active compound of bitter melon (Momordica charantia Linn.) fruit is charantin, which is believed to have important role on antihyperglycemic effect. However, charantin compound has a large molecular weight and is easily hydrolysed when given orally. Therefore, a colloidal drug delivery system, such as solid lipid nanoparticles (SLN), is required to provide a suitable and effective delivery of charantin, which is contained in a bitter melon fraction (BMF). Objective: This study aimed to prepare and evaluate SLN containing BMF with an appropriate characteristic for transdermal delivery. Methods: Bitter melon fruits were extracted with ionic liquid of [BMIM]BF4 using ultrasound-assisted extraction (UAE) and fractionated with dichloromethane. Four formulas of BMF loaded SLN were prepared with various ratio of BMF to surfactant and various ratio of lipids using high-shear homogenization followed by ultrasonication method. The obtained SLN were characterized, including morphology, particle size distribution, zeta potential, and entrapment efficiency. Furthermore, the stability study of BMF-loaded SLN was also conducted. Results: The result showed that BMF was a dry powder and brownish fraction with a specific smell. The BMF loaded SLN showed a spherical shape with the SLN F1 formula as a selected formula. The SLN F1 showed a particle size (Z-average) of 98.3±1.98 nm, polydispersity index of 0.26±0.01, zeta potential of -39.53±0.15 mV, and entrapment efficiency of 82.96±1.42 %. According to the stability study, it revealed that the BMF loaded SLN F1 had an acceptable stability, which the charantin content in the SLN was 96.52% after 3 months storage at 25°C ± 2°C. Conclusion: The BMF loaded SLN F1 with 1:12 ratio of BMF to surfactant and 1:2 ratio of capric caprylic triglyceride to glyceryl monostearate was selected as the best formula with the appropriate characteristics for transdermal delivery.

10aBitter melon10aCharantin10aMomordica charantia Linn10aSolid lipid nanoparticles1 aAnggraini, Rahayu1 aSurini, Silvia1 aSaputri, Fadlina, Chany uhttps://www.phcogj.com/article/1668