Deferasirox Nanosuspension Loaded Dissolving Microneedles for Intradermal Delivery

Abstract

Microneedles are minimally invasive systems that can deliver drugs intradermally without pain and bleeding and can advantageously replace the hypodermal needles and oral routes of delivery. Deferasirox (DFS) is an iron chelator employed in several ailments where iron overload plays an important role in disease manifestation. In this study, DFS was formulated into a nanosuspension (NSs) through wet media milling employing PVA as a stabilizer and successfully loaded in polymeric dissolving microneedles (DMNs). The release studies for DFS-NS clearly showed a threefold increased dissolution rate compared to pure DFS. The mechanical characterization of DFS-NS-DMNs revealed that the system was sufficiently strong for efficacious skin penetration. Optical coherence tomography images confirmed an insertion of up to 378 µm into full-thickness porcine skin layers. The skin deposition studies showed 60% drug deposition from NS-DMN, which was much higher than from the DFS-NS transdermal patch (DFS-NS-TP) (without needles) or pure DFS-DMNs. Moreover, DFS-NS without DMNs did not deposit well inside the skin, indicating that DMNs played an important role in effectively delivering drugs inside the skin. Therefore, it is evident from the findings that loading DFS-NS into novel DMN devices can effectively deliver DFS transdermally.

A Novel Combined Dry Powder Inhaler Comprising Nanosized Ketoprofen-Embedded Mannitol-Coated Microparticles for Pulmonary Inflammations: Development, In Vitro–In Silico Characterization, and Cell Line Evaluation

“…PVA is a polymer used as a stabilizing agent in media milling. It reduces the cohesive forces between the milled particles and can enhance the lung deposition upon respiration [ 80 , 81 ]. SDS is a popular anionic surfactant used in the creation of core–shell nanoparticles, and it maintains the electrostatic stability during the milling process [ 33 , 82 , 83 ], so it was combined with the PVA in milling process.…”

Calcipotriol Nanosuspension-Loaded Trilayer Dissolving Microneedle Patches for the Treatment of Psoriasis: In Vitro Delivery and In Vivo Antipsoriatic Activity Studies

“…28 , 29 This method can be applied to small sample sizes and provides advantages in early drug development and industrial pharmaceutical production. 29 − 31 …”

Nanosuspension-Based Dissolvable Microneedle Arrays to Enhance Diclofenac Skin Delivery

“…However, this particular class of MNAs usually shows a limited drug loading capability, especially with hydrophobic drugs [ 21 , 22 ]. To overcome this issue, the nanocrystal technology can be exploited to obtain homogeneous polymeric dispersion with high concentration of poorly water-soluble drugs for the preparation of MNAs [ 23 , 24 ]. In this study, a DCF-NS was prepared with a wet ball media milling technique and then used to prepare Polyvinylpyrrolidone (PVP)-based dissolving MNAs (DCF-NS-MNAs), with needle lengths of 500 and 800 µm.…”