Development and Optimization of Roflumilast-loaded Nanostructured Lipid Carrier (NLCs) Formulation for Topical Delivery

The development of innovative drug delivery methods is essential to getting past the drawbacks of present pharmacological regimens, including fast metabolism, high toxicity, low solubility, and fluctuations in plasma drug levels. With fewer side effects and improved medication solubility, stability, bioavailability, and targeted delivery, nanostructured lipid carriers (NLCs) offer a viable alternative. The creation and improvement of Roflumilast-loaded NLCs, a phosphodiesterase-4 (PDE-4) inhibitor used to treat psoriasis, is the main topic of this work. A two-factor, three-level experimental design and Design Expert® software were used for creating eight formulation batches with varying quantities of oleic acid, Tween 80, and glyceryl monostearate (GMS). UV spectrophotometry, NMR, FTIR, DSC, XRD, particle size measurement, transmission electron microscopy (TEM), % entrapment efficiency (%EE), and in-vitro cumulative drug release (%CDR) were among the methods used to characterize the NLCs. With a particle size of 122.65nm, the polydispersity index (PDI) was 0.278 and the zeta potential of −20.16 mV, the optimized formulation (F3) demonstrated exceptional stability and uniformity. While FTIR and DSC analyses showed that Roflumilast and the excipients were compatible without causing significant chemical interactions, TEM investigation verified the spherical morphology and absence of aggregation. F3 had %EE and %CDR of 87.76% and 88.29%, respectively, demonstrating the effective drug encapsulation and release characteristics of the NLCs. XRD analysis verified that the medication was crystalline inside the lipid matrix. All things considered, the created Roflumilast-loaded NLCs show great promise for better medication delivery in dermatological applications, providing increased therapeutic efficacy and stability.