Indrati Oktavia, Martien Ronny, Rohman Abdul, Nugroho Akhmad Kharis
Department of Pharmacy, Faculty of Mathematics and Natural Sciences, Universitas Islam Indonesia, Sleman, Yogyakarta, Indonesia.
Department of Pharmaceutics, Faculty of Pharmacy, Universitas Gadjah Mada, Sekip Utara, Yogyakarta, Indonesia.
J Pharm Bioallied Sci. 2020 Nov;12(Suppl 2):S816-S820. doi: 10.4103/jpbs.JPBS_174_20. Epub 2020 Nov 5.
Andrographolide is a compound that shows various pharmacological activities, which can be applied topically or orally. Nanoemulsion can improve drug solubility and stability, but has limitations for topical application. Incorporation of nanoemulsion into hydrogel can increase the viscosity of the system which can prolong the drug residence time. The aim of this study was to develop andrographolide nanoemulsion-based hydrogel for topical application.
Andrographolide nanoemulsion was prepared using Capryol 90 as the oil, Kolliphor RH 40 as the surfactant, and propylene glycol as the cosurfactant. Droplet size and polydispersity index of the nanoemulsions were evaluated using particle size analyzer. D-optimal mixture design was employed to generate the total number of runs (formulation), and obtain the optimum formulation. Fourteen formulations of nanoemulsion-based hydrogel were prepared by incorporating nanoemulsion into the hydrogel base (1:1). Carbopol was employed as the gelling agent, whereas other excipients including propylene glycol, oleic acid, triethanolamine, methylparaben, and propylparaben were also added to produce hydrogel base. Nanoemulsion-based hydrogel was evaluated for its pH, viscosity, and physical appearance (after 8 weeks of storage).
The result revealed that nanoemulsion-based hydrogel containing 34.65% of carbopol, 1.35% of triethanolamine, and 9% of propylene glycol was selected as an optimum formulation which shows acceptable pH, viscosity, and physical appearance. This optimum nanoemulsion-based hydrogel has pH of 6.50 ± 0.02, and 2492.33 ± 36.91 cP of viscosity with milky white color, and smooth homogeneous texture.
This study suggested that andrographolide can be successfully formulated into an acceptable nanoemulsion-based hydrogel.
穿心莲内酯是一种具有多种药理活性的化合物,可局部或口服应用。纳米乳内酯。纳米乳剂可提高药物溶解度和稳定性,但局部应用存在局限性。将纳米乳剂掺入水凝胶中可增加体系粘度,从而延长药物停留时间。本研究的目的是开发用于局部应用的穿心莲内酯纳米乳剂基水凝胶。
以辛酸癸酸甘油三酯为油相、聚氧乙烯氢化蓖麻油RH40为表面活性剂、丙二醇为助表面活性剂制备穿心莲内酯纳米乳剂。使用粒度分析仪评估纳米乳剂的液滴大小和多分散指数。采用D-最优混合设计确定实验次数(配方),并获得最佳配方。通过将纳米乳剂与水凝胶基质(1:1)混合制备了14种纳米乳剂基水凝胶配方。使用卡波姆作为凝胶剂,同时添加其他辅料如丙二醇、油酸、三乙醇胺、甲基对羟基苯甲酸酯和丙基对羟基苯甲酸酯来制备水凝胶基质。对纳米乳剂基水凝胶的pH值、粘度和外观(储存8周后)进行评估。
结果表明,含有卡波姆34.65%、三乙醇胺1.35%和丙二醇9%的纳米乳剂基水凝胶被选为最佳配方,其pH值、粘度和外观均可接受。这种最佳纳米乳剂基水凝胶的pH值为6.50±0.02,粘度为2492.33±36.91 cP,呈乳白色,质地均匀光滑。
本研究表明穿心莲内酯可成功制备成可接受的纳米乳剂基水凝胶。