Quality by Design of Pranoprofen Loaded Nanostructured Lipid Carriers and Their Ex Vivo Evaluation in Different Mucosae and Ocular Tissues

Abstract

Transmucosal delivery is commonly used to prevent or treat local diseases. Pranoprofen is an anti-inflammatory drug prescribed in postoperative cataract surgery, intraocular lens implantation, chorioretinopathy, uveitis, age-related macular degeneration or cystoid macular edema. Pranoprofen can also be used for acute and chronic management of osteoarthritis and rheumatoid arthritis. Quality by Design (QbD) provides a systematic approach to drug development and maps the influence of the formulation components. The aim of this work was to develop and optimize a nanostructured lipid carrier by means of the QbD and factorial design suitable for the topical management of inflammatory processes on mucosal tissues. To this end, the nanoparticles loading pranoprofen were prepared by a high-pressure homogenization technique with Tween 80 as stabilizer and Lanette® 18 as the solid lipid. From, the factorial design results, the PF-NLCs-N6 formulation showed the most suitable characteristics, which was selected for further studies. The permeability capacity of pranoprofen loaded in the lipid-based nanoparticles was evaluated by ex vivo transmucosal permeation tests, including buccal, sublingual, nasal, vaginal, corneal and scleral mucosae. The results revealed high permeation and retention of pranoprofen in all the tissues tested. According to the predicted plasma concentration at the steady-state, no systemic effects would be expected, any neither were any signs of ocular irritancy observed from the optimized formulation when tested by the HET-CAM technique. Hence, the optimized formulation (PF-NLCs-N6) may offer a safe and attractive nanotechnological tool in topical treatment of local inflammation on mucosal diseases.

A Novel Approach for Dermal Application of Pranoprofen-Loaded Lipid Nanoparticles for the Treatment of Post-Tattoo Inflammatory Reactions

“…PRA-loaded NLC were formulated and optimized using a 2 3 central composite rotatable factorial design. This formulation was prepared via a high-pressure homogenization technique (Figure 1), as described previously [26,28]. The composition formula of PRA-NLC is shown in Table 1.…”

“…The prepared PRA-NLC batches were allowed to se le at room temperature for at least 10 h before further assays. The prepared formulation was characterized physicochemically for mean particle size, polydispersity index, zeta potential, and encapsulation efficiency percentage [26]. The Zetasizer Nano ZS was used to determine the particle size, its distribution (polydispersity index), and the zeta potential.…”

“…The encapsulation efficiency (EE %) of pranoprofen in the nanoparticles was evaluated by the indirect method which consists of measuring the concentration of the drug in the medium; that is, the unencapsulated drug. The unencapsulated pranoprofen was isolated via centrifugation using Ultracel-100K centrifugal filters (Amicon Ultra, Millipore The prepared formulation was characterized physicochemically for mean particle size, polydispersity index, zeta potential, and encapsulation efficiency percentage [26]. The Zetasizer Nano ZS was used to determine the particle size, its distribution (polydispersity index), and the zeta potential.…”

“…In previous studies of our research group, a formulation of PRA-loaded NLC (PRA-NLC) was optimized, prepared by the high-pressure homogenization technique, and physiochemically characterized [26]. Considering that post-tattoo care with an appropriate product is essential to relieve pain, promote skin repair, and, consequently, improve the aesthetic appearance of the tattoo, the present work aimed at investigating the potential use of this lipoidal nanocarrier for the topical delivery of PRA as a tattoo aftercare formulation to reduce inflammation associated with tattooing.…”

Recent Progress of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers as Ocular Drug Delivery Platforms

“…Various nanoscale drug delivery systems, such as liposomes [ 22 , 23 ], niosomes [ 24 , 25 ], solid lipid/polymeric nanoparticles [ 26 , 27 , 28 , 29 ], nanostructured lipid carriers [ 30 , 31 ], nanomicelles [ 32 , 33 ], microemulsions [ 34 , 35 ], and dendrimers [ 36 ], have been successfully developed for ocular delivery purposes, and have been reported to achieve enhanced bioavailability, sustained and controlled drug release, and a reduction in the number of applications, as well as side effects. SLNs and NLCs raise great interest due to their excellent biocompatibility and tolerability, tunable physiochemical characteristics, and scaling-up capabilities [ 37 , 38 , 39 ].…”