Prospects for Improved Systemic Administration of Nimodipine Via Transdermal Dissolving Microneedles Loaded Nanoparticles
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Keywords

cerebral aneurysms
nimodipine
carboxymethyl cellulose
nanoparticle
transdermal

How to Cite

Prospects for Improved Systemic Administration of Nimodipine Via Transdermal Dissolving Microneedles Loaded Nanoparticles. (2024). African Journal of Biomedical Research, 27(3S), 2567-2575. https://doi.org/10.53555/AJBR.v27i3S.2728

Abstract

Nimodipine has been approved by FDA with a therapeutic use to prevent subarachnoid hemorrhage (SAH) and ruptured cerebral aneurysms. The purpose of this study was to develop a noninvasive and painless delivery system that improves low solubility and lowers oral bioavailability resulting from extensive first pass metabolism. This system would help with frequent dosing, inconsistent clinical responses, and poor patient compliance by utilizing a combination of polymeric nanoparticles (NP) and microneedles to create nimodipine as a polymeric nanoparticle incorporated in a dissolving microneedle(DMN)patch.  Using the solvent antisolvent process, the nimodipine NPs formula was created with a drug-to-polymer ratio of 1:8 (Soluplus®) and 1% Tween 80. The formula was evaluated by calculating the entrapment efficiency (%EE), particle size[PS], zeta potential and polydisperse index (PDI).Morphological study was determined through Field Emission-Scanning Electron Microscope(FE-SEM) .The results revealed a spherical shape with  PS (81.86 nm),%EE (84.84) and PDI (0.053) with 98 % of drug released in 45min  were observed. Micro molding in polydimethylsiloxane (PDMS) molds was used to create the dissolved microneedles (DMNs) from the formula using water soluble polymer carboxymethylcellulose (5% CMC) that are either used alone or  in conjunction with polyvinyl alcohol(PVA) and glycerin as plasticizers . The optimal MN formula was evaluated by measuring weight variation ,thickness, drug content, surface pH, mechanical strength, penetration test and stability study . There was a significant level of resistance observed in mechanical and insertion experiments. Results showed that nimodipine-NP-DMNs increased transdermal delivery of NID with noninvasive, pain free MNs with improving the solubility and release, decreased first pass effect resulting in enhanced patient compliance, and decreased side effects.

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