Rachmat Mauludin, Asti RAHAYU Satrialdi, Neng Fisheri Kurniati
Bedaquiline (BDQ), a poorly water-soluble drug, was successfully encapsulated in nanostructured lipid carriers (NLCs) to enhance its physicochemical properties. For the first time, BDQ-NLCs were optimized using a hybrid Taguchi and central composite design (CCD) methodology. This study selected cetyl palmitate, caprylic triglyceride, and Plantacare® 1200 in formulation development. The independent variables in this study, based on the Taguchi design approach, include the solid-liquid binary ratio, the surfactant concentration, and the sonication time. The dependent variables include particle size, encapsulation efficiency, and drug loading. The optimized BDQ-NLCs exhibited a particle size of 153.5 ± 2.3 nm, an encapsulation efficiency of 94.46 ± 0.09%, and a drug loading capacity of 3.04 ± 0.02%. The characterization of the optimum BDQ-NLCs revealed a zeta potential of -47.75 mV, a round particle morphology, and an endothermic event occurring between 45.94 and 54.60°C, indicating a transformation phase from solid to liquid. In vitro drug release profiles demonstrated that the optimized BDQ-NLCs formulation provides controlled and pH-dependent drug release, governed by a diffusion-driven mechanism. The stability evaluation of BDQ-NLCs demonstrated consistent stability under refrigerated conditions, while significant particle growth was observed at 25°C and 40°C, indicating temperature-dependent stability. Therefore, the developed BDQ-NLC formulation represents a physicochemically optimized system that may serve as a platform for further development of BDQ delivery, with therapeutic potential to be validated in future biological studies.
Department of Pharmaceutics, School of Pharmacy, Institut Teknologi Bandung, Bandung, Indonesia; Program Doctoral, School of Pharmacy, Institut Teknologi Bandung, Bandung, Indonesia; Department of Pharmaceutics, Faculty of Health Sciences, Universitas PGRI Adi Buana Surabaya, Indonesia; Department of Pharmacology and Clinical Pharmacy, School of Pharmacy, Institut Teknologi Bandung, Bandung, Indonesia
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